Quinazoline and Quinoline Derivatives

<p>Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.</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>Apixaban Impurity 1 is an impurity found in Apixaban, a drug used for the prevention of stroke. It is produced by condensation of 2-aminopyridine and 3-hydroxybenzaldehyde in ethanol with sodium hydroxide as a catalyst. The reaction proceeds via amination of the pyridine ring followed by transesterification. The yield of this impurity is low at about 4%.</p>

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

AGPS-IN-2i inhibits alkylglycerol phosphate synthase, affecting ether lipid metabolism and reducing cancer cell migration and proliferation.

<p>PG-116800 (PG-530742) is a matrix metalloproteinase (MMP) inhibitor. PG-116800 can be used in studies about the treatment of osteoarthritis.</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>Stepronin (TTPG) shows expectorant activities and inhibits airway secretion.</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>Edoxaban: potent, selective FXa inhibitor; Ki 0.561 nM. Used as an oral anticoagulant for stroke prevention, also inhibits thrombin and FIXa.</p>

<p>Empagliflozin S-furanose is a Custom synthesis drug product. It is an analytical standard with CAS No. 1620758-32-8, and it is used in research and development of new drugs. Empagliflozin S-furanose has been found to be a metabolite of empagliflozin, a drug that is used to treat type 2 diabetes mellitus. It is also used as an impurity standard for HPLC analysis of empagliflozin because it does not have any biological activity.</p>

<p>(S)-Rabeprazole sodium is an anticancer drug that acts as a kinase inhibitor. It is an analog of Rabeprazole and has been shown to inhibit the growth of cancer cells in vitro and in vivo. (S)-Rabeprazole sodium inhibits the activity of kinases, which are enzymes that play a key role in cell signaling pathways. This inhibition leads to apoptosis, or programmed cell death, in cancer cells. (S)-Rabeprazole sodium has been tested against various types of cancer, including Chinese hamster ovary cells and tumor xenografts in mice. It has also been shown to inhibit elastin degradation, which is important for preventing metastasis of cancer cells. (S)-Rabeprazole sodium may be a promising candidate for the development of new anticancer drugs that target specific kinases and proteins involved in cancer cell growth and survival.</p>

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

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

<p>Pitolisant is a potent and selective nonimidazole inverse agonist that acts on the recombinant human histamine H3 receptor with Ki of 0.16 nM.</p>

<p>UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays.</p>

<p>Roflumilast impurity A is a metabolite of roflumilast. It is a drug product that is used as an analytical standard for the determination of roflumilast in HPLC analysis. Roflumilast impurity A is not natural and is synthetic. It has been shown to be a substrate for CYP1A2, CYP2C8, CYP2C9, and CYP3A4 enzymes. Studies have shown that it may be involved in the metabolism of roflumilast through hydroxylation and deamination.</p>

<p>Lapatinib is a tyrosine kinase inhibitor that blocks the epidermal growth factor receptor (EGFR) and other tyrosine kinases. It is used in cancer treatment to inhibit tumor growth, with a high success rate. Lapatinib is also used to treat lung cancer and other types of cancer. The drug has been shown to inhibit EGFR phosphorylation in vitro, which leads to inhibition of cell proliferation and induction of apoptosis. Lapatinib also inhibits the expression of EGFR downstream target genes such as b-raf, serine/threonine-protein kinase, and cyp3a5.</p>

<p>Amlodipine EP Impurity E maleate is a high purity and analytical grade chemical. It is a metabolite of Amlodipine, which is used in the treatment of hypertension. This chemical has been shown to be a natural product that is produced by the human body. It also has been shown to have pharmacological properties, such as anti-inflammatory and vasodilatory effects. The impurity standard for this compound is available from Sigma-Aldrich.br&gt;br&gt;</p>

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

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

<p>Yonkenafil, a PDE5 inhibitor, may reduce stroke damage and aid in Alzheimer's treatment.</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>Pirtobrutinib: a selective, non-covalent BTK inhibitor effective against BTK C481 mutations, causing tumor regression in lymphoma models.</p>

<p>MMP3 inhibitor 1 is a potent and highly selective inhibitor of MMP-3 (IC50 of 1 nM).</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>MMP-145 is used as a protease inhibitor.</p>

