SBC-115076

Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with important roles in lipoprotein metabolism. PCSK9 overexpression in wild-type mice doubles plasma total cholesterol, possibly through acceleration of degradation of the LDL receptor (LDLR). SBC-115076 is an inhibitor of PCSK9 action that blocks LDLR degradation in HEK293T cells expressing PCSK9. Through this mechanism, submicromolar concentrations of SBC-115076 increase the uptake of LDL by liver cells in vitro. SBC-115076 is effective in vivo, lowering cholesterol levels in mice that are fed a high fat diet.Formal Name: 1,5-dihydro-3-hydroxy-4-[3-methyl-4-(phenylmethoxy)benzoyl]-1-[3-(4-morpholinyl)propyl]-5-(4-pyridinyl)-2H-pyrrol-2-one. CAS Number: 489415-96-5. Molecular Formula: C31H33N3O5. Formula Weight: 527.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 234, 320 nm. SMILES: CC1=CC(C(C(C(C2=CC=NC=C2)N3CCCN4CCOCC4)=C(O)C3=O)=O)=CC=C1OCC5=CC=CC=C5. InChi Code: InChI=1S/C31H33N3O5/c1-22-20-25(8-9-26(22)39-21-23-6-3-2-4-7-23)29(35)27-28(24-10-12-32-13-11-24)34(31(37)30(27)36)15-5-14-33-16-18-38-19-17-33/h2-4,6-13,20,28,36H,5,14-19,21H2,1H3. InChi Key: UNINQWCCZAGYSH-UHFFFAOYSA-N.