Reagenti sintetici

<p>Applications MKT-077 is used in the treatment of Alzheimer’s diseases and other tauopathie’s. Also, is a rhodacyanine derivative that selectively targets cancer cells and overcomes tamoxifen resistance<br>References Jinwal, U. K., et al.: Pharm. Nanotechnol., 2, 217, (2014); Koren, J., et al. : PLoS One, 7, 35566 (2012)<br></p>

<p>Applications Tocainide Hydrochloride is used as an anti-arrythmic drug as myocardial depressants.<br>References Courtney, K. et al. J. Molec. Cell. Cardiol., 12, 1273 (1980); Kwok, D. et al.: Res. Comm. Chem. Path. Pharm., 67, 395 (1990);<br></p>

<p>Applications Ethyl Isobutyrylacetate is used in the synthesis of piperazine derivatives as possible multireceptor atypical antipsychotics, affecting dopamine and serotonin receptor properties . Also used in the synthesis of pyrazinecarboxamide DGAT1 (diacylglycerol acyltransferase 1) inhibitors used in the treatment of obesity.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Chen, Y. et al.: J. Med. Chem., 56, 4671 (2013); J. Med. Chem., 55, 10610 (2012);<br></p>

<p>Applications Savolitinib is a potent and highly selective c-Met inhibitor. Savoltinib demonstrated anti-tumor efficacy in a panel of cMet-dysregulated gastric cancer PDX models. Savolitinib also demonstrated good antitmuor activities.<br>References Gavine, P., et al.: Mol. Oncol., 9, 323 (2015); Jia, H., et al.: J. Med. Chem., 57, 7577 (2014);<br></p>

<p>Applications AZD 6244 and MK 2206 are targeted small-molecule drugs that inhibit MEK and AKT responses. The combination of AZD6244 and MK2206 has a significant synergistic effect on tumor growth in vitro and in vivo and leads to increased survival rates in mice bearing highly aggressive human lung tumors. Antitumor agents. Potent AKT inhibitor.<br>References Yeh, T., et al.: Clin. Cancer Res., 13, 1576 (2007), Meng, J., et al.: Cancer Biol. Ther., 8, 2073 (2009),<br></p>

<p>Applications 2,2-Difluoro-1,3-benzodioxole is used in the synthesis of Kv3 inhibitors as well as in the preparation of renin inhibitors.<br></p>

<p>Applications Alk 5 Inhibitor II is a selective ATP competitive inhibitor of transforming growth factor-β (TGFβ). A potential drug for the treatment of fibrosis and cancer.<br>References Ren, J. et al.: Eur. J. Med. Chem., 44, 4259 (2009)<br></p>

<p>Applications Ammonium Bicarbonate is a useful reagent in the synthesis of double-shelled CoMn2O5 hollow microcubes used as anode material for lithium-ion batteries.<br>References Zhou, L., et al.: Adv. Mater., 24, 745 (2012);<br></p>

<p>Applications Iproniazid is a hydrazine based drug used as an antidepressant. Iproniazid acts as an irreversible and nonselective monoamine oxidase inhibitor.<br>References Fagervall, I. et al.: Biochem. Pharmacol., 35, 1381 (1986); Horita, A.: Princ. Psychopharmacol., 279 (1970); O'Donnell, J.M. et al.: Psychopharmacology, 78, 214 (1982);<br></p>

<p>Applications IWP-2 is an inactivator of Porcn function; inhibitor of Wnt production. IWP-2 is useful in the treatment diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.<br>References Poss, K., et al.: Dev. Biol., 222, 347 (2000), Tanaka, K., et al.: Eur. J. Biochem., 267, 4300 (2000), Clevers, H., et al.: Cell, 2006, 127, 469 (2006),<br></p>

<p>Applications Tributylhexadecylphosphonium Bromide (CAS# 14937-45-2) is a dynamic compound used as a surface modifier for thermal properties of palygorskite, an additive in water to improve resistance of epoxy-anhydride matrices, and as a modifier of phenolic resin to improve thermal degradation.<br>References Cisneros-Rosado, D. E.; et al.: Polym. Compos., 39, E1531 (2018).; Capiel, G.; et al.: Polym. Adv. Technol., 28, 886 (2017); Asaro, L.; J. Therm. Anal. Calorim., 128, 1463 (2017).<br></p>