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

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

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

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>Collagen proline hydroxylase inhibitor is an inhibitor collagen proline hydroxylase and useful for antifibrotic proliferative agents.</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>Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs)</p>

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

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

<p>Ro 32-7315 is a selective inhibitor of ADAM17.</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>KB-R7785 is a novel ADAM12/MMP inhibitor improving heart function and insulin sensitivity by blocking HB-EGF and TNF-alpha.</p>

<p>ONO-4817 suppresses MMPs, limiting plaque progression and aortic hyperplasia in hyperlipidemic rabbits.</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>Brasofensine, a benztoalkane MA reuptake inhibitor, shows promise for Parkinson's and Alzheimer's.</p>

<p>Caroverine is a potential chemotherapeutical agent in HNSCC cell lines.</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>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>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>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>ND-378 is a potent and selective inhibitor of MMP-2 with no inhibition on MMP-9 and MMP-14.</p>

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

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

<p>IK-862 is a selective TACE inhibitor with potential anti-inflammatory and anticancer activity for the study of neuritis.</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>Brilaroxazine (RP5063): multimodal dopamine/5-HT modulator, partial agonist at D2/D3/D4, 5-HT1A/2A, and antagonist at 5-HT2B/7.</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>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>Cobimetinib racemate (Cobimetinib (racemate)) (GDC-0973 racemate) is a selective inhibitor of MEK.Cobimetinib racemate is also known as a mitogen-activated</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>Levocarbastine: 2nd-gen H1 antagonist, treats allergic conjunctivitis, selective NTS2 neurotensin inhibitor.</p>

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

<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>Frovatriptan, potent 5-HT 1B/D agonist, shows high cerebroselectivity and efficacy for migraine with aura.</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>Z-PDLDA-NHOH is a potent, specific vertebrate collagenase inhibitor [1].</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>Pure antiestrogen that downregulates estrogen receptor expression</p>

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

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

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

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

<p>ROCK2 inhibitor is a chemical compound associated with the therapeutic management of psoriasis.</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>Bufuralol hydrochloride is a potent, non-selective, orally active β-blocker with partial agonist effects and a CYP2D6 probe.</p>

<p>Collagen proline hydroxylase inhibitor-1 具有抗纤维增生活性。</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>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>Maralixibat Chloride (LUM001 chloride), an apical, sodium-dependent, bile acid transport inhibitor, prevents enterohepatic bile acid recirculation.</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>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>Lumateperone (ITI 722) is a 5HT2A receptor antagonist and a dopamine receptor phosphoprotein modulator (DPPM).</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>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>Arterolane is an antimalarial compound. For against P. falciparum Ro73 and W2, the IC50s are both 1.1 nM.</p>

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

<p>BAY-7598 is a potent, selective, and orally bioavailable MMP12 inhibitor (IC50s: 0.085, 0.67, and 1.1 nM for human/murine/rat MMP12).</p>

<p>CM-352 is a metalloproteinase inhibitor that reduces brain damage and improves functional recovery in rat models of cerebral hemorrhage.</p>

<p>UK-370106 is a potent and highly selective inhibitor of MMP-3 with IC50 of 23 nM and MMP-12 with IC50 of 42 nM, and potently inhibits cleavage of [3H]-</p>

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

<p>Aclidinium, a dual-action compound, serves as a long-acting muscarinic antagonist and a β2-adrenoceptor (β2-AR) agonist, exhibiting bronchodilator properties. It effectively reduces lung hyperinflation, enhances lung function, and prolongs exercise endurance time. This compound is commonly utilized in studies focusing on chronic obstructive pulmonary disease (COPD).</p>

<p>Finafloxacin is a pH-activated fluoroquinolone, most effective at pH 5.0-6.0, targeting bacterial topoisomerases, used for UTIs and H. pylori infections.</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>SD-7300 (SC-81490) functions as an orally active inhibitor targeting MMP-2, MMP-9, and MMP-13, exhibiting potent inhibition with K_i values of 0.03, 0.01, and 0.03 nM, respectively. By inhibiting these metalloproteinases, SD-7300 effectively reduces extracellular matrix degradation by tumor cells, thereby curbing their invasion and metastasis. Additionally, this compound acts as a dose-dependent inhibitor of mouse corneal angiogenesis and prevents interleukin-1-induced degradation of bovine cartilage. SD-7300 is applicable in the study of breast cancer.</p>