1. Metabolic Enzyme/Protease
  2. CETP PCSK9 LDLR
  3. Obicetrapib hemicalcium

Obicetrapib hemicalcium  (Synonyms: TA-8995 hemicalcium; DEZ-001 hemicalcium; AMG-899 hemicalcium)

Cat. No.: HY-18778C
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Obicetrapib calcium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib calcium 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 calcium 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. It also exerts a synergistic effect with Ezetimibe (HY-17376) to reduce non-HDL-C levels and improve atherosclerosis. Obicetrapib calcium can be used in studies related to atherosclerosis and dyslipidemia.

For research use only. We do not sell to patients.

Obicetrapib hemicalcium

Obicetrapib hemicalcium Chemical Structure

CAS No. : 866399-89-5

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Description

Obicetrapib calcium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib calcium 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 calcium 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. It also exerts a synergistic effect with Ezetimibe (HY-17376) to reduce non-HDL-C levels and improve atherosclerosis. Obicetrapib calcium can be used in studies related to atherosclerosis and dyslipidemia[1][2].

In Vivo

Obicetrapib alone or in combination with Ezetimibe (HY-17376) or Ezetimibe plus Atorvastatin (HY-B0589) inhibits CETP, modulates lipoprotein metabolism, reduces atherosclerotic lesion burden, increases lesion stability, and (in triple therapy) promotes 44% regression of established lesions in apoE*3-LEIDEN/CETP transgenic mice[1].
Obicetrapib (28 weeks) reduces non-HDL-C by enhancing LDL receptor-mediated VLDL clearance, strongly inhibiting atherosclerotic lesion progression by 90% and improving plaque stability in APOE*3-Leiden.CETP mice fed a Western-type diet[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

742.65

Formula

C32H31F9N4O5·1/2Ca

CAS No.
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]

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Obicetrapib hemicalcium
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HY-18778C
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