<p>Applications A useful synthetic intermediate. Used for asymmetric hydroxylation.<br>References Davis, F.A., et al.: J. Am. Chem. Soc., 112, 6679 (1990)<br></p>

<p>Applications Dimethyl Acetylenedicarboxylate is a biocide that is added to biodiesels to inhibit and remove microbial growth. It can rapidly penetrate the skin and cause aberrations in the activities of the glycogenic, lipogenic, and tricarboxylic acid metabollic pathways. It also causes delayed and pain-free dermal burns.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Poon, R., et al.: Arch. Toxicol., 85(11), 1419-1427 (2011); Klain, George J., et al.: Fund. Appl. Toxicol., 10(4), 730-5 (1988); Slovak, A. J. M., et al.: Contact Dermatitis, 11(1), 29-30 (1984)<br></p>

<p>Impurity Atomoxetine EP Impurity D<br>Applications m-Methyl Atomoxetine Hydrochloride (Atomoxetine EP Impurity D) is an impurity of Atomoxetine (A791400), a norepinephrine reuptake inhibitor.<br>References Farid, N.A., et al.: J. Clin. Pharmacol., 25, 296 (1985), Gehlert, D.R., et al.: J. Neurochem., 64, 2792 (1995), Hwamg. et al.: Neurosci. Lett., 265, 151 (1999), Ring, B.J., et al.: Drug Metab. Dispos., 30, 319 (2002),<br></p>

<p>Stability Light Sensitive, Volatile<br>Applications 1,5-Hexadien-3-ol is a reactant used in the synthesis of laurencia metabolite obtusenye.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Crimmins, M.T., et al.: J. Am. Chem. Soc., 125, 7592-7595 (2003)<br></p>

<p>Applications Platinum(0)-1,3-divinyl-1,1,3,3-tetramethyldisiloxane Complex Solution is a catalyst in the preparation of phenol functional silanes which are used as adhesion promoters.<br>References Amako, M., et al.: From Eur. Pat. Appl. (2000), EP 1041076 A2 20001004<br></p>

<p>Stability Light Sensitive<br>Applications (S)-β-Pinene is a monoterpene that naturally occur in various plants. Due to its pine-like smell, its been used as a major constituent of hop aroma and flavor.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Li, Jingyi., et la.: J. Neurochem., 121, 881 (2012); Wu, J., et al.: J. Med. Plants. Res., 6, 2832 (2012);<br></p>

<p>Applications (S)-(+)-Benzyl Glycidyl Ether is used as a reactant in the synthesis of (+)-Discodermolide.<br>References Smith, A.B. et al.: J. Am. Chem. Soc., 122, 8654 (2000);<br></p>

<p>Applications trans-2,5-Dimethylpiperazine is a C-alkyl substituted piperazine used in the preparation of opioid receptor ligands as well as other biologically active compounds.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Janetka, J.W. et al.: J. Org, Chem., 68, 3976 (2003);<br></p>

<p>Applications 4-Hydroxy-3,5-dimethylbenzoic Acid is used in the synthesis of Mexiletine (M340800) derivatives as orally bioavailable inhibitors. Also, used as a chemical reagent in the preparation of potent transthyretin (TTR) amyloidogenesis inhibitors affecting thyroid hormone.<br>References Frederickson, M. et al.: J. Med. Chem., 51, 183 (2008); Johnson, S. et al.: J. Med. Chem., 51, 260 (2008);<br></p>

<p>Applications TAE 684 is a potent, selective, and efficacious inhibitor of NPM-ALK, a fusion protein that is a key regulator of oncogenic events that drives the survival and proliferation of anaplastic large-cell lymphomas. Potent ALK inhibitor<br>References Schoenherr, C., et al.: Oncogene., 31, 5193 (2012); Tanizaki, J., et al.: Clin. Cancer. Res., 18, 6219 (2012); Heuckmann, J.M., et al.: Clin. Cancer. Res., 18, 4682 (2012);<br></p>

