1. GPCR/G Protein
    Apoptosis
  2. P2Y Receptor
    Apoptosis
  3. MRS 2578

MRS 2578 

Cat. No.: HY-13104 Purity: 95.67%
Handling Instructions

MRS 2578 is a selective and potent P2Y6 receptor antagonist with IC50s of 37 nM (human) and 98 nM (rat). MRS 2578 exhibits insignificant activity at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.

For research use only. We do not sell to patients.

MRS 2578 Chemical Structure

MRS 2578 Chemical Structure

CAS No. : 711019-86-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 210 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

MRS 2578 is a selective and potent P2Y6 receptor antagonist with IC50s of 37 nM (human) and 98 nM (rat). MRS 2578 exhibits insignificant activity at P2Y1, P2Y2, P2Y4, and P2Y11 receptors[1][2].

IC50 & Target

IC50: 37 nM (human P2Y6 receptor), 98 nM (rat P2Y6 receptor)[2]

In Vitro

MRS2578 (1 μM) completely blocks the protection by UDP undergoing TNFα-induced apoptosis in 1321N1 astrocytoma cells[1].
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[2].

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)[4].

Animal Model: 6-week-old male C57BL/6J mice[4]
Dosage: 3 mg/kg
Administration: Intraperitoneal injection; daily for 3 days after TAC
Result: Significantly suppressed pressure overload-induced collagen deposition.
Molecular Weight

472.67

Formula

C₂₀H₂₀N₆S₄

CAS No.

711019-86-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 80 mg/mL (169.25 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.29 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.29 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MRS 2578MRS2578MRS-2578P2Y ReceptorApoptosisInhibitorinhibitorinhibit

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Product name:
MRS 2578
Cat. No.:
HY-13104
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