MRS 2578

Name: MRS 2578
Brand: MedChemExpress
SKU: HY-13104
Rating: 5.0 (6 reviews)

Cat. No.: HY-13104 Purity: 98.15%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 711019-86-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 50	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 50	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 48	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 231	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE MRS 2578

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Biological Activity
Purity & Documentation
References
Customer Review

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

P2Y6 Receptor

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Appearance

Solid

Color

White to off-white

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (105.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.15%

Select Batch:

Data Sheet (272 KB) SDS (584 KB)

COA (242 KB) HNMR (286 KB) