Quinazoline and Quinoline Derivatives

<p>MMP2-IN-3 is a potent inhibitor of matrix metalloproteinases (MMP-2) (IC50: 31 μM).</p>

<p>Ezetimibe ketone is a lipid-lowering agent that inhibits cholesterol absorption through the inhibition of Niemann-Pick C1-like 1 (NPC1L1). Ezetimibe ketone is used to reduce the levels of low-density lipoprotein cholesterol (LDL-C) in patients with primary hypercholesterolemia, sitosterolemia, and familial combined hyperlipidemia. Ezetimibe ketone has been shown to be bioequivalent to ezetimibe, which is an oral drug that inhibits cholesterol absorption by blocking NPC1L1. The drug binds to the NPC1L1 receptor in the brush border membrane of enterocytes and prevents cholesterol uptake. Ezetimibe ketone has a high solubility in organic solvents such as dichloromethane or chloroform. It also has a high melting point, which makes it suitable for use on chromatographic columns.</p>

<p>Gemigliptin (LC15-0444) is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor(KD : 7.25 nM.)</p>

<p>Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.</p>

<p>Amlodipine EP Impurity F maleate is an impurity of amlodipine, a drug product. It is a natural substance that has been classified as an API impurity in the United States Pharmacopeia (USP). The chemical name for this drug is 3-(2-chlorophenyl)-1-methyl-5-(o-tolyloxy)-2,4-dihydro-6H-[1,3]thiazolo[3,2-a]pyrimidin-7-one. Amlodipine EP Impurity F maleate has the following properties: C12H9ClNO2S and a melting point of 210°C with a purity of 99.5%. This compound was synthesized by custom synthesis and is used as an analytical standard for HPLC. This compound was also used during the development of amlodipine to determine its metabolism studies.</p>

Ephedrine and its salts

Lactams, nesoi

<p>Please enquire for more information about 3-Trifluoroacetylamino linagliptin including the price, delivery time and more detailed product information at the technical inquiry form on this page</p>

<p>(Z)-Thiothixene (Thiothixene) is an antagonist of serotonergic receptor.</p>

<p>Cyamemazine is an antipsychotic compound with sedative and anxiolytic activity.Cyamemazine is a 5-HT3, 5-HT2A, and 5-HT2C receptor antagonist.</p>

<p>Linagliptin impurity G is an impurity in the drug product Linagliptin. It is a natural substance and its CAS number is 668270-11-9. Impurity G can be synthesized from L-phenylalanine and cyclohexane carboxaldehyde in a two step process. The first step involves the reaction of L-phenylalanine with cyclohexane carboxaldehyde to yield methylcyclohexanecarboxylate, which then undergoes hydrolysis to give phenylcyclohexanol. In the second step, phenylcyclohexanol reacts with hydrochloric acid to produce phenylcyclohexanone, which is then oxidized with hydrogen peroxide to yield impurity G. Impurity G can also be found in the pharmacopoeia as a high purity HPLC standard for linagliptin.</p>

<p>Pitavastatin N-oxide is a drug product that is an analytical standard and natural API impurity. It is used in the synthesis of other drugs, such as pitavastatin, which is a statin drug used to lower cholesterol levels. Pitavastatin N-oxide has been shown to be a potent inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) to mevalonate. This inhibits cholesterol production and lowers levels of low density lipoprotein (LDL) cholesterol in the blood.</p>

<p>Vildagliptin related compound F (VRCF) is a drug product that has been custom synthesized. VRCF is a high purity, analytical standard. It is metabolized in the body and can be used as a research and development standard to study the metabolism of vildagliptin. VRCF is a natural metabolite that has been identified as an impurity in the drug product Vildagliptin. VRCF has not been recognized by the USP or EP for use as an impurity standard. CAS no: 1789703-36-1</p>

<p>Givinostat HCl (ITF2357 HCl) inhibits HDAC1/3 (IC50: 198/157 nM) with anti-inflammatory, anti-angiogenic, and antineoplastic properties.</p>

