MRS2179 (ammonium salt) |
Catalog No.GC44249
One-Click Copy Product Info
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MRS2179 is a competitive P2Y1 receptor antagonist (Kb = 100 nM) with no appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 μM, or at P2Y12 and P2Y13 at concentrations up to 10 and 100 μM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 228264-19-5
Sample solution is provided at 25 µL, 10mM.
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MRS2179 is a competitive purinergic P2Y1 receptor antagonist (Kb = 102 nM).[1] It is selective for P2Y1 over P2Y2, P2Y4, P2Y6, P2Y12, and P2Y13, as well as P2X1-4, receptors at 10 µM.2,3 MRS2179 reduces phospholipase C (PLC) activity induced by the P2Y receptor agonist 2-methylthioadenosine diphosphate with an IC50 value of 331 nM in turkey erythrocyte membranes that endogenously express high levels of the P2Y1 receptor.[1] It inhibits platelet shape change and aggregation induced by ADP in washed isolated human platelets when used at a concentration of 10 µM.[4] MRS2179 (50 mg/kg, i.v.) prolongs the length of tail bleeding time in mice, as well as decreases platelet thrombus formation in a mouse model of iron chloride-induced arterial thrombosis.[4],[5]
Reference:
[1]. Nandanan, E., Camaioni, E., Jang, S.-Y., et al. Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists. J. Med. Chem. 42(9), 1625-1638 (1999).
[2]. von Kügelgen, I. Pharmacological profiles of cloned mammalian P2Y-receptor subtypes. Pharmacol. Ther. 110(3), 415-432 (2006).
[3]. Brown, S.G., King, B.F., Kim, Y.-C., et al. Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors. Drug Dev. Res. 49(4), 253-259 (2000).
[4]. Tovar, C., Higgins, B., Deo, D.D., et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle 9(16), 3364-3375 (2010).
[5]. Lenain, N., Freund, M., Léon, C., et al. Inhibition of localized thrombosis in P2Y1-deficient mice and rodents treated with MRS2179, a P2Y1 receptor antagonist. J. Thromb. Haemost. 1(6), 1144-1149 (2003).
| Cas No. | 228264-19-5 | SDF | |
| Chemical Name | 2′-deoxy-N-methyl-3′-adenylic acid, 5′-(dihydrogen phosphate), ammonium salt, hydrate | ||
| Canonical SMILES | OP(OC[C@@H]1[C@@H](OP(O)(O)=O)C[C@H](N2C=NC3=C2N=CN=C3NC)O1)(O)=O.N | ||
| Formula | C11H17N5O9P2•XNH3[XH2O] | M.Wt | 425.2 |
| Solubility | 42.5mg/ml in water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3518 mL | 11.7592 mL | 23.5183 mL |
| 5 mM | 470.4 μL | 2.3518 mL | 4.7037 mL |
| 10 mM | 235.2 μL | 1.1759 mL | 2.3518 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)