MRS 2500 tetraammonium salt
Cat. No. 2159
Chemical Name: (1R*,2S*)-4-[2-Iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester tetraammonium salt
Biological ActivityHighly potent and selective antagonist of the platelet P2Y1 receptor (Ki = 0.78 nM). Inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Inhibits the upregulation of NTPDase1 by ATPγS. Prevents thrombus formation in vivo.
Licensing InformationSold under license from the NIH, US Patent 10/169975
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Kim et al (2003) 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. J.Med.Chem 46 4974. PMID: 14584948.
Cattaneo et al (2004) Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor. Biochem.Pharmacol. 68 1995. PMID: 15476670.
Hechler et al (2006) MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3', 5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice. J.Pharmacol.Exp.Ther. 316 556. PMID: 16236815.
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.
If you know of a relevant citation for this product please let us know.
View Related Products by Target
Keywords: MRS 2500 tetraammonium salt, supplier, potent, selective, P2Y1, antagonists, Receptors, Purinergic, purinoceptors, MRS2500, prevents, thrombus, formation
Find multiple products by catalog number
New Products in this Area
GPR35 agonist; more potent than zaprinast (Cat. No. 0947)H2L 5765834
LPA1,3,5 antagonistCYM 50308
Potent and selective S1P4 agonistH2L5186303
Potent and selective LPA2 receptor antagonistMEDICA 16
FFA1 (GPR40) agonist. Also inhibits ATP citrate lyaseBX 471
Potent, selective CCR1 antagonistPF 04418948
Potent and selective EP2 receptor antagonistLatanoprost
FP prostaglandin receptor agonist; also exhibits agonist activity at EP1 and EP3 receptorsGRI 977143
Selective LPA2 receptor non-lipid agonistCYM 50260
Potent and selective S1P4 agonistG-36
Selective GPR30 antagonistStrontium chloride
Calcium sensing receptor (CaSR) agonistCS 2100
Selective S1P1 agonistSMANT hydrochloride
Inhibits Smoothened (Smo) accumulationTUG 891
Potent and selective GPR120 agonist
Potent, selective LRRK2 inhibitor
Tocris is the first to launch GSK2578215A, licensed from GlaxoSmithKline, for the study of Parkinson's Disease.