<p>Ecopipam: orally active, selective dopamine D1/D5 antagonist (Ki: 1.2 nM/2.0 nM). 40x more selective over D2/D4/5-HT/α2a. For schizophrenia, obesity research.</p>

<p>MMP-2/MMP-9-IN-1: oral IV collagenase inhibitor; IC50: 0.24 μM (MMP-9), 0.31 μM (MMP-2); targets cancer.</p>

<p>Amiodarone impurity E is a nucleophilic compound that is synthesized by the acylation of a diazonium salt with an amine. It has been shown to be active against staphylococci, but not against subtilis. The reaction may be catalyzed by acid or chloride. Amiodarone impurity E is also demethylated and dehydrated to form the final product, amiodarone.</p>

<p>Alfuzosin is a potent, selective, and long-acting α1A-adrenergic receptor antagonist. It is used to treat benign prostatic hyperplasia (BPH) in males. Alfuzosin is also used as an antihypertensive agent, for the treatment of pheochromocytoma, and for the treatment of benign prostatic hyperplasia in males. The hydrogenation of 2,3,4,5-tetradehydroalfuzosin to alfuzosin hydrochloride is performed by liquid hydrogenation or by hydrogenation on a palladium catalyst in a mixture of dimethylformamide and hexamethylphosphoramide. This process minimizes the formation of impurities such as 2,3,4-trimethoxy alfuzosin.</p>

<p>Sovaprevir is a non-structural 3 (NS3) protease inhibitor with antiviral activity for the treatment of HCV infection.</p>

<p>Fluvalinate is a synthetic chemical compound and can be commonly used to control varroa mites in honey bee colonies.</p>

<p>MMP-7-IN-2 acts as a selective and potent MMP7 inhibitor and can be used to study inflammatory responses and vascular-related diseases.</p>

<p>FGIN-1-27 is a high-affinity agonist of the translocator protein and a specific peripheral benzodiazepine receptor (PBR) ligand(Ki = 5.0 nM).</p>

<p>Brasofensine, a benztoalkane MA reuptake inhibitor, shows promise for Parkinson's and Alzheimer's.</p>

<p>XL-784 free base selectively inhibits MMPs with IC50: MMP-1 (1.9µM), MMP-2 (0.81nM), MMP-3 (120nM), MMP-8 (10.8nM), MMP-9 (18nM), MMP-13 (0.56nM).</p>

<p>Ro 32-7315 is a selective inhibitor of ADAM17.</p>

<p>Z-PDLDA-NHOH is a potent, specific vertebrate collagenase inhibitor [1].</p>

<p>Ro 31-9790 is a synthetic inhibitor of metalloproteinase (MMP).</p>

<p>Thioquinapiperifil is a type of phosphodiesterase-5 (PDE-5) inhibitor found in dietary supplements.</p>

<p>ONO-4817 suppresses MMPs, limiting plaque progression and aortic hyperplasia in hyperlipidemic rabbits.</p>

<p>XL-784 is a selective MMP inhibitor with low IC50s for MMP-1,2,3,8,9,13, modulating extracellular matrix remodeling, tumor invasion, and metastasis in cancer.</p>

<p>PIM447 (LGH447) is a pan-PIM kinase inhibitor with anti-tumor and bone protective effects. PIM447 reduces the viability, and motility of HuH6 cell.</p>

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity.

<p>Dibenamine hydrochloride is a competitive and irreversible blocking agent of the β-adrenergic receptor.</p>

<p>Brilaroxazine (RP5063): multimodal dopamine/5-HT modulator, partial agonist at D2/D3/D4, 5-HT1A/2A, and antagonist at 5-HT2B/7.</p>

<p>Collagen proline hydroxylase inhibitor is an inhibitor collagen proline hydroxylase and useful for antifibrotic proliferative agents.</p>

<p>MMP3 inhibitor 1 is a potent and highly selective inhibitor of MMP-3 (IC50 of 1 nM).</p>

LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM).

