MRS 2365
- CAS No.
- 436847-09-5
- Chemical Name:
- MRS 2365
- Synonyms
- MRS 2365;MRS 2365, CID: 73755043;Diphosphoric acid, P-[[(1R,2R,3S,4R,5S)-4-[6-amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl] ester;[[(1R,2R,3S,4R,5S)-4-[6-Amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl]diphosphoricacidmonoestertrisodiumsalt;[[(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
- CBNumber:
- CB7847532
- Molecular Formula:
- C13H19N5O9P2S
- Molecular Weight:
- 483.33
- MDL Number:
- MFCD08703094
- MOL File:
- 436847-09-5.mol
- TDS File:
- TDS
| Boiling point | 875.5±75.0 °C(Predicted) |
|---|---|
| Density | 2.37±0.1 g/cm3(Predicted) |
| storage temp. | Desiccate at -20°C |
| pka | 1.42±0.10(Predicted) |
| form | Powder |
| Water Solubility | Soluble in water (supplied pre-dissolved at a concentration of 10mM) |
| FDA UNII | YQI4GCR8ST |
MRS 2365 price More Price(5)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biosynth | FM30703 | MRS 2365 | 436847-09-5 | 1mg | $917.94 | 2026-06-04 | Buy |
| ApexBio Technology | B5264 | MRS 2365 | 436847-09-5 | 1mg | $900 | 2026-05-06 | Buy |
| Tocris | 2157 | MRS2365 ≥98%(HPLC) | 436847-09-5 | 1 | $389 | 2021-12-16 | Buy |
| TRC | M750253 | MRS2365 | 436847-09-5 | 1mg | $355 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | API0008065 | MRS 2365 95.00% | 436847-09-5 | 5MG | $501.99 | 2021-12-16 | Buy |
MRS 2365 Chemical Properties,Uses,Production
Uses
MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors[1][2][3][4].
Biological Activity
Highly potent, selective P2Y 1 receptor agonist (EC 50 = 0.4 nM). Displays no activity at P2Y 12 receptors and only very low agonist activity at P2Y 13 receptors (at concentrations up to 1 μ M).
in vivo
MRS2365 (0.03-0.3 mg/kg; i.p.; single dose) significantly alleviates the mechanical allodynia in the male wistar rats neuropathy (Seltzer) model with dose-dependent manner[3].
MRS2365 (0.1-2 mg/kg; i.p.; single dose) increases the paw withdrawal threshold (PWT) in male wistar rats with neuropathic pain model[3].
| Animal Model: | Male Wistar rats with neuropathic pain(250-350 g)[3]. |
| Dosage: | 0.03, 0.1, 0.3, 1 and 2 mg/kg. |
| Administration: | Intraperitoneal injection; single dose. |
| Result: | Relieved mechanical allodynia and increased the paw withdrawal threshold. |
IC 50
P2Y1 Receptor: 0.4 nM (EC50)
References
[1] Mariya Chhatriwala, et al. 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. 2004 Dec;311(3):1038-43. DOI:10.1124/jpet.104.068650
[2] D M Bourdon, et al. (N)-methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets. J Thromb Haemost. 2006 Apr;4(4):861-8. DOI:10.1111/j.1538-7836.2006.01866.x
[3] Andó RD, et al. A comparative analysis of the activity of ligands acting at P2X and P2Y receptor subtypes in models of neuropathic, acute and inflammatory pain. Br J Pharmacol. 2010 Mar;159(5):1106-17. DOI:10.1111/j.1476-5381.2009.00596.x
[4] Gao ZG, et al. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Mol Pharmacol. 2017 Nov;92(5):613-626. DOI:10.1124/mol.117.109660
MRS 2365 Preparation Products And Raw materials
Raw materials
Preparation Products
MRS 2365 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| 3B Pharmachem (Wuhan) International Co.,Ltd. | 18930552037 | 3bsc@sina.com | China | 15813 | 69 |
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8435 | 60 |
| Jinan Yaoyan Pharmaceutical Co., Ltd. | jnyaoyan@163.com | China | 3057 | 58 | |
| Nanjing Meihao Pharmaceutical Technology Co., Ltd. | meitaochem@126.com | meitaochem@126.com | China | 19087 | 58 |
| Alfa Chemistry | +1-5166625404; | Info@alfa-chemistry.com | United States | 20000 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| JinOu Biomedical (Nanjing) Co., Ltd. | 13000000000 | jinoupharma@163.com | China | 11706 | 58 |
| Shanghai Universal Biotech Co.,Ltd | 15921930842 15921930842 | yh-wang@univ-bio.com | China | 25030 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
