| Identification | Back Directory | [Name]
sbc-115076 | [CAS]
489415-96-5 | [Synonyms]
CS-2068
CS-1638
sbc-115076
SBC-115076;SBC 115076;SBC115076
4-[hydroxy-(3-methyl-4-phenylmethoxyphenyl)methylidene]-1-(3-morpholin-4-ylpropyl)-5-pyridin-4-ylpyrrolidine-2,3-dione
1,5-Dihydro-3-hydroxy-4-[3-methyl-4-(phenylmethoxy)benzoyl]-1-[3-(4-morpholinyl)propyl]-5-(4-pyridinyl)-2H-pyrrol-2-one
2H-Pyrrol-2-one, 1,5-dihydro-3-hydroxy-4-[3-methyl-4-(phenylmethoxy)benzoyl]-1-[3-(4-morpholinyl)propyl]-5-(4-pyridinyl)- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C31H33N3O5 | [MDL Number]
MFCD03296540 | [MOL File]
489415-96-5.mol | [Molecular Weight]
527.61 |
| Chemical Properties | Back Directory | [Boiling point ]
754.2±60.0 °C(Predicted) | [density ]
1.266±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO:46.0(Max Conc. mg/mL);87.18(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.95(Max Conc. mM)
DMF:2.0(Max Conc. mg/mL);3.79(Max Conc. mM) | [form ]
A crystalline solid | [pka]
4.50±1.00(Predicted) | [color ]
White to off-white | [SMILES]
CC1=CC(C(C(C(C2=CC=NC=C2)N3CCCN4CCOCC4)=C(O)C3=O)=O)=CC=C1OCC5=CC=CC=C5 |
| Hazard Information | Back Directory | [Uses]
SBC-115,076 is an anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compound used in treatment and/or prevention of cardiovascular diseases and hypercholesterolemia. | [Biological Activity]
SBC-115076 is an inhibitor of PCSK9 (proprotein convertase subtilisin-kexin 9). PCSK9 binds to the LDL receptor, preventing it from removing LDL cholesterol from the blood. SBC-115076 was shown to inihbit PCSK9, blocking LDLR degradation in HEK293T cells expressing PCSK9 and to increase the uptake of LDL by liver cells in vitro. SBC-115076 lowered cholesterol levels in mice fed a high f at diet. | [in vivo]
SBC-115076 (4 mg/kg; s.c.; daily for 3 weeks) reduces obesity and dyslipidemia, as well as improves insulin sensitivity in HFD-fed rats[1]. | Animal Model: | Female Wistar rats (high-fat diet (HFD)- fed)[1] | | Dosage: | 4 mg/kg | | Administration: | S.c.; daily for 3 weeks | | Result: | Superior to atorvastatin in instigating weight loss, cholesterol reduction, and attenuation of mitochondrial oxidative stress in oxidative muscle fibers of obese female rats.
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| Company Name: |
D&C Chemicals
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| Tel: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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