<p>Pirtobrutinib: a selective, non-covalent BTK inhibitor effective against BTK C481 mutations, causing tumor regression in lymphoma models.</p>

<p>Zandelisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K)(p110δ, IC50 of 3.5 nM), and with antineoplastic activity.</p>

<p>Yonkenafil, a PDE5 inhibitor, may reduce stroke damage and aid in Alzheimer's treatment.</p>

<p>Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs)</p>

<p>MMP-7-IN-3 (compound 15) is a potent and selective MMP-7 inhibitor, inhibiting renal fibrosis in a unilateral ureteral obstruction mouse model.</p>

<p>Mefenidil (McN-2378), a selective cerebral vasodilator, was shown to increase CBF in healthy brains without stimulating O2 uptake in a dog anesthesia model.</p>

<p>Cipemastat is a competitive inhibitor of human collagenases 1, 2, and 3 (Kis: 3.0, 4.4, and 3.4 nM).</p>

<p>Matrix metalloproteinase-3 (MMP-3), also known as stromelysin-1, is a critical enzyme involved in tissue remodeling and repair through its role in degrading extracellular matrix proteins, facilitating cell migration. This enzyme has been implicated in various physiological processes including vascular remodeling associated with aneurysm formation, wound healing, the progression of atherosclerosis, and tumor initiation. MMP-3 inhibitor VIII, a cell-permeable sulfonamide-based hydroxamic acid, effectively inhibits MMP-3 by binding to its active site (Ki = 23 nM), thus blocking its enzymatic activity. Additionally, this inhibitor has been demonstrated to suppress the activity of mouse macrophage metalloelastase MME/MMP-12, with an IC50 value of 13 nM, highlighting its potential utility in research on tissue remodeling and disease processes involving MMPs.</p>

<p>Ritodrine (DU21220) is a β-adrenergic agonist as well as an effective uterine relaxant that can be used in arrest premature labor research[1] [2].</p>

<p>ICI 204448 is a potent and peripherally selective κ-opioid agonist.</p>

<p>TP0556351: potent MMP2 inhibitor with 0.2 nM IC50, reduces collagen in pulmonary fibrosis mice.</p>

<p>Naxagolide is a sustained release formulation. It is a dopamine agonist.</p>

<p>LY52 is a matrix metalloproteinase-2 inhibitor. It acts by suppressing tumor invasion and metastasis.</p>

<p>Cobimetinib racemate (Cobimetinib (racemate)) (GDC-0973 racemate) is a selective inhibitor of MEK.Cobimetinib racemate is also known as a mitogen-activated</p>

<p>Etidocaine Hydrochloride (W19053) is a long-acting anesthetic and a blocker of the voltage-gated sodium channel.</p>

<p>Quizalofop (Xylafop) is a reagent of biochemical.</p>

<p>MMP-145 is used as a protease inhibitor.</p>

<p>MMP13-IN-3 is an oral, selective MMP-13 inhibitor with IC50 of 1 nM, &gt;1000x selective, for osteoarthritis treatment.</p>

<p>ROCK2 inhibitor is a chemical compound associated with the therapeutic management of psoriasis.</p>

<p>Ubrogepant (MK-1602) is an antagonist of calcitonin gene-related peptide receptor that can be used in the acute treatment of migraine studies.</p>

<p>Pure antiestrogen that downregulates estrogen receptor expression</p>

<p>Gepirone is a 5-HT1A receptor agonist belonging to the buspirone family. Gepirone HCl possesses greater selectivity for the 5-HT1A receptor than SSRIs.</p>

<p>Saredutant (SR 48968) is a selective neurokinin-2 (NK2) receptor antagonist that inhibits neurokinin A by blocking NK2 receptor, antidepressant and anxiolytic.</p>

<p>Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human.</p>

<p>Gisadenafil (UK-369003) is a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM and prevents degradation of cGMP.</p>

