BMS-433796

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服活性 γ-分泌酶抑制剂，细胞 IC50 为 0.3 nM。

A potent, orally active γ-secretase inhibitor with cell IC50 of 0.3 nM; exhibits Abeta lowering activity in a transgenic mouse model of Alzheimer's disease with acceptable pharmacodynamic and pharmacokinetic profile..Alzheimer's Disease Discontinued.

BMS-433796 cause a concentration-dependent decrease in [3H]IN973 binding, with IC50 value of 1.2 nM, very similar to the IC50 values for inhibition of Aβ40 in human embryonic kidney cells overexpressing the Swedish mutation of APP of 0.8 nM, respectively, and for inhibition of Aβ42 of 0.4 nM, respectively.

BMS 433796 is characterized in pharmacokinetic studies in male Sprague-Dawley rats. Following a 10-min intravenous infusion at 2.3 μmol/kg in PEG-400, the total body clearance of 40 is 5.2±0.82 mL/min/kg (means±SEM; n=3), indicating low clearance. The apparent terminal elimination half-life is 4.6±0.48 h. Oral administration of a PEG-400 suspension at 35 μmol/kg shows an oral bioavailability of 31% with prolonged absorption. BMS 433796 has satisfactory metabolic stability in human liver microsomal preparations and is not an inhibitor of human CYPs (IC50>100 μM). Brain Aβ40 is reduced as a result of administering BMS-433796 in a dose-dependent manner, with ED50 value of 2.4 mg/kg, respectively.

BMS433796 | BMS-433796 | BMS 433796.

Wnt/Notch/Hedgehog

γ-secretase

γ-secretase

Neurological Disease

Alzheimer Disease

935525-13-6

430.4

C21H20F2N4O4

>98% (HPLC)

DMSO

C[C@H](NC([C@H](C1=CC(F)=CC(F)=C1)O)=O)C(N[C@H]2C3=CC=CC=C3C=NN(C)C2=O)=O

Benzeneacetamide, N-[(1S)-2-[[(5S)-4,5-dihydro-3-methyl-4-oxo-3H-2,3-benzodiazepin-5-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-α-hydroxy-, (αS)-

(-20℃)

With Ice Pack

≥ 2 years