MRS 2365 ([[(1R,2R,3S,4R,5S)-4-[6-Amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl] diphosphoric acid mono ester trisodium salt) | 436847-09-5

name

mrs 2365

chemical name

[[(1r,2r,3s,4r,5s)-4-[6-amino-2-(methylthio)-9h-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl] diphosphoric acid mono ester trisodium salt

activity

highly potent, selective p2y1 receptor agonist (ec50 = 0.4 nm). displays no activity at p2y12 receptors and only very low agonist activity at p2y13 receptors (at concentrations up to 1 μm). increases the upregulation of ntpdase1 by atpγs.

MW

549.28

Formula:

c13h16n5o9p2sna3

Solubility:

soluble in water (supplied pre-dissolved at a concentration of 10mm)

Purity:

>98 %

Storage:

store at -20°c

CAS No:

436847-09-5

Ravi et al (2002) Adenine nucleotide analogues locked in a northern methanocarba conformation: enhanced stability and potency as P2Y₁ receptor agonists. J.Med.Chem. 45 2090. PMID: 11985476.

Chhatriwala et al (2004) Induction of novel agonist selectivity for the ADP-activated P2Y₁ receptor versus the ADP-activated P2Y₁₂ and P2Y₁₃ receptors by conformational constraint of an ADP analog. J.Pharmacol.Exp.Ther. 311 1038. PMID: 15345752.

Lu et al (2007) Stimulation of the P2Y₁ receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells. J.Pharmacol.Exp.Ther. 323 157. PMID: 17626796.