L1790

L-685,458

>96% (HPLC), solid

• Synonim(y): (5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide
• Wzór empiryczny (zapis Hilla): C₃₉H₅₂O₆N₄
• Numer CAS: 292632-98-5
• Masa cząsteczkowa: 672.85
• Numer MDL: MFCD03093402
• Kod UNSPSC: 12352200
• Identyfikator substancji w PubChem: 329817393
• NACRES: NA.77

Właściwości

• Próba: >96% (HPLC)
• Formularz: solid
• kolor: white
• rozpuszczalność: DMSO: >10 mg/mL
• inicjator: Merck & Co., Inc., Kenilworth, NJ, U.S.
• temp. przechowywania: −20°C
• ciąg SMILES: O[C@@H]([C@H](CC1=CC=CC=C1)NC(OC(C)(C)C)=O)C[C@@H](CC2=CC=CC=C2)C(N[C@@H](CC(C)C)C(N[C@@H](CC3=CC=CC=C3)C(N)=O)=O)=O
• InChI: 1S/C39H52N4O6/c1-26(2)21-33(37(47)41-32(35(40)45)24-29-19-13-8-14-20-29)42-36(46)30(22-27-15-9-6-10-16-27)25-34(44)31(23-28-17-11-7-12-18-28)43-38(48)49-39(3,4)5/h6-20,26,30-34,44H,21-25H2,1-5H3,(H2,40,45)(H,41,47)(H,42,46)(H,43,48)/t30-,31+,32+,33+,34-/m1/s1
• Klucz InChI: MURCDOXDAHPNRQ-ZJKZPDEISA-N
• informacje o genach: human ... APH1A(51107) , APH1B(83464) , NCSTN(23385) , NOTCH1(4851) , NOTCH2(4853) , NOTCH3(4854) , NOTCH4(4855) , PSEN1(5663) , PSEN2(5664) , PSENEN(55851) ; mouse ... Aph1a(226548) , Aph1b(208117) , Ncstn(59287) , Notch1(18128) , Notch2(18129) , Notch3(18131) , Notch4(18132) , Psen1(19164) , Psen2(19165) , Psenen(66340) ; rat ... Aph1a(365872) , Aph1b(300802) , Ncstn(289231) , Notch1(25496) , Notch2(29492) , Notch3(56761) , Notch4(406162) , Psen1(29192) , Psen2(81751) , Psenen(292788)

Opis

Zastosowanie

L-685,458 has been used to attenuate Notch signalling in ovary culture.[1] It has also been used to analyze the specificity of the γ-secretase activity in brain tissue samples.[2]

Działania biochem./fizjol.

L-685,458 is a potent, selective, structurally novel γ-secretase inhibitor; equipotent inhibitor of both Aβ_1-42 and Aβ_1-40 production.

L-685,458 mimics the transition state in aspartyl protease. It possesses an IC50 of 17nM with respect to inhibition of Aβ synthesis.[3] It is known to block Notch (neurogenic locus notch homolog protein) signaling, which in turn reduces ERK (extracellular signal regulated kinase) phosphorylation by EGF (epidermal growth factor).[4] L-685,458 targets the active site and substrate binding site of the enzyme.[5]

Cechy i korzyści

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Informacje prawne

Manufactured and sold under license from Merck & Co., Inc., Kenilworth, NJ, U.S.

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable
• Środki ochrony indywidualnej: Eyeshields, Gloves, type N95 (US)