<p>Applications Tetraethyl Orthocarbonate is used in the synthesis of chemokine receptor-5 inhibitors against HIV-1. Also used in the synthesis of benzobisoxazoles used in the preparation of organic semiconductors.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Kazmierski, W. et al.: J. Med. Chem., 54, 3756 (2011); Mike, J. et al.: Org. Lett., 10, 4915 (2008);<br></p>

<p>Applications 1,4-Diazabicyclo[2.2.2]octane is an aliphatic amine that is used as a catalyst in organic synthesis.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Baghernejad, B.: Eur. J. Chem., 1, No pp. given (2010); Guzonas, D., et al.: Langmuir, 6, 11002 (1990)<br></p>

<p>Applications Ixazomib is a proteasome inhibitor that acts by preventing cell growth in solid tumours. It is an anticancer agent that is used to treat patients with multiple myeloma and is potentially neurotoxic.<br>References Anderson, K.: J. Nat. Comp. Canc. Net., 12, 808 (2014); Chattopadhyay, N., et al.: Mol. Cancer Ther., 12, B156 (2013); Vallet, S. &amp; Podar, K.: Exp. Opin. Biol. Ther., 13, S35 (2013)<br></p>

<p>Applications 6-Quinolinol is used in the preparation of potential antifungal agents containing a quinoline structure. Also used in the preparation of novel pyridocoumarins.<br>References Galariniotou, E. et al.: Tetrahedron 63, 8298 (2007); Vandekerckhove, S. et al.: Bioorg. Med. Chem. Lett., 23, 4641 (2013);<br></p>

<p>Stability Moisture Sensitive<br>Applications Heptanoyl Chloride is used in the synthesis of novel class of 2-Aminopyrimidines as CDK1 and CDK2 inhibitors.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Samanta, R., et al.: Org. Lett., 14, 5518 (2012); Sabbah, M., et al.: Bioorg. Med. Chem., 20, 4727 (2012);<br></p>

<p>Stability Very Hygroscopic<br>Applications Labelled Plerixafor, it is a hematopoietic stem cell (HSC) mobilizer that inhibits the CXCR4 chemokine receptor and blocks binding of its ligand, stromal cell-derived factor-1-α (SDF-1-α). This agent was approved on Dec. 15, 2008, as treatment in combination with granulocyte-colony stimulating factor (G-CSF) to mobilize HSCs to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM).<br>References Xie, T., et al.: Science, 290, 328 (2000), Leone, D., et al.: J. Pharmacol. Exp. Ther., 305, 1150 (2003), Chigaev, A., et al.: J. Immunol. 178, 6828 (2007), Kiel, M., et al.: Cell Stem Cell, 1, 204 (2007),<br></p>

<p>Applications (R)-Ethyl 4-chloro-3-hydroxybutanoate is used in biological studies for asymmetric reduction of ethyl 4-chloro-3-oxobutanoate to ethyl (R)-4-chloro-3-hydroxybutanoate with two co-existing, recombinant Escherichia coli strains.<br>References Liu, Y., et al.: Biotech. Lett., 27, 119 (2005);<br></p>

<p>Stability Unstable in Solution<br>Applications 2-Pyrimidineacetic acid is a reagent that is used in the preparation of pyrimidine derivatives for treating and or preventing sexual dysfunction.<br>References Huang, Z., Faming Zhuanli Shenqing, 2012:400114<br></p>

<p>Applications Acetylhistamine, is a histamine metabolite, and can be used as a potential biomarker of histidine metabolism for anaphylactoid reactions.<br>References Xu Y, et al. Asian Pac J Allergy Immunol. 2017 Dec;35(4):224-232.;<br></p>

<p>Applications (-)-DIBENZOYL-L-TARTARIC ACID MONOHYDRATE (cas# 62708-56-9) is a useful research chemical.<br></p>

