Avagacestat
Cat. No.：YN380143
CAS No. ：1146699-66-2
| 产品名称: | Avagacestat |
| CAS No.: | 1146699-66-2 |
| Chemical Name: | (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoro-pentanamide |
| Synonyms: | BMS-708163 |
| 分子量: | 520.89 |
| 分子式: | C₂₀H₁₇ClF₄N₄O₄S |
| SMILES: | O=S(N([C@@H](C(N)=O)CCC(F)(F)F)CC1=CC=C(C2=NOC=N2)C=C1F)(C3=CC=C(Cl)C=C3)=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Avagacestat (BMS-708163) 是有效的γ-secretase抑制剂，抑制 Aβ42 和 Aβ40 的产生，IC50值分别为 0.27 nM 和 0.30 nM；BMS-708163 同时抑制 Notch 胞内结构域 (NICD) 和 CYP2C19，IC50值分别为 0.84 nM 和 20 μM。 |
| IC50和靶点: | |
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Andersson, E.R., and Lendahl, U.Therapeutic modulation of Notch signalling - are we there yet?Nat. Rev. Drug Discov.13(5),357-378(2014)
Jurisch-Yaksi, N., Sannerud, R., and Annaert, W.A fast growing spectrum of biological functions of γ-secretase in development and diseaseBiochim. Biophys. Acta1828(12),2815-2827(2013)
Gillman, K.W., Starrett, J.E., Jr., Parker, M.F., et al.Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitorACS Med. Chem. Lett.1(3),120-124(2010)
Albright, C.F., Dockens, R.C., Meredith, J.E., Jr., et al.Pharmacodynamics of selective inhibition of γ-secretase by avagacestatJ. Pharmacol. Exp. Ther.344(3),686-695(2013)
Mitani, Y., Yarimizu, J., Saita, K., et al.Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic miceJ. Neurosci.32(6),2037-2050(2012)
Crump, C.J., Castro, S.V., Wang, F., et al.BMS-708,163 targets presenilin and lacks notch-sparing activityBiochemistry51(37),7209-7211(2012)
