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| 25mg |
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Purity: ≥98%
MRS2578 (MRS-2578; MRS 2578) is a potent and selective P2Y6 receptor antagonist with potentially usefulness in controlling persistent storage symptoms in obstructed patients. It inhibits P2Y6 receptor with an IC50 of 37 nM and exhibits little activity against closely related P2Y1, P2Y2, P2Y4, and P2Y11 receptors. Activation of P2Y6 receptor amplifies mucosal adenosine triphosphate release underlying bladder overactivity in patients with benign prostatic hyperplasia. Therefore, selective P2Y6 receptor blockade as a novel therapeutic strategy is potentially useful to control persistent storage symptoms in obstructed patients.
| ln Vitro |
MRS2578 (1 μM) totally prevents 1321N1 astrocytoma cells from being protected by UDP during TNFα-induced apoptosis[1]. In HMEC-1 cells, MRS 2578 (10 μM) totally eliminates TNF-α-induced NF-κB reporter activity. In HMEC-1 cells, MRS 2578 (10 μM) dramatically lowers TNF-α-induced proinflammatory gene expression[2].
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| ln Vivo |
After transverse aortic constriction (TAC), MRS2578 (3 mg/kg; ip; for 3 days) dramatically reduces pressure overload-induced collagen deposition without influencing cardiomyocyte hypertrophy[4].
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| Animal Protocol |
Animal/Disease Models: 6weeks old male C57BL/6J mice[4]
Doses: 3 mg/kg Route of Administration: intraperitoneal (ip)injection; daily for 3 days after TAC Experimental Results: Dramatically suppressed pressure overload-induced collagen deposition. |
| References |
[1]. Mamedova LK, et al. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem Pharmacol, 2004, 67(9), 1763-1770.
[2]. Nishida M, et al. P2Y6 receptor-Galpha12/13 signalling in cardiomyocytes triggers pressure overload-induced cardiacfibrosis. EMBO J. 2008 Dec 3;27(23):3104-15. [3]. Riegel AK, et al. Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation. Blood, 2011, 117(8), 2548-2555. [4]. Vieira RP, et al. Purinergic receptor type 6 contributes to airway inflammation and remodeling in experimental allergic airway inflammation. Am J Respir Crit Care Med, 2011, 184(2), 215-223. |
| Molecular Formula |
C20H20N6S4
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| Molecular Weight |
472.67
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| CAS # |
711019-86-2
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| Related CAS # |
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| SMILES |
S=C(N([H])C1C([H])=C([H])C([H])=C(C=1[H])N=C=S)N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(N([H])C1C([H])=C([H])C([H])=C(C=1[H])N=C=S)=S
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.29 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1156 mL | 10.5782 mL | 21.1564 mL | |
| 5 mM | 0.4231 mL | 2.1156 mL | 4.2313 mL | |
| 10 mM | 0.2116 mL | 1.0578 mL | 2.1156 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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