Chemical Structure : RWJ-58259
CAS No.:
315203-31-7
RWJ-58259
(RWJ 58259)
Catalog No.: PC-20577Not For Human Use, Lab Use Only.
RWJ-58259 (RWJ58259) is a potent, selective thrombin receptor PAR-1 antagonist with binding IC50 of 0.15 uM, and IC50 of 0.07 uM in RASMC calcium mobilization assays.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
RWJ-58259 (RWJ58259) is a potent, selective thrombin receptor PAR-1 antagonist with binding IC50 of 0.15 uM, and IC50 of 0.07 uM in RASMC calcium mobilization assays.
RWJ-58259 exhibit an IC50 of 0.02 uM in PAR1-mediated iCa2+ mobilization assay in presence of 5 μM TFLLRN-NH2.
RWJ-58259 demonstrated in vivo antirestenotic activity in a rat balloon angioplasty model.
Perivascular administration of RWJ-58259 (10 mg) significantly reduced neointimal thickness in rats.
Physicochemical Properties
|
M.Wt
|
791.73
|
|
Formula
|
C40H42Cl2F2N8O3
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
O=C(NCC1=CC=CC=C1)[C@@H](NC([C@@H](NC(NC2=CC3=C(C=C2)C(CN4CCCC4)=NN3CC5=C(Cl)C=CC=C5Cl)=O)CC6=CC=C(F)C(F)=C6)=O)CCN
|
References
1. Zhang HC, et al. J Med Chem. 2001 Mar 29;44(7):1021-4.
2. Andrade-Gordon P, et al. J Pharmacol Exp Ther. 2001 Jul;298(1):34-42.
Contact Us
sales@probechem.com
