BVT-14225

• 常用名: BVT-14225
• 英文名: BVT-14225
• CAS号: 376638-65-2
• 分子量: 401.93
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₆H₂₀ClN₃O₃S₂
• 熔点: N/A
• 闪点: N/A

BVT-14225用途

BVT-14225是选择性的11β羟基类固醇脱氢酶1型(11β-HSD1)抑制剂,IC50值为52 nM。

BVT-14225名称

• 中文名: BVT-14225
• 英文名: BVT-14225

BVT-14225生物活性

• 描述: BVT-14225是选择性的11β羟基类固醇脱氢酶1型(11β-HSD1)抑制剂,IC50值为52 nM。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 代谢疾病
• 靶点实验:

  IC50: 52 nM (11β-HSD1)[1]

• 体外研究: 选择性抑制11β-HSD1可降低高血糖小鼠的血糖浓度。 11β-HSD1的选择性抑制剂作为治疗许多未满足的医学需求的疾病具有相当大的潜力,例如2型糖尿病,肥胖症和代谢综合征,多因素疾病。 BVT-14225在酶测定中显示出高活性,在10μM时具有90％抑制。它对人体酶测定的11β-HSD1的IC50为52 nM [2]。
• 参考文献:

  [1]. Barf T, et al. Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. J Med Chem. 2002 Aug 29;45(18):3813-5.

  [2]. Vicker N, et al. Novel non-steroidal inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1. J Steroid Biochem Mol Biol. 2007 May;104(3-5):123-9.

BVT-14225物理化学性质

• 分子式: C₁₆H₂₀ClN₃O₃S₂
• 分子量: 401.93
• InChIKey: PNFMZAHWOASGJC-UHFFFAOYSA-N
• SMILES: CCN(CC)C(=O)Cc1csc(NS(=O)(=O)c2cccc(Cl)c2C)n1
• 外观性状: light yellow solid
• 储存条件: -20℃

BVT-14225靶点实验

查看更多实验

实验名称：Inhibition of human 11beta HSD1 expressed in HEK293 cells assessed as assessed as inh... 来源：ChEMBL 靶标：11-beta-hydroxysteroid dehydrogenase 1 External Id：CHEMBL1837224

实验名称：Cellular viability qHTS for adrenocortical cancer (ACC) cell line SW-13 来源：NCGC 靶标：N/A External Id：ACC-ATC-p1-SW13-72hr

实验名称：ASTRAZENECA: Octan-1-ol/water (pH7.4) distribution coefficent measured by a shake fl... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3301363

实验名称：Cellular viability qHTS for adrenocortical cancer (ACC) cell line NCI-H295R 来源：NCGC 靶标：N/A External Id：ACC-ATC-p1-H295R-72hr

实验名称：Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry 来源：NCGC 靶标：N/A External Id：TRND-SARS-CoV-2-cytotox-48hr

实验名称：Inhibition of human 11betaHSD1 by scintillation proximity assay 来源：ChEMBL 靶标：11-beta-hydroxysteroid dehydrogenase 1 External Id：CHEMBL2155280

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

实验名称：ASTRAZENECA: Solubility in pH7.4 buffer using solid starting material using the metho... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3301364

实验名称：Primary qHTS to identify inhibitors of SARS-CoV-2 cell entry 来源：NCGC External Id：TRND-SARS-CoV-2-PP

实验名称：Displacement of [3H]cortisone from human 11beta-HSD1 expressed in baculovirus-infecte... 来源：ChEMBL 靶标：11-beta-hydroxysteroid dehydrogenase 1 External Id：CHEMBL1101380

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BVT-14225英文别名

• MFCD25976913
• 2-(2-{[(3-Chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-4-yl)-N,N-diethylacetamide