In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Vorapaxar is a potent PAR1 inhibitor and antiplatelet that was completed in phase III clinical trial.
PAR1 is one of the 4 thrombin receptor types that belong to G-protein coupled receptors super family. By binding to thrombin, the N-terminal at the arginine 41 and serine 42 bond of PAR1 on platelet surface can be enzymatically cleaved, resulting in the activation of platelet and subsequent hemostasis process.
Vorapaxar is an ethyl-carbamate molecule that derived from natural himbacine and has been determined to be a selective PAR 1 inhibitor through direct binding. In human plasma enriched with platelets, Vorapaxar was able to inhibit the aggregation of platelet with an IC50 value of 47 nM. In addition, vorapaxar is able to inhibitthe platelet aggregation that triggered by the addition of thrombin receptor activating peptide with an IC50 value of 25 nM. At the same time, however, vorapaxar does not interfere thrombin’s enzymatic activity on fibrin formation or thromboxane A2 receptors-induced platelet aggregation, as was demonstrated by its inability to inhibit platelet aggregation that induced by the addition of 9,11-dideoxy-11R,9R-epoxymethanoprostaglandin F2R (a thromboxane mimetic) .
In vivo, oral administration of 0.1 mg/kg of Vorapaxar completely inhibited the platelet aggregation monkey model for 24 hrs. In phase III clinical trial that involved 26,449 patients , administration of vorapaxar (2.5 mg/day) reduced the occurrence of cardiovascular death or ischemic events compared with placebo group by a statistically significant 1.2%.
. Chackalamannil S & XIA, Y. Thrombin receptor (PAR-1) antagonists as novel antithrombotic agents. Expert Opinion on Therapeutic Patents, 2006.16:493-505.
. Chackalamannil S, Wang Y, Greenlee W J et al. 2008. Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem, 2008,51: 3061-3064.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥24.65mg/mL in DMSO|
|Chemical Name||ethyl N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-1-methyl-3-oxo-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-1H-benzo[f]benzofuran-6-yl]carbamate|
|Description||Vorapaxar（SCH 530348）是一种有效的具有口服活性的凝血酶受体（PAR-1）拮抗剂，Ki值为8.1 nM。|
|IC50||8.1 nM (Ki)|