CVT-12012

小分子

CVT 12012; CVT12012 | AC-36268 | 2-Hydroxy-N-(2-(3-methyl-2-oxo-7-(((3-(trifluoromethyl)phenyl)methyl)amino)-1,2-dihydroquinoxalin-1-yl)ethyl)acetamide | 2-hydroxy-N-(2-(3-methyl-2-oxo-7-(3-(trifluoromethyl)benzylamino)quinoxalin-1(2H)-yl)ethyl)acetamide

CVT-12012

C649842-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC 50 s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively. In Vitro CVT-12012 (Compound 5b) displays the highest potency in both the microsomal and the HEPG2 SCD assays (IC 50 38 nM and 6.1 nM, respectively) compared to the other methyl-substituted compounds. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 38 nM (rat microsomal), 6.1 nM (human HEPG2)

CVT-12012 是一种强效且可口服的硬脂酰-coA 去饱和酶 (SCD) 抑制剂，对大鼠微粒体和人类 HEPG2 的 IC 50 s 分别为 38 nM 和 6.1 nM。

1018675-35-8

C21H21F3N4O3

434.41 g/mol

25195516

CC1=NC2=C(C=C(C=C2)NCC3=CC(=CC=C3)C(F)(F)F)N(C1=O)CCNC(=O)CO

2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)phenyl]methylamino]quinoxalin-1-yl]ethyl]acetamide

1S/C21H21F3N4O3/c1-13-20(31)28(8-7-25-19(30)12-29)18-10-16(5-6-17(18)27-13)26-11-14-3-2-4-15(9-14)21(22,23)24/h2-6,9-10,26,29H,7-8,11-12H2,1H3,(H,25,30)

HRAQDVZJYIAWOV-UHFFFAOYSA-N

CC1=NC2=C(C=C(C=C2)NCC3=CC(=CC=C3)C(F)(F)F)N(C1=O)CCNC(=O)CO

25195516

1018675-35-8

DMSO : 125 mg/mL (287.75 mM; Need ultrasonic)

3

8

7

434.157 Da

434.157 Da

94.000 Ų

31

0

685

0

1

1.9