MK0524, a fused indole-based antagonist of prostaglandin D2 (DP), has a Ki binding affinity of 0.57 nM and a Kd dissociation constant of 0.03 nM. With the exception of the TxA2 receptor (Ki = 2.95 nM), MK0524 has excellent selectivity over a number of other prostanoid receptors (EP family, FP, and IP). In a functional activity assay in platelet-rich plasma and washed platelets, MK0524 had an IC50 of 0.09 nM. [1]
MK-0524 has been shown to block nicotinic acid-induced cutaneous vasodilation and also antagonizes prostaglandin D1 (DP1) in a mouse DP1 functional assay at an IC50 of 1.1 nM. [2]
Technical information:
| Chemical Formula: | C21H19ClFNO4S | |
| CAS #: | 571170-77-9 | |
| Molecular Weight: | 435.9 | |
| Purity: > 98% | ||
| Appearance: | White | |
| Chemical Name: | [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid | |
| Solubility: | Up to 50 mM in DMSO | |
| Synonyms: | MK-0524, MK-0524A, MK0524, Laropiprant, Cordaptive, Tredaptive |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Sturino et al., Discovery of a Potent and Selective Prostaglandin D2 Receptor Antagonist, [(3R)-4-(4-Chlorobenzyl)- 7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic Acid (MK-0524). J. Med. Chem. 2007, 50, 794-806. Pubmed ID: 17300164 |
| 2. | Cheng et al., Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans. Proc. Natl. Acad. Sci. 2006, 103(17), 6682-6687. Pubmed ID: 16617107 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
