496000

OM99-2

InSolution, ≥90%, analog inhibitor of human brain memapsin 2

• Sinônimo(s): InSolution OM99-2, EVNLΨAAEF
• Fórmula empírica (Notação de Hill): C₄₁H₆₄N₈O₁₄
• Número CAS: 314266-76-7
• Peso molecular: 892.99
• Número MDL: MFCD03452932
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥90% (HPLC)
• forma: liquid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated; protect from light
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C
• 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
• chave InChI: JCNFYXCBSRPSLY-QYTLZHMISA-N

Descrição

Descrição geral

A peptidomimetic, highly potent, tight-binding transition-state analog inhibitor of human brain β-secretase (K_i = 1.6 nM, recombinant memapsin-2; K_i = 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 (K_i = 48 nM).

An eight residue peptidomimetic, tight binding transition-state analog inhibitor of human brain memapsin 2 (K_i = 1.6 nM, recombinant memapsin 2; K_i = 9.58 nM, recombinant pro-memapsin 2). Also inhibits cathepsin D (K_i = 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.

Ações bioquímicas/fisiológicas

Cell permeable: no

Primary Target
human brain memapsin 2

Product does not compete with ATP.

Reversible: no

Target K_i: 1.6 nM against recombinant memapsin 2; 9.58 nM against recombinant pro-memapsin 2; 48 nM against cathepsin D

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Sequência

Glu-Val-Asn-Leu-Ψ-Ala-Ala-Glu-Phe [Ψ denotes replacement of CONH by (S)-CH(OH)CH₂]

forma física

A 1 mM (250µg in 280 µl) solution in DMSO. Supplied as a trifluoroacetate salt.

Reconstituição

Following initial thaw, aliquot and freeze (-20°C). Avoid freeze/thaw cycles of solutions.

Outras notas

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.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 10 - Combustible liquids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Ponto de fulgor (°C): 87 °C - closed cup - (Dimethylsulfoxide)