L1790

L-685,458

>96% (HPLC), solid

• Synonyme(s) : (5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide
• Formule empirique (notation de Hill): C₃₉H₅₂O₆N₄
• Numéro CAS: 292632-98-5
• Poids moléculaire : 672.85
• Numéro MDL: MFCD03093402
• Code UNSPSC : 12352200
• ID de substance PubChem : 329817393
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: >96% (HPLC)
• Forme: solid
• Couleur: white
• Solubilité: DMSO: >10 mg/mL
• Auteur: Merck & Co., Inc., Kenilworth, NJ, U.S.
• Température de stockage: −20°C
• Chaîne 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
• Clé InChI: MURCDOXDAHPNRQ-ZJKZPDEISA-N
• Informations sur le gène: 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)

Description

Application

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.

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable
• Équipement de protection individuelle: Eyeshields, Gloves, type N95 (US)