A pyridine derivative that acts as a highly selective antagonist of A3 receptor with excellent potency in both humans and rodents (Ki = 18.9 nM for human A3R, and 113 nM for rat A3R). Exhibits only a trivial antagonistic activity towards A1 and A2A receptors (Ki = 15.6 µM and 2.05 µM for rat A1R and A2AR, respectively). Abolishes the agonistic effects of Cl-IB-MECA (Cat. No. 119139) on A3R-mediated proliferation of primary human coronary smooth muscle cells. Also, reported to block NECA (Cat. No. 119140)-induced bronchoconstriction in an allergic murine model.
Chen, Z., 2012. FASEB J.26, 1855. Chanyshev, B., et al. 2012. Pharmacol Res.65, 338. Choi, I., et al. 2011. Am J Pathol.179, 2042. Fan, M., et al. 2003. Am J Physiol Lung Cell Mol Physiol.284, L1012. Li, A. H., et al. 1998. J Med Chem.41, 3186. Jacobson, K. A., et al. 1999. Drug Dev Res.45, 113.
Product Information
CAS number
212329-37-8
Form
Clear to light brown oil
Hill Formula
C₂₃H₂₉NO₃S
Chemical formula
C₂₃H₂₉NO₃S
Reversible
Y
Structure formula Image
Applications
Biological Information
Primary Target
A₃ Receptor
Primary Target K<sub>i</sub>
18.9 nM
Purity
≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity
Standard Handling
Storage
+2°C to +8°C
Protect from Light
Protect from light
Do not freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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