| Identification | Back Directory | [Name]
5H-Cyclopentapyrimidine-2,4-diamine, 7-(4-fluorophenyl)-6,7-dihydro-N2-[3-methoxy-4-(3-methyl-1H-1,2,4-triazol-1-yl)phenyl]-N4-methyl-, (7S)- | [CAS]
1263871-36-8 | [Synonyms]
BMS-932481
BMS-932481(BMS932481
5H-Cyclopentapyrimidine-2,4-diamine, 7-(4-fluorophenyl)-6,7-dihydro-N2-[3-methoxy-4-(3-methyl-1H-1,2,4-triazol-1-yl)phenyl]-N4-methyl-, (7S)- | [Molecular Formula]
C24H24FN7O | [MOL File]
1263871-36-8.mol | [Molecular Weight]
445.49 |
| Hazard Information | Back Directory | [Uses]
BMS-932481 is an orally active modulator for γ-secretase, selectively reduce Aβ1-42 and Aβ1-40 production, with IC50s of 6.6 and 25.3 nM, respectively[1]. | [in vivo]
BMS-932481 (2-30 mg/kg, po, single dose) reduces the levels of Aβ1-42 and Aβ1-40, increases levels of Aβ1-38 and Aβ1-37, without changing overall amounts of Aβ peptides in dog models[1].
BMS-932481 (2.5-15 mg/kg, iv, single dose) exhibits moderate brain penetration with brain-to-plasma ratio and AUCbrain to AUCplasma ratio of about 0.23 and 0.6 in Sprague-Dawley rats[1]. | Animal Model: | Beague dog model[1] | | Dosage: | 2-30 mg/kg | | Administration: | po, single dose | | Result: | Reduced levels of Aβ1-42 and Aβ1- 40 of 65% with 30 mg/kg dose, increased levels of Aβ1-38 and Aβ1-37 by 1.8 and 5 fold. |
| [References]
[1] Toyn JH, et al., Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects. J Pharmacol Exp Ther. 2016 Jul;358(1):125-37. DOI:10.1124/jpet.116.232249 |
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