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CVT-12012 目录号 GC31447

A stearoyl-CoA desaturase inhibitor

规格 价格 库存 购买数量
10mM*1mLinDMSO
¥982.00
现货
5mg
¥893.00
现货
10mg
¥1,339.00
现货
25mg
¥2,767.00
现货
50mg
¥4,284.00
现货
100mg
¥6,962.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1018675-35-8 SDF Download SDF
别名 N/A
化学名 N/A
Canonical SMILES O=C(NCCN1C(C(C)=NC2=C1C=C(NCC3=CC=CC(C(F)(F)F)=C3)C=C2)=O)CO
分子式 C21H21F3N4O3 分子量 434.41
溶解度 DMSO : 125 mg/mL (287.75 mM) 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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产品描述

CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.

CVT-12012 (Compound 5b) displays the highest potency in both the microsomal and the HEPG2 SCD assays (IC50 38 nM and 6.1 nM, respectively) compared to the other methyl-substituted compounds[1].

In a rat PK study, CVT-12012 demonstrates good oral bioavailability (78%). It appears that the oral absorption of CVT-12012 is not affected by a significant Pgp efflux, which is expected based on Caco-2 assay result. The plasma clearance of CVT-12012 is high (88 mL/min/kg) with elimination half-life of approximately 1 h[1].

[1]. Koltun DO, et al. Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. [2]. Atkinson KA, et al. N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5.