MRS 2578

Research use only, not for human use.

MRS2578, an effective P2Y6 receptor antagonist with IC50 of 37 nM, shows insignificant inhibition at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.

MRS-2578 is a selective antagonist of P2Y6 nucleotide receptors (IC50 values are 37 and 98 nM at human and rat P2Y6 receptors respectively). 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.

MRS2578 (1 μM) completely blocks the protection by UDP undergoing TNFα-induced apoptosis in 1321N1 astrocytoma cells. ?MRS 2578 (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. MRS 2578 (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells.

MRS2578 (3 mg/kg; i.p.; for 3 days) significantly suppresses pressure overload-induced collagen deposition without affecting cardiomyocyte hypertrophy after transverse aortic constriction (TAC). Animal Model:6-week-old male C57BL/6J mice Dosage:3 mg/kg Administration:Intraperitoneal injection; daily for 3 days after TAC Result:Significantly suppressed pressure overload-induced collagen deposition.

MRS-2578 | MRS2578 | MRS 2578

Others

Other Targets

P2Y6

Cardiovascular Disease

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711019-86-2

472.67

C20H20N6S4

>98% (HPLC)

DMSO : ≥ 80 mg/mL; 169.25 mM

S=C=NC1=CC=CC(NC(=S)NCCCCNC(=S)NC2=CC(=CC=C2)N=C=S)=C1

1,1'-(butane-1,4-diyl)bis(3-(3-isothiocyanatophenyl)thiourea)

(-20℃)

With Ice Pack

≥ 2 years