<p>KB-R7785 is a novel ADAM12/MMP inhibitor improving heart function and insulin sensitivity by blocking HB-EGF and TNF-alpha.</p>

<p>Tianagliflozin, a sodium/glucose cotransporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.</p>

<p>Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective dopamine D2 receptor agonist with antihypertensive activity in vivo.</p>

<p>ND-378 is a potent and selective inhibitor of MMP-2 with no inhibition on MMP-9 and MMP-14.</p>

<p>Dothiepin (Dosulepin; Dothep), an antidepressant with sedative/anxiolytic properties, preferentially inhibits noradrenaline over serotonin uptake, enhancing</p>

<p>AZD-1656 is a glucokinase activator (GKA) that can cause dose-limiting hypoglycemia in normal animals used in embryofetal development studies and type 2</p>

<p>Levocarbastine: 2nd-gen H1 antagonist, treats allergic conjunctivitis, selective NTS2 neurotensin inhibitor.</p>

<p>Caroverine is a potential chemotherapeutical agent in HNSCC cell lines.</p>

<p>Bufuralol (Ro 3-4787) is a 尾-adrenergic receptor blocker with a certain degree of sympathomimetic effects and can be used to study cardiovascular diseases.</p>

<p>IK-862 is a selective TACE inhibitor with potential anti-inflammatory and anticancer activity for the study of neuritis.</p>

<p>Bufuralol hydrochloride is a potent, non-selective, orally active β-blocker with partial agonist effects and a CYP2D6 probe.</p>

<p>Frovatriptan, potent 5-HT 1B/D agonist, shows high cerebroselectivity and efficacy for migraine with aura.</p>

<p>(Rac)-Lonafarnib is a racemic FTase inhibitor, effective against H-ras, K-ras, N-ras (IC50: 1.9, 5.2, 2.8 nM), and has anti-HDV properties.</p>

<p>MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively).</p>

<p>Maralixibat Chloride (LUM001 chloride), an apical, sodium-dependent, bile acid transport inhibitor, prevents enterohepatic bile acid recirculation.</p>

<p>Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor indicated for the study of allergic asthma, COPD and pulmonary fibrosis.</p>

<p>1-(6-Chloro-9H-carbazol-2-yl)ethanone is a chemical substance that belongs to the class of synthetic drugs. It is used as a pharmaceutical intermediate in the production of other chemical substances, including antibiotics and antihypertensives. 1-(6-Chloro-9H-carbazol-2-yl)ethanone has been shown to be metabolized by cytochrome P450 enzymes and by glucuronidases or esterases. This product can also be used as an impurity standard for HPLC analyses of fluoroquinolones.</p>

<p>4-[(2RS)-2-Hydroxy-3-[(1-methylethyl)amino]propoxy]-benzaldehyde hydrochloride is a drug product. It is used as an analytical standard and in the development of drugs. The metabolite of 4-[(2RS)-2-Hydroxy-3-[(1-methylethyl)amino]propoxy]-benzaldehyde hydrochloride, 4-[(2RS)-2-hydroxy-3-[(1-methylethyl)amino]propoxy]-N-(4-nitrophenyl)benzamide, has been shown to inhibit the production of cytokines IL6 and TNFα by human monocytes, macrophages, and dendritic cells. Metabolism studies have shown that 4-[(2RS)-2-hydroxy-3-[(1-methylethyl)amino]propoxy]-N</p>

<p>Collagen proline hydroxylase inhibitor-1 具有抗纤维增生活性。</p>

<p>Sitagliptin impurity E is an inhibitor of dipeptidyl peptidase-4 (DPP-IV) that is used as a hypoglycemic agent. Sitagliptin impurity E has been shown to increase the glucose-lowering effect in diabetic patients with type 2 diabetes mellitus. It is also effective in reducing postprandial glucose and insulin levels. Sitagliptin impurity E has been shown to increase the concentration of insulin in plasma for up to 24 hours after administration, which suggests that it may be useful for the treatment of metabolic disorders such as obesity and type 2 diabetes mellitus.</p>

