Vorapaxar (MK-5348)

Catalog No.S8067 Synonyms: SCH 530348

For research use only.

Vorapaxar (SCH 530348, MK-5348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.

Vorapaxar (MK-5348) Chemical Structure

CAS No. 618385-01-6

Selleck's Vorapaxar (MK-5348) has been cited by 7 Publications

Purity & Quality Control

Choose Selective PAR Inhibitors

Biological Activity

Description Vorapaxar (SCH 530348, MK-5348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.
Targets
PAR-1 [1]
(Cell-free assay)
8.1 nM(Ki)
In vitro

SCH 530348 is a synthetic tricyclic 3-phenylpyridine and an orally active himbacine-based thrombin-receptor antagonist. SCH 530348 shows potent inhibition of thrombin-induced platelet aggregation with an IC50 of 47 nM and haTRAP-induced platelet aggregation with an IC50 of 25 nM, whereas it shows no inhibition of platelet aggregation induced by other agonists such as ADP, collagen and a PAR-4 agonist peptide. SCH 530348 also has no affect on the prothrombin time (PT), partial thromboplastin time (PTT), or activated partial thromboplastin time (aPTT). Moreover, SCH 530348 causes no increase in the bleeding time or in surgical bleeding compared with inactive control. SCH530348 is found to be selective for PAR-1 when tested over a number of ion channels and receptors, including PAR-4 receptor. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 NY\KNGl4TnWwY4Tpc44h[XO|YYm= MlWzNVUhdWmwcx?= Mo\GRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBRSVJzIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiY3:t[ZhxemW|c3nu[{BI[WyyaHGxOUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIhiXFKDUD3pcoR2[2WmIHPhcINqfW1ibX;ibYxqgmG2aX;uJJBz\WmwY4XiZZRm\CCob4KgNVUhdWmwczDmc4xtd3enZDDifUBp[VSUQWCgZYRlcXSrb36gZpkh[2GuY3n1cU01KGS7ZTDiZZNm\CCITFnQVkBie3OjeTygTWM2OCB;IECuNFY1KM7:TT6= NFrUPY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe0OVUxPyd-Mki3OFU2ODd:L3G+
Assay
Methods Test Index PMID
Western blot AKT / JNK / NF-κB / GAPDH ; ATM / ATR / GSK / Cyclin D1 / GAPDH ; fibronectin / tubulin 31059055 29114573
Immunofluorescence proinflammatory signaling ; PLP / Olig2 25587041 31911460
In vivo SCH 530348 is well absorbed in rat (68%; 10 mg/kg) and in monkey (82%; 1 mg/kg) models. Tmax is observed at about 3 h in rats and 1 h in monkeys. The elimination half-life is 5.1 h in rats and 13 h in monkeys. The oral bioavailability is 33% in rats and 86% in monkeys. In preclinical studies in cynomolgus monkey platelets, oral administration of SCH 530348 at a dose greater than 0.1 mg/kg resulted in 100% inhibition of thrombin-receptor agonist peptide (TRAP)-induced platelet aggregation for 24 h with partial recovery occurring at 48 h. [1]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: cynomolgus monkeys
  • Dosages: 0.5, 0.3, 0.1, and 0.05 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 492.58
Formula

C29H33FN2O4

CAS No. 618385-01-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)NC1CCC2C(C1)CC3C(C2C=CC4=NC=C(C=C4)C5=CC(=CC=C5)F)C(OC3=O)C

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