<p>Applications (S)-(-)-2-Chloropropionic Acid (cas# 29617-66-1) is a compound useful in organic synthesis.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br></p>

<p>Applications BAY 11-7085 is a NF-κB (nuclear factor-κB) inhibitor and can be used as a therapeutic agent for the treatment of endometriosis. BAY 11-7085 inhibits the cell proliferation and DNA synthesis of endometriotic cyst stromal cells (ECSCs) and induces apoptosis by surpressing antiapoptotic proteins.<br>References Berger, N., et al.: Exp. Hematol., 35, 1495 (2007); Nasu, K., et al.: Am. J. Physiol., 293, E16 (2007)<br></p>

<p>Applications 2-(2-Boc-aminoethoxy)ethanol is a reactant that has been used in the synthesis of RGD-conjugated MEK1/2 kinase inhibitors for integrin-targeted cancer therapy.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Li, X., et. al.: Molecules, 18, 13957 (2013)<br></p>

<p>Applications An Aurora kinase inhibitor, used to treat patients with advanced solid tumors.<br>References Carlson, H., et al.: Mol. Pharmacol., 57, 213 (2000), Hou, T., et al.: Curr. Pharm. Des., 10, 1011 (2004), Verdonk, M., et al.: J. Med. Chem., 48, 6504 (2005),<br></p>

<p>Applications Methyl 8-Chloro-8-oxooctanoate is used as a reagent in the synthesis of β-cyclodextrin-6-deoxy-6-NHC(O)(CH2)6C(O)NHOH which is a β-cyclodextrin-capped histone deacetylase inhibitor that may have potential for use in treatment of cancers and inflammatory diseases. It is also used in one synthetic route for tubacin which is a known anticancer agent.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Amin, J., et al.: Bioorg. Med. Chem. Lett., 23, 3346 (2013); Hong, J., et al.: Lett. Org. Chem., 7, 50 (2010);<br></p>

<p>Applications Sodium Metasilicate is an antibacterial pharmaceutical compound containing Sodium Hydrogen Carbonate.<br>References Karaagac, M., et al.: Turk. Pat. Appl., (2017);<br></p>

<p>Applications Aclidinium Bromide is a novel long-acting antimuscarinic bronchodilator in phase II clinical trials for the treatment of chronic obstructive pulmonary disease (1,2).<br>References (1) Gupta, V. and Singh, D.: Expert Rev Respir Med. 6, 581 (2012) (2) De La Motte, S., et al.: Int. J. Clin. Pharmacol. Therap., 50,403 (2012)<br></p>

<p>Applications Cyclopropylacetylene is used in a variety of chemical reactions in organic syntheses. Used in the synthesis of BACE1 inhibitors used in the treatment of Alzheimer’s disease. It is also used in cycloaddition reactions and the synthesis of fluoromethylsydnones.<br>References Xu, Y. et al.: Bioorg. Med. Chem. Lett., 23, 3075 (2013); Foster, R. et al.: J. Org. Chem., 78, 4049 (2013);<br></p>

<p>Stability Hygroscopic<br>Applications 3-(2-Benzothiazolyl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-1-benzopyran-4-one is involved in the pharmacological inactivation of Skp2 E3 ligase.<br>References Chan, C., et al.: Cell, 154, 556-568 (2013)<br></p>

<p>Applications 5-Chloropent-1-yne is an intermediate in the synthesis of Efavirenz (E425000), a nonnucleoside HIV-1 reverse transcriptase inhibitor. Antiviral.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Young, S.D., et al.: Antimicrob. Ag. Chemother., 39, 2602 (1995)<br></p>

<p>Applications 2-(1,3-Dioxolan-2-yl)ethyltriphenylphosphonium Bromide (cas# 86608-70-0) is a useful research chemical.<br></p>

<p>Applications 4-Formyl-2-nitrophenol is an Intermediate used in synthesis of novel amodiaquine analogs as potential antimalarial and antifilarial compounds.<br>References Jiang, D.X., et al.: Int. J. Environ. Res., 5, 923 (2011); Al-Zereini, W., et al.: J. Antibiotic., 63, 297 (2010);<br></p>

<p>Applications 3,5-Dibromobenzaldehyde is a dibrominated benzaldehyde that is a very useful building block for the preparation of a wide range of biologically active compounds such as a antibacterials<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Nielsen, S. et al.: Bioorg. Med, Chem., 12, 3017 (2004); Balderamos, M. et al.: Exp. Biol. Med., 233, 1395 (2008);<br></p>

<p>Stability Hygroscopic<br>Applications Ethoxyamine Hydrochloride acts as a reagent in the preparation of biflorin derivatives (hydrazones, oximes, terpene ketones) and determination of their activity as antibacterial and anticancer agents.<br>References Souza, L. G., et al.: Bioorg. Med. Chem. Lett., 26, 435 (2016)<br></p>

<p>Applications 4-Bromobenzotrifluoride is an aromatic compound that is used as a reagent to synthesize Bergenin (B318650), a compound that originates in Mallotus japonicus that exhibits hepatoprotective and antioxidant effects. 4-Bromobenzotrifluoride is also used as a reagent to prepare (±)-Preclamol, a partial dopamine D2 agonist that is used to treat Parkinson’s disease.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Lim, H., et al.: Pharmacology, 63, 71 (2001); Parkan, K., et al.: Chem. Eur. J., 20, 4414 (2014); Pirtosek, Z., et al.: Clin. Neuro., 16, 550 (1993); Takahashi, H., et al.: Bioorg. Med. Chem., 11, 1781 (2003); Vasdev, N., et al.: Synapse, 60, 314 (2006)<br></p>

<p>Applications SKF 81297C is a dopamine D1 agonist (1).<br>References (1) Bergman, J., et. al.: J. Pharmacol. Exp. Ther., 273, 40 (1995)<br></p>

<p>Applications Copper(II) Chloride Dihydrate is a substance used in the release of copper complexes from a nanostructured sol-gel titania for cancer treatment. Also in the solubilization of thymol in Tween 80 micelle to study solubilization mechanism of thymol and effect of solubilization on its antioxidant activity.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Deng, L., et al.: Scientific Reports, 6, 38160 (2016); Lopez, T., et al.: J. Mater. Sci., 50, 2410 (2015)<br></p>

<p>Applications Ammonium Vanadium Oxide is used in pharmaceutical composition of metformin decavanadate for prevention and treatment of metabolic syndrome, obesity and diabetes. Chimeric design, synthesis, and biological assays of new nonpeptide insulin-mimetic vanadium compounds to inhibit protein tyrosine phosphatase 1B.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Scior, T., et al.: Drug Des. Devel. Ther., 4, 231 (2010); Gonzalez V., et al.: Pat. Appl. (2016), MX 2015003461 A 20160919;<br></p>

<p>Applications Bismuth Citrate is a reagent used in the preparation of nano-array wires and nanotubes. Also used in the preparation of collidal bismuth subcitrate with ulcer healing properties.<br>References Chen, R. et al.: Chem. Commun (Camb)., 21, 2265 (2006); Asato, E. et al.: Inorg. Chem., 34, 2447 (1995);<br></p>

<p>Applications (R)-3-(Boc-amino)piperidine is Boc protected (R)-3-Aminopiperidine (A627920, Dihydrochloride salt) which has been used as a reactant for the preparation of dipeptidyl peptidase IV inhibitors derived from Alogliptin.<br>References Xie, Hui., et. al.: Eur. J. Med. Chem., 68, 312 (2013)<br></p>

<p>Applications Trimethylphenylammonium tribromide is a brominating agent, and is also used as an oxidizing agent in the preparation of disulfides and sulfoxides from thiols and sulfides.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Ghorbani-Choghamarani, A., et al.: Phosphorus Sulfur, 186, 1665 (2011); Gonzalez, A., et al.: Phytochemistry, 12, 1113 (1973)<br></p>

<p>Stability Hygroscopic<br>Applications PHA-793887 is a potent CDK (cyclin-dependent kinase) inhibitor. Recent studies shows that PHA-793887 has promising therapeutic activity against acute leukemias in vitro and in vivo. PHA-793887 was used to successfully modulate E2F transcriptional factor-dependent cell cycle, DNA replication, mitosis and apoptosis related gene in both tumors and skin biopsy from patients with solid tumors.<br>References Alzani, R. et al.: Exp. Hematol., 38, 259 (2010); Locatelli, G. et al.: Mol. Cancer Ther., 9, 1265 (2010); Brasca, M. et al.: Bioorg. Med. Chem., 18, 1844 (2010);<br></p>

<p>Applications Methyl Dimethoxyacetate is used as a reagent in the synthesis of benzimidazole derivatives for use as respiratory syncytial virus inhibitors.<br>References Cooymans, Ludwig Paul; D., et al. PCT Int. Appl. WO 2012080446 A1 20120621. Jun 21, 2012<br></p>

<p>Applications 2,6-Dichlorobenzyl Bromide is used in the preparation of potent epoxide hydrolase inhibitors. Has shown thus far to relieve hypotension in lipopolysaccharide deficient murine models. As well they have been used in the synthesis of anti-HIV drugs based on diaryltriazine (DATA) analogues.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Hwang, S. et al.: J. Med. Chem., 50, 3825 (2007); Ludovici, D. et al.: Bioorg. Med. Chem. Lett., 11, 2229 (2001);<br></p>

<p>Applications 18α-Glycyrrhetinic Acid rapidly and reversibly blocks gap junction intercellular communication (GJIC).<br>References Guo, Y., et. al.: Am. J. Phys.: 276, L1018 (1999)<br></p>

<p>Applications trans-2-[3-(4-tert-Butylphenyl)-2-methyl-2-propenylidene]malononitrile (cas# 300364-84-5) is a useful research chemical.<br></p>

<p>Applications WAY-100135 is a selective and potent 5-HT1A receptor antagonist.<br></p>

<p>Applications A metabolite of Cilostazol (C441500), used as internal standard.<br>References Akiyama, H., et al.: Arzneim.-Forsch./Drug Res., 35, 1133 (1985), Akiyama, H., et al.: J. Chromatogr., 338, 456 (1985),<br></p>

<p>Applications Diethyl L-(+)-Tartrate is used as a chiral reagent in a host of chemical reactions, such as the synthesis of isoquinoline alkaloids and arundic acid, which has been used in acute ischemic stroke therapy.<br>References Ziolkowski, M. et al.: Tetrahedron Lett., 41, 1963 (2000); Fernandes, R. et al.: Tetrahedron Lett. 50, 5903 (2009);<br></p>

<p>Applications D-Glyceraldehyde is the simplest of all aldoses and have been shown to be the one of the carbonyl metabolite of dietary fructose.<br>References Yang, K., et al.: Chem-Biol. Interact., 191, 315 (2011); Zheng, X.H., et al.: Chem. Med. Chem., 7, 1921 (2012);<br></p>

<p>Applications A phopshine ligand used in transition-metal mediated organic synthesis, in particular in wittig reactions to improved (Z) selectivity.<br>References Andersen N.G. et al.: Chem. Rev., 101, 997 (2001); Appel M. et al.: Eur. J. Org. Chem., 1143, (2002);<br></p>

<p>Applications VU0357017 is a subtype-selective M1 muscarinic acetylcholine allosteric agonist. VU0357017 has a potency of 200 nM and Achmax of 81% and had no activity at M2-M5 up to the highest concentrations tested and also had little or no detectable antagonist activity at any other mAChR subtype at concentrations over 2 orders of magnitude higher than those required to activate M1 or activity at a large panel of GPCRs, ion channels, and transporters. In contrast, TBPB inhibited responses to ACh at each of the other mAChR subtypes. VU0357017 was active in reversing cognitive deficits induced by Scopolamine (S200000) in a preclinical rodent model.<br>References Bridges, et al.: Bioorg. Med. Chem. Lett., 20, 1972 (2010); Lebois, et al.: ACS Chem. Neurosci., 1, 104 (2010),<br></p>