MRS 2500 tetraammonium salt

Name: MRS 2500 tetraammonium salt
Brand: Tocris Bioscience
SKU: 2159

Tocris Bioscience, part of Bio-Techne | Catalog # 2159

Citations (28)

COA / SDS

Highly potent and selective P2Y1 antagonist

Key Product Details

Description:	Highly potent and selective P2Y₁ antagonist
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
Purity:	≥96% (HPLC)
Molecular Weight:	629.29

View Full Technical Details for MRS 2500 tetraammonium salt

Technical Data
Citations

Biological Activity for MRS 2500 tetraammonium salt

MRS 2500 tetraammonium salt is a highly potent and selective antagonist of the platelet P2Y₁ receptor (K_i = 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 Information

Sold under license from the NIH, US Patent 10/169975

Technical Data for MRS 2500 tetraammonium salt

M. Wt	629.29
Formula	C₁₃H₁₈N₅O₈P₂I.4NH₃
Storage	Store at -20°C
Purity	≥96% (HPLC)
CAS Number	630103-23-0
PubChem ID	90488745
InChi Key	FVTFHHDVLNQSME-AVAGOIHISA-N
Smiles	IC4=NC1=C(C(NC)=N4)N=CN1[C@H]2C[C@H](OP(O)(O)=O)[C@@]3(COP(O)(O)=O)[C@@H]2C3.N.N.N.N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for MRS 2500 tetraammonium salt

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	12.59	20

Preparing Stock Solutions for MRS 2500 tetraammonium salt

The following data is based on the product molecular weight 629.29.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	7.95 mL	39.73 mL	79.45 mL
1 mM	1.59 mL	7.95 mL	15.89 mL
2 mM	0.79 mL	3.97 mL	7.95 mL
10 mM	0.16 mL	0.79 mL	1.59 mL

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References for MRS 2500 tetraammonium salt

References are publications that support the biological activity of the product.

Lu Stimulation of the P2Y₁ receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells. J.Pharmacol.Exp.Ther. 2007 PMID: 17626796
Cattaneo Antiaggregatory activity in human platelets of potent antagonists of the P2Y₁ receptor. Biochem.Pharmacol. 2004 PMID: 15476670
Hechler 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. 2006 PMID: 16236815
Kim 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 2003 PMID: 14584948