|4-(2-氯苯氧基)-N-(3-((甲基氨基)羰基)苯基)-1-哌啶甲酰胺|CsnPharm

CAS No.: 1032229-33-6

A939572/SCD1抑制剂 Catalog No. CSN12797

Synonyms: SCD1 Inhibitor;Stearoyl-CoA Desaturase 1 Inhibitor;Stearoyl-CoA Desaturase Inhibitor

A939572 is an inhibitor of SCD1 with IC50 values of 4 nM and 37 nM for mSCD1 and hSCD1.

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技术信息

生物活性

描述SCD1 (stearoyl-CoA desaturase1) plays an important role in lipid metabolism and body weight control. Higher SCD1 activity in humans has been correlated with elevated plasma triglyceride levels. A939572 is an orally bioavailable and potent SCD1 inhibitor with IC₅₀ values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively ^[3]. A939572 demonstrated a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC₅₀s of 65 nM, 50 nM, 65 nM, and 6 nM respectively). Moreover, A939572 induced apoptosis in all four cell lines ^[4]. A939572 has modest volume of distribution and high oral bioavailability in mice (CL_p= 0.4 L/h/kg; V_ss= 0.4 L/kg; F= 92%). In ob/ob mice, A939572 (10 mpk bid) consistently reduced desaturation indices of all these lipid categories (cholesterol ester, diacylglycerol, free fatty acid, free cholesterol, total phospholipids, and triacylglycerol) to lean level, or even lower. A dose dependent triglyceride desaturation index reduction by A939572 was also observed in ob/ob mice ^[3].
参考文献

[1] von Roemeling CA, Marlow LA, et al. Stearoyl-CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Clin Cancer Res. 2013 May 1;19(9):2368-80.
[2] Xin Z, Zhao H, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302.
[3] Xin Z, Zhao H, Serby MD, Liu B, Liu M, Szczepankiewicz BG, Nelson LT, Smith HT, Suhar TS, Janis RS, Cao N, Camp HS, Collins CA, Sham HL, Surowy TK, Liu G. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302. doi: 10.1016/j.bmcl.2008.06.088. Epub 2008 Jun 28. PMID: 18632269.
[4] von Roemeling CA, Marlow LA, Wei JJ, Cooper SJ, Caulfield TR, Wu K, Tan WW, Tun HW, Copland JA. Stearoyl-CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Clin Cancer Res. 2013 May 1;19(9):2368-80. doi: 10.1158/1078-0432.CCR-12-3249. Epub 2013 Apr 30. PMID: 23633458; PMCID: PMC3644999.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5782 mL
- 12.8912 mL
- 25.7825 mL
- 5 mM
- 0.5156 mL
- 2.5782 mL
- 5.1565 mL
- 10 mM
- 0.2578 mL
- 1.2891 mL
- 2.5782 mL

技术信息

CAS号

1032229-33-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22ClN3O3

运输

蓝冰

分子量

387.86

别名

SCD1 Inhibitor;Stearoyl-CoA Desaturase 1 Inhibitor;Stearoyl-CoA Desaturase Inhibitor;SCD Inhibitor

溶解度

DMSO	95.0 mg/mL (244.9 mM) warming

动物实验配方

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A939572/SCD1抑制剂 Catalog No. CSN12797

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