CVT-12012

Modify Date: 2024-01-12 12:02:48

CVT-12012 structure	Common Name	CVT-12012
	CAS Number	1018675-35-8	Molecular Weight	434.41200
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₁H₂₁F₃N₄O₃	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of CVT-12012

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.

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

Description	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.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Stearoyl-CoA Desaturase (SCD) Research Areas >> Metabolic Disease
Target	IC50: 38 nM (rat microsomal), 6.1 nM (human HEPG2)[1][2].
In Vitro	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 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[1].
References	[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.

Molecular Formula	C₂₁H₂₁F₃N₄O₃
Molecular Weight	434.41200
Exact Mass	434.15700
PSA	99.74000
LogP	3.35760
Storage condition	2-8℃

{2-[3-methyl-2-oxo-7-(3-trifluoromethyl-benzylamino)-2H-quinoxalin-1-yl]-ethylcarbamoyl}-methyl acetate structure

{2-[3-methyl-2-...

CAS#:1018675-34-7

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CVT-12012 Structure

CVT-12012

CAS#:1018675-35-8

Literature: Koltun, Dmitry O.; Zilbershtein, Timur M.; Migulin, Vasily A.; Vasilevich, Natalya I.; Parkhill, Eric Q.; Glushkov, Andrei I.; McGregor, Malcolm J.; Brunn, Sandra A.; Chu, Nancy; Hao, Jia; Mollova, Nevena; Leung, Kwan; Chisholm, Jeffrey W.; Zablocki, Jeff Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4070 - 4074

Precursor 1
CAS#:1018675-34-7 {2-[3-methyl-2-...
DownStream 0

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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: CVT-12012
Price: Negotiable
Purity: 98.0%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: CVT-12012
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

DC Chemicals Limited
China
Product Name: CVT-12012
Price: $450.0/100mg $900.0/250mg $1800.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

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Price: ￥1100/10 mM * 1 mL in DMSO

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