866399-89-5
Chemical Structure
Obicetrapib hemicalcium
Synonym(s): TA-8995 hemicalcium; DEZ-001 hemicalcium; AMG-899 hemicalcium
- CAS No.: 866399-89-5
- Formula:C32H31F9N4O5·1/2Ca
- Molecular Weight:742.65
SMILES: FC(F)(F)C1=CC(C(F)(F)F)=CC(CN(C2=NC=C(OCCCC(O)=O)C=N2)[C@@H]3C4=CC(C(F)(F)F)=CC=C4N([C@@H](C3)CC)C(OCC)=O)=C1.[Ca].[1/2]
Biological Activity: Obicetrapib hemicalcium (TA-8995 hemicalcium) is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib hemicalcium shifts the plasma lipoprotein profile toward more HDL-C particles, reduces circulating PCSK9 levels, increases hepatic LDLR expression and LDLR mRNA levels, and promotes hepatic clearance of VLDL remnants. Obicetrapib hemicalcium increases the number of large HDL particles, reduces the number and area of atherosclerotic lesions and alleviates lesion severity, increases the proportion of unaffected arterial segments, improves lesion stability, and promotes regression of aortic root lesions. Obicetrapib hemicalcium also exerts a synergistic effect with Ezetimibe (HY-17376) to reduce non-HDL-C levels and improve atherosclerosis. Obicetrapib hemicalcium can be used in studies related to atherosclerosis and dyslipidemia[1][2].
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Obicetrapib hemicalcium | Obicetrapib hemicalcium (TA-8995 hemicalcium) is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib hemicalcium shifts the plasma lipoprotein profile toward more HDL-C particles, reduces circulating PCSK9 levels, increases hepatic LDLR expression and LDLR mRNA levels, and promotes hepatic clearance of VLDL remnants. Obicetrapib hemicalcium increases the number of large HDL particles, reduces the number and area of atherosclerotic lesions and alleviates lesion severity, increases the proportion of unaffected arterial segments, improves lesion stability, and promotes regression of aortic root lesions. Obicetrapib hemicalcium also exerts a synergistic effect with Ezetimibe (HY-17376) to reduce non-HDL-C levels and improve atherosclerosis. Obicetrapib hemicalcium can be used in studies related to atherosclerosis and dyslipidemia. | |||||||||||||||||||||
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- [1]. Toth PP, et al. Obecetrapib, CETP inhibition, and atherosclerosis: there is light at the end of the tunnel. J Lipid Res. 2026 May;67(5):101029. [Content Brief]
- [2]. Inia JA, et al. Obicetrapib and ezetimibe enhance LDL receptor-mediated VLDL clearance and regress atherosclerosis on atorvastatin background. Journal of lipid research. 2026 May;67(5):101028. [Content Brief]
Keywords