| Identification | Back Directory | [Name]
N-((1R,2S,5R)-5-(ISOPROPYL(METHYL)AMINO)-2-((S)-2-OXO-3-((6-(TRIFLUOROMETHYL)QUINAZOLIN-4-YL)AMINO)PYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE | [CAS]
1004757-96-3 | [Synonyms]
BMS-741672
N-((1R,2S,5R)-5-(ISOPROPYL(METHYL)AMINO)-2-((S)-2-OXO-3-((6-(TRIFLUOROMETHYL)QUINAZOLIN-4-YL)AMINO)PYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE | [Molecular Formula]
C25H33F3N6O2 | [MDL Number]
MFCD30829467 | [MOL File]
1004757-96-3.mol | [Molecular Weight]
506.56 |
| Hazard Information | Back Directory | [Description]
BMS-741672 is a potent, selective CCR2 antagonist for the treatment of neuropathic pain. | [Uses]
BMS-741672 is a selective and orally active CCR2 antagonist with an IC50 of 1.1 nM. BMS-741672 shows >700-fold selective for CCR2 than CCR5[1]. | [in vivo]
BMS-741672 is found to have 51% oral bioavailability in a rat with a t1/2 value of 5.1 h (IV), and there is 46% oral bioavailability in a cynomolgus monkey with a t1/2 of 3.2 h (IV)[1]. | [IC 50]
CCR2: 1.1 nM (IC50); CCR5: 780 nM (IC50) | [References]
[1] Michael G Yang, et al. Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672. ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. DOI:10.1021/acsmedchemlett.8b00439 |
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| Company Name: |
AstaTech, Inc
|
| Tel: |
(215) 785 3197 |
| Website: |
www.astatechinc.com |
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