BMS-708163 (Avagacestat)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BMS-708163是一个高效的、口服生物可利用的γ分泌酶选择性抑制剂，IC50值是0.3 nM[1]。
γ分泌酶分解淀粉样前体蛋白（APP）生成Aβ40和Aβ42，具有细胞毒性，可引起AD。体外实验表明，BMS-708163抑制H4-8Sw细胞中Aβ40和Aβ42的形成，它也抑制人重组CYP同工酶，IC50值为20 μM。Notch受体是γ分泌酶的另一个底物，Notch信号通路的抑制可导致一些副作用。研究表明，BMS-708163对Notch的抑制活性比对APP 弱190倍。在雌性大鼠中，口服给药10 mg/kg和100 mg/kg的BMS-708163显著降低血浆和脑中Aβ的生成。此外，BMS-708163也减少雄性比格犬脑和脑脊液中Aβ的含量[1]。
参考文献：
[1] Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE. Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. ACS Med Chem Lett. 2010 Mar 22;1(3):120-4.
| Storage | Store at -20°C |
| M.Wt | 520.88 |
| Cas No. | 1146699-66-2 |
| Formula | C20H17ClF4N4O4S |
| Solubility | insoluble in H2O; ≥177.6 mg/mL in DMSO; ≥47.6 mg/mL in EtOH with ultrasonic |
| Chemical Name | (2R)-2-[(4-chlorophenyl)sulfonyl-[[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC=C1S(=O)(=O)N(CC2=C(C=C(C=C2)C3=NOC=N3)F)C(CCC(F)(F)F)C(=O)N)Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 描述 | BMS-708163是一个有效的、选择性的、口服生物可利用的γ分泌酶抑制剂，对Aβ40和Aβ42的IC50值分别是0.3 nM和0.27 nM。 | |||||
| 靶点 | γ-secretase | γ-secretase | ||||
| IC50 | 0.3 nM (Aβ40) | 0.27 nM (Aβ42) | ||||
质量控制和MSDS
- 批次:
化学结构
