MRS 2578

SKU: orb1221853

Description

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.

Key Properties

• CAS Number: 711019-86-2
• MW: 472.67
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₀N₆S₄
• SMILES: S=C=NC1=CC=CC(NC(=S)NCCCCNC(=S)NC2=CC(=CC=C2)N=C=S)=C1
• Target: P2Y6
• Solubility: DMSO : ≥ 80 mg/mL; 169.25 mM

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MRS-2578 | MRS2578 | MRS 2578

Quick Database Links

Gene Symbol

P2Y6