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Cat. No. Product Name CAS No. Information
PC-63147

Tenapanor

1234423-95-0

Tenapanor (AZD-1722;RDX5791) is a potent, selective inhibitor of the Na+/H+ exchanger 3 (NHE3) with IC50 of 5 and 10 nM for human and rat NHE3, respectively; displays no inhibitory activities against . human intestinal transporters NHE1 (SLC9A1), NHE2 (SLC9A2), TGR5 (GPBAR1), ASBT and Pit-1; inhibits sodium uptake acted exclusively in the gastrointestinal tract in vivo, reduces extracellular fluid volume, left ventricular hypertrophy, albuminuria, and blood pressure in salt-fed nephrectomized rats, also reduces sodium and phosphorus absorption, protects against vascular calcification in rat model of CKD.

Dyslipidemia

Phase 3 Clinical

PC-63146

Tenapanor hydrochloride

1234365-97-9

Tenapanor (AZD-1722;RDX5791) is a potent, selective inhibitor of the Na+/H+ exchanger 3 (NHE3) with IC50 of 5 and 10 nM for human and rat NHE3, respectively; displays no inhibitory activities against . human intestinal transporters NHE1 (SLC9A1), NHE2 (SLC9A2), TGR5 (GPBAR1), ASBT and Pit-1; inhibits sodium uptake acted exclusively in the gastrointestinal tract in vivo, reduces extracellular fluid volume, left ventricular hypertrophy, albuminuria, and blood pressure in salt-fed nephrectomized rats, also reduces sodium and phosphorus absorption, protects against vascular calcification in rat model of CKD.

Dyslipidemia

Phase 3 Clinical

PC-61150

Seladelpar

851528-79-5

A potent, selective, orally bioavailable PPARδ agonist for the treatment of dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).

Dyslipidemia

Phase 2 Clinical

PC-35463

CKD-519

1402796-27-3 CKD-519 (Rocacetrapib, CKD519) is a potent, selective cholesteryl ester transfer protein (CETP) inhibitor, inhibits the CETP-mediated transfer of cholesteryl ester in human serum with IC50 of 2.3 nM; exhibites a maximum of 70%-86% inhibition of CETP activity and 25%-48% increase of HDL-C levels after two weeks of oral administration of 1, 3, or 10 mg/kg in transgenic mice expressing human CETP/apolipoprotein AI; CKD-519 (Rocacetrapib, CKD519) is being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol.

Dyslipidemia

Phase 2 Clinical

PC-63559

Obicetrapib

866399-87-3 Obicetrapib (AMG-899, TA-8995, DEX-001) is a potent, ora cholesteryl ester transfer protein (CETP) inhibitor for treatment of dyslipidaemia.

Dyslipidemia

Phase 2 Clinical

PC-43496

Evacetrapib

1186486-62-3 Evacetrapib (LY2484595) is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) with IC50 of 5.5 nM for human recombinant CETP protein; inhibits CETP activity in human plasma with IC50 of 36 nM; shows no significant inhibition in the CEREP cell surface receptor screening, as well as the nuclear receptor panel; exhibits an ex vivo CETP inhibition ED50 of < 5 mg/kg at 8 h post oral dose and significantly elevates HDL cholesterol in vivo; Evacetrapib is a potent and selective CETP inhibitor without torcetrapib-like off-target liabilities.

Dyslipidemia

Discontinued

PC-43398

Avasimibe

166518-60-1 Avasimibe (CI-1011, PD-148515) is a potent, selective inhibitor of acyl-CoA: cholesterol O-acyl transferase (ACAT) with IC50 of 60 nM; potently reduces plasma cholesterol in chow-fed rats and in rabbits fed a cholesterol-free, casein-containing diet characterized by both hepatic overproduction of apo B-containing lipoproteins and delayed lipoprotein clearance; decreases both VLDL and LDL apolipoprotein B production in miniature pigs; synergistically reduces cholesteryl ester content in THP-1 macrophages combined with Atorvastatin,

Dyslipidemia

Phase 3 Discontinued

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