496000

OM99-2

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

• Synonim(y): InSolution OM99-2, EVNLΨAAEF
• Wzór empiryczny (zapis Hilla): C₄₁H₆₄N₈O₁₄
• Numer CAS: 314266-76-7
• Masa cząsteczkowa: 892.99
• Numer MDL: MFCD03452932
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥90% (HPLC)
• Postać: liquid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated; protect from light
• Warunki transportu: ambient
• temp. przechowywania: −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
• Klucz InChI: JCNFYXCBSRPSLY-QYTLZHMISA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Sekwencja

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

Postać fizyczna

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

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

Ta strona może zawierać tekst przetłumaczony maszynowo.

Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 10 - Combustible liquids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Temperatura zapłonu (°C): 87 °C - closed cup - (Dimethylsulfoxide)