商品介绍
BMS-708163 (Avagacestat) is a potent and selective inhibitor for gamma-secretase, especially at inhibiting cleavage of amyloid precursor protein (APP) to form amyloid-ß (Aß)(1-40) (IC50=0.3nM) and Aß(1-42) (0.27nM). BMS-708163 is ??Notch sparing??, with more than 100 folds more selective for APP than for Notch protein (IC50 of 58nM). BMS-708163 is developed for treating Alzheimer??s disease (AD). Oral administration of BMS-708163 significantly reduced Aß(1-40) levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs [1]. The results of Phase II clinical trial in mild-to-moderate AD patients demonstrated acceptable tolerability at a single-dose range of 0.3 to 800 mg with a biphasic effect on plasma Aß(1-40) [2].
Technical information:
| Chemical Formula: | | C20H17ClF4N4O4S |
| CAS #: | | 1146699-66-2 |
| Molecular Weight: | | 520.88 |
| Purity: | | >98% |
| Appearance: | | White |
| Chemical Name: | | (2R)-2-(N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-4-chlorophenylsulfonamido)-5,5,5-trifluoropentanamide |
| Solubility: | | Up to 50 mM in DMSO |
| Synonyms: | | BMS-708163, BMS 708163, BMS708163, Avagacestat |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Gillman, KW., et al. Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable ?-Secretase Inhibitor. ACS Med. Chem. Lett., 2010, 1 (3): 120??124 |
| 2. | Tong G., et al., Multicenter, randomized, double-blind, placebo-controlled, single-ascending dose study of the oral ?-secretase inhibitor BMS-708163 (Avagacestat): tolerability profile, pharmacokinetic parameters, and pharmacodynamic markers. Clin Ther. 2012 . 34(3):654-67. Pubmed ID:22381714 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
品牌介绍
Cellagen Technology 公司位于美国加州San Diego，该公司致力于干细胞相关产品的研发和生产。基于多年为世界*的生物公司提供OEM产品的经验，目前Cellagen Technology公司利用自身优势，拓展了原有产品线，推出了以StemRegenin 1（SR1）为代表的多种自有品牌产品。 NamePriceCat # （Powder）Cat # （10 mM in DMSO）Pathway/Target7,8-Dihydroxyflavone1173C7181-10N/ATrkBA7696622023C2769-10N/AAMPKA83-011513C2831-2C2831-2sTGF-β/ALK4,5,7Abiraterone1853C2247-2C2247-2sP450-CYP17BEZ235833C2392-2C2392-2sPI3K, mTORBIX-012941513C2491-5C2491-5sEpigenetics/G9a HMTCHIR990213553C2447-2C2447-2sGSK3β CP-6905501343C2716-2C2716-2sJAK1,2,3Cyclopamine2193C2925-2C2925-2sHedgehog/SmoDAPT1853C3178-5C3178-5sNotch/γ-secretaseForskolin1853C3677-10N/AAdenylate cyclaseFTY7201173C3897-5C3897-5sS1P receptorsGDC-09411513C4321-5C4321-5sPI3KHh-Ag1.53043C4412-2C4412-2sHedgehog/SmoINCB0184241853C4622-2C4622-2sJAK1/2IWP-31853BackorderBackorderWntKHS1011853C5471-5C5471-5sNeural differentiationLDE2252363C5332-2C5332-2sHedgehog/SmoLDN-1931893723C5361-2C5361-2sBMP/ALK2,3Leukadherin-1#VALUE!C5385-2C5385-2sCD11b, CD18LY2940022193C5929-5C5929-5sPI3KP7C32363C7723-10N/Aneurogenic, neuroprotectivePD03259013723C7303-2C7303-2sMEK1, MEK2PD03329912193C7306-2C7306-2sCdk4, Cdk6PS481343C7748-5C7748-5sPDK1Pyrintegrin3383C7974-1C7974-1sES cell survivalR4062193C7406-2C7406-2sSykR7883723C7788-5C7788-5sSykRapamycin2193C7272-5C7272-5smTORReversine1173C7383-2C7383-2sA3 Adenosine ReceptorRO49290972703C7649-2C7649-2sNotch/γ-secretaseSB4315421513C7243-5C7243-5sTGF-β/ALK4,5,7SF16703723C7316-2C7316-2spTENSitagliptin1513C7482-5C7482-5sDPP-4SRT17202363C7781-2C7781-2sSIRT1StemRegenin1 （SR1）3723C7710-1C7710-1sAryl hydrocarbon receptorSU54022703C7854-1C7854-1sFGFRThiazovivin3553C8442-1C8442-1sROCKUrsolic Acid1853C8776-10N/ASTAT3VX-6801173C8916-10N/AAurora kinaseWnt-C592703C7641-2C7641-2sWntXAV9392703C9289-2C9289-2sWntY-276321853C9127-2C9127-2sROCKhuman Activin A5423P4228-1031910 µg37383P4228-1002199100 µghuman BMP-4 3723P4267-1021910 µg25483P4267-1001499100 µghuman bFGF 3383P4234-5019950 µg23783P4234-5001399500 µgmouse LIF 3383P6543-1019910 µg23783P6543-1001399100 µghuman Wnt-3a 3723P4968-1021910 µg
