211513-37-0
2-Methylpropanethioic acid S-[2-[1-(2-ethylbutyl)cyclohexylcarboxamido]phenyl] ester
CAS: 211513-37-0
Molecular Formula: C23H35NO2S
211513-37-0 - Names and Identifiers
211513-37-0 - Physico-chemical Properties
| Molecular Formula | C23H35NO2S |
| Molar Mass | 389.59 |
| Density | 1.06±0.1 g/cm3(Predicted) |
| Melting Point | 63-63.5 °C |
| Boling Point | 528.9±33.0 °C(Predicted) |
| Solubility | 78 mg/mL in DMSO <1 mg/mL in Water 78 mg/mL in Ethanol |
| pKa | 13.95±0.70(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Use | A CETP inhibitor |
| In vitro study | Dalcetrapib regulates cholesteryl ester transfer protein activity. Addition of Dalcetrapib to human plasma induces conformational changes in cholesteryl ester transfer protein. The CETP-induced pre-β-high-density lipoprotein in human plasma was unchanged at concentrations of Dalcetrapib below 3 µm but increased when it was 10 µm. Dalcetrapib significantly increased the formation of pre-β-high-density lipoprotein. Dalcetrapib inhibits cholesterol ester transfer protein activity by 50% in human plasma at a concentration of 9 μm. Dalcetrapib inhibited cholesteryl ester transfer protein activity in Hep G2 cells in a dose-dependent manner. |
| In vivo study | Dalcetrapib treatment significantly increased high-density lipoprotein cholesterol levels. In the injection [. Dalcetrapib inhibited cholesterol ester transfer protein activity by 95% at a dose of 30 mg/kg orally in a male Japanese white rabbit model. Dalcetrapib increased plasma HDL cholesterol levels by 27% and 54%, respectively. Oral doses of 30 mg/kg or 100 mg/kg 3 times daily significantly increased serum high-density lipoprotein cholesterol in male Japanese white rabbits. Dalcetrapib significantly increased HDL-C levels. After 5 and 7 months of Dalcetrapib treatment, the proportion of HDL 2-C to HDL 3-C increased significantly compared with the control group, the results showed that the inhibition of cholesteryl ester transfer protein activity by Dalcetrapib affected the change of high density lipoprotein subfraction and preferentially increased HDL 2C content. Dalcetrapib treatment increased serum esterase activity and high-density lipoprotein-associated platelet-activating factor acetylhydrolase activity, but decreased plasma lysophosphatidylcholine concentrations. |
211513-37-0 - Introduction
Dalcetrapib (JTT-705, RO4607381) is a rhCETP inhibitor with an IC50 of 0.2 μM, which increases high density lipoprotein (HDL) cholesterol in plasma.
Last Update：2022-10-16 17:14:55
211513-37-0 - Reference Information
| biological activity | Dalcetrapib (JTT-705, RO4607381) is a rhCETP inhibitor with an IC50 of 0.2 μM, which increases high density lipoprotein (HDL) cholesterol in plasma. Phase 3. |
| Target | Value |
| rhCETP | 0.2 μM |
Last Update：2024-04-10 22:29:15
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View History
211513-37-0
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