产品说明
一般描述
An eight residue peptidomimetic, tight binding transition-state analog inhibitor of human brain memapsin 2 (Ki = 1.6 nM, recombinant memapsin 2; Ki = 9.58 nM, recombinant pro-memapsin 2). Also inhibits cathepsin D (Ki = 48 nM). This aspartyl protease inhibitor is designed from the template of the β-secretase site of Swedish β-amyloid precursor protein (APP) with Asp to Ala replacement; also includes a nonhydrolyzable hydroxyethylene isostere between Leu and Ala.
A peptidomimetic, highly potent, tight-binding transition-state analog inhibitor of human brain β-secretase (Ki = 1.6 nM, recombinant memapsin-2; Ki = 9.58 nM, recombinant pro-memapsin 2). Designed from the template of the β-secretase site of Swedish β-amyloid precursor protein (APP) with Asp to Ala replacement. Includes a nonhydrolyzable hydroxyethylene isostere between Leu and Ala. Also reported to inhibit cathepsin D at higher levels (Ki = 48 nM).
包装
250 μg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Product does not compete with ATP.
Target Ki: 1.6 nM against recombinant memapsin 2; 9.58 nM against recombinant pro-memapsin 2; 48 nM against cathepsin D
Primary Target
human brain memapsin 2
Reversible: no
Cell permeable: no
警告
Toxicity: Standard Handling (A)
序列
Glu-Val-Asn-Leu-Ψ-Ala-Ala-Glu-Phe [Ψ denotes replacement of CONH by (S)-CH(OH)CH₂]
外形
A 1 mM (250µg in 280 µl) solution in DMSO. Supplied as a trifluoroacetate salt.
重悬
Following initial thaw, aliquot and freeze (-20°C). Avoid freeze/thaw cycles of solutions.
其他说明
Ghosh, A.K., et al. 2001. J. Med. Chem.44, 2865.
Turner III, R.T., et al. 2001. Biochemistry40, 10001.
Ghosh, A.K., et al. 2000. J. Am. Chem. Soc.122, 3522.
Hong, L., et al. 2000. Science290,150.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C41H64N8O14 |
| 分子量 | 892.99 |
| MDL编号 | MFCD03452932 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥90% (HPLC) |
| 形式 | liquid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze desiccated protect from light |
| 运输 | ambient |
| 储存温度 | −20℃ |
| InChI | 1S/C39H60N8O14/c1-18(2)12-24(43-36(57)25(16-29(41)49)45-38(59)32(19(3)4)47-35(56)23(40)15-30(50)51)28(48)13-20(5)33(54)42-21(6)34(55)44-26(17-31(52)53)37(58)46-27(39(60)61)14-22-10-8-7-9-11-22/h7-11,18-21,23-28,32,48H,12-17,40H2,1-6H3,(H2,41,49)(H,42,54)(H,43,57)(H,44,55)(H,45,59)(H,46,58)(H,47,56)(H,50,51)(H,52,53)(H,60,61)/t20-,21+,23+,24+,25+,26+,27+,28+,32+/m1/s1 |
| InChI key | JCNFYXCBSRPSLY-QYTLZHMISA-N |
安全信息
| 储存分类代码 | 10 - Combustible liquids |
| WGK | WGK 1 |
| 闪点(F) | 188.6 °F - (Dimethylsulfoxide) |
| 闪点(C) | 87 ℃ - (Dimethylsulfoxide) |
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