496000

OM99-2

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

• 동의어(들): InSolution OM99-2, EVNLΨAAEF
• 실험식(Hill 표기법): C₄₁H₆₄N₈O₁₄
• CAS Number: 314266-76-7
• Molecular Weight: 892.99
• MDL number: MFCD03452932
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥90% (HPLC)
• 형태: liquid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; desiccated; protect from light
• 배송 상태: ambient
• 저장 온도: −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
• InChI key: JCNFYXCBSRPSLY-QYTLZHMISA-N

설명

일반 설명

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.

생화학적/생리학적 작용

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

서열

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

물리적 형태

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

재구성

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

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 1
• Flash Point (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Flash Point (°C): 87 °C - closed cup - (Dimethylsulfoxide)