MRS 2578

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MRS2578 是一种有效的 P2Y6 受体拮抗剂，IC50 为 37 nM，对 P2Y1、P2Y2、P2Y4 和 P2Y11 受体显示出微弱的抑制作用。

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

——

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