L1790

L-685,458

>96% (HPLC), solid

• Sinónimos: (5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide
• Fórmula empírica (notación de Hill): C₃₉H₅₂O₆N₄
• Número de CAS: 292632-98-5
• Peso molecular: 672.85
• Número MDL: MFCD03093402
• Código UNSPSC: 12352200
• ID de la sustancia en PubChem: 329817393
• NACRES: NA.77

Propiedades

• Análisis: >96% (HPLC)
• formulario: solid
• color: white
• solubilidad: DMSO: >10 mg/mL
• emisor: Merck & Co., Inc., Kenilworth, NJ, U.S.
• temp. de almacenamiento: −20°C
• cadena 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
• Clave InChI: MURCDOXDAHPNRQ-ZJKZPDEISA-N
• Información sobre el gen: 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)

Descripción

Aplicación

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

Acciones bioquímicas o fisiológicas

L-685,458 mimics the transition state in aspartyl protease. It possesses an IC50 of 17nM with respect to inhibition of Aβ synthesis. 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). L-685,458 targets the active site and substrate binding site of the enzyme.

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

Características y beneficios

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable
• Equipo de protección personal: Eyeshields, Gloves, type N95 (US)