<p>7'-Methyl-2'-propyl-2,5'-bi-1H-benzimidazole (7'-MPB) is a benzimidazole derivative that is used as a medicine. It is made from recycled chemicals and has shown to have industrial applications as a catalyst for cyclization reactions. 7'-MPB is also used in the production of benzenesulfonic acid, which is an organic solvent. This chemical has been shown to be effective against high blood pressure, but has not been tested on humans yet. Telmisartan, which belongs to the angiotensin II receptor blocker class of drugs, can inhibit the synthesis of prostaglandins.</p>

<p>Elobixibat (A 3309) blocks IBAT in mice/humans/dogs (IC50: 0.13/0.53/5.8 nM); used for constipation research.</p>

<p>Lumateperone (ITI 722) is a 5HT2A receptor antagonist and a dopamine receptor phosphoprotein modulator (DPPM).</p>

<p>This is a synthetic, impurity standard for 2-Amino-5,6-dichloro-3-(4H)-quinazoline acetic acid (CAS No. 1159977-03-3) that can be used in the drug product development process. This product is available as a custom synthesis and as an analytical standard for HPLC. It is also available as a pharmacopoeia grade material. The compound has been shown to have niche applications in metabolism studies and natural products research.</p>

<p>11,11'-(1,4-Piperazinediyl)bis-dibenzo[b,f][1,4]thiazepine is a molecule that inhibits the replication of DNA and RNA in viruses. The structure of 11,11'-(1,4-Piperazinediyl)bis-dibenzo[b,f][1,4]thiazepine has been determined by X-ray crystallography. Hepatocyte cells were used for this study because they are important for the metabolism of drugs. This molecule binds to serine proteases and prevents them from functioning properly. It also inhibits the replication of hepatitis C virus and human immunodeficiency virus type 1 (HIV-1). 11,11'-(1,4-Piperazinediyl)bis-dibenzo[b,f][1,4]thiazepine can be used as a template for designing other molecules with antiviral</p>

<p>(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib is a JAK3 inhibitor(IC50 : 1 nM).</p>

<p>Lisuride: an oral D2 dopamine agonist, ergot derivative, used in Parkinson's, migraine, and high prolactin research.</p>

<p>Macitentan n-butyl analogue, an oral ETA/ETB receptor blocker, may treat IPF and PAH.</p>

<p>COTI-219 is an oral inhibitor of KRAS with antitumor properties [1].</p>

<p>Indinavir monohydrate is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.</p>

<p>Quinagolide Free Base is a non-ergot dopamine D(2)-agonist.</p>

<p>Vibegron (MK-4618) is an effective and selective Beta 3 adrenergic receptor agonist, used to treat overactive bladder (OAB).</p>

<p>RuDiOBn exhibits low antioxidant activity by scavenging DPPH and ABTS free radicals with scavenging rates of 13.2% and 5.9% at a concentration of 100 μg/mL. It inhibits collagen glycation and reduces the formation of advanced glycation end-products (AGE) with an IC50 of 2.45 μg/mL. RuDiOBn also enhances fibroblast proliferation and migration, stimulates collagen synthesis, and aids in skin repair and regeneration while inhibiting collagenase.</p>

<p>Tipelukast (KCA 757), an oral drug for asthma research, blocks leukotrienes and fights inflammation and fibrosis.</p>

<p>SD-2590 HCl is an MMP-2,-3, -9, -8, 13, and -14 inhibitor.</p>

<p>HU-308, a synthetic cannabinoid analogue, is a highly selective agonist of the CB2 receptor. It demonstrates an affinity for the CB2 receptor that is over 440 times greater than its affinity for the CB1 receptor, which are predominantly found in immune cells. This compound plays a crucial role in modulating the immunosuppressive effects of the endocannabinoid system (ECS). Additionally, HU-308 possesses anti-inflammatory and neuroprotective properties, and it regulates the function of microglia. Its potential applications include research into neuroinflammation and retinal diseases.</p>