Name: MRS 2578
Brand: Selleck Chemicals
SKU: S2855
Availability: InStock
Rating: 5 (2 reviews)

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Batch: S285501 DMSO]42 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.02%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.02

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other P2 Receptor Products	A-438079 Hydrochloride A-804598 A-740003 5-BDBD JNJ-47965567 BX430 Eliapixant Aurintricarboxylic acid A-317491 AZ10606120 dihydrochloride

Solubility

In vitro
Batch:

DMSO : 42 mg/mL (88.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (63.47mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	472.67	Formula	C₂₀H₂₀N₆S₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	711019-86-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=CC(=C1)N=C=S)NC(=S)NCCCCNC(=S)NC2=CC(=CC=C2)N=C=S

Mechanism of Action

Targets/IC₅₀/Ki	P2Y6 37 nM
In vitro	MRS2578 selectively blocks P2Y6 receptor activity versus activity at P2Y1, P2Y2, P2Y4 or P2Y11 receptors. This compound (1 μM) completely blocks the protection by UDP undergoing TNFalpha-induced apoptosis in 1321N1 astrocytoma cells. It inhibits basal NF-κB activity in time and dose dependent manner in HMEC-1 cells transfected with 0.25 μg NF-κB promoter reporter. This chemical (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. It (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. The compound potentiates ATPγS and UDP response at concentrations below 316 nM whereas above this concentration, it inhibits ATPS- and UDP-induced IP accumulation in neonatal rat cardiac myofibroblasts. MRS2578-treated mice shows reduced bronchial hyperresponsiveness toward methacholine in OVA-sensitized mice. This compound completely blocks UDP-induced the release of IL-6, KC, and IL-8 in lung epithelial cells.
In vivo	MRS 2578 (10 μM) attenuates Keratinocyte-derived chemokine serum protein levels in LPS-induced vascular inflammation in C57BL/6 mice. This compound (10 μM, intratracheally) reduces BALF eosinophilia and the levels of IL-5 and IL-13 in the BALF in OVA-sensitized mice and leads to a markedly attenuated change in methacholine responsiveness after OVA challenge. This compound (10 μM, intratracheally) inhibits house dust mite–induced allergic airway inflammation in OVA-sensitized mice. This compound (10 μM, intratracheally) reduces of IL-6 and KC levels in BALF in OVA-sensitized mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15081875/ [2] https://pubmed.ncbi.nlm.nih.gov/21173118/ [3] https://pubmed.ncbi.nlm.nih.gov/19422377/ [4] https://pubmed.ncbi.nlm.nih.gov/21512170/

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MRS 2578 P2 Receptor inhibitor

Chemical Structure

Molecular Weight: 472.67