Vorapaxar (SCH 530348)

Catalog No.: A12832

PAR-1 Antagonist

Vorapaxar (SCH 530348)

Vorapaxar (SCH 530348) Chemical Structure

CAS NO. 618385-01-6

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

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  • Cansu Tekin, .et al. Macrophage-secreted MMP9 induces mesenchymal transition in pancreatic cancer cells via PAR1 activation, Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
  • Cansu Tekin, .et al. PAR1 signaling on tumor cells limits tumor growth by maintaining a mesenchymal phenotype in pancreatic cancer, Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
  • Claushuis TA, .et al. Thrombin contributes to protective immunity in pneumonia-derived sepsis via fibrin polymerization and platelet-neutrophil interactions, J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
  • Maaike Waasdorp, .et al. Plasmin reduces fibronectin deposition by mesangial cells in a protease-activated receptor-1 independent manner, Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
  • Joseph C. Mudd, .et al. Inflammatory Function of CX3CR1+ CD8+ T Cells in Treated HIV Infection Is Modulated by Platelet Interactions, J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
  • Corey E. Tabit, .et al. Elevated Angiopoietin-2 Level in Patients With Continuous-Flow Left Ventricular Assist Devices Leads to Altered Angiogenesis and Is Associated With Higher Non-Surgical Bleeding, Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285

Biological Activity

Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.
Targets
PAR-1
8.1 nM(Ki)
In vitro DMSO 96 mg/mL (194.89 mM)
Water Insoluble
Ethanol 96 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 20.3 mL 101.51 mL 203.01 mL
0.5 mM 4.06 mL 20.3 mL 40.6 mL
1 mM 2.03 mL 10.15 mL 20.3 mL
5 mM 0.41 mL 2.03 mL 4.06 mL

*The above data is based on the productmolecular weight 492.58. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A12832
Actions Antagonist
CAS No. 618385-01-6
Formula C29H33FN2O4
M. Wt 492.58
Purity >98%
Synonyms SCH530348, SCH-530348, MK-5348, MK5348, MK 5348
SMILES CCOC(=O)N[[email protected]@H]1CC[[email protected]@H]2[[email protected]@H](C1)C[[email protected]@H]3[[email protected]]([[email protected]]2/C=C/C4=NC=C(C=C4)C5=CC(=CC=C5)F)[[email protected]](OC3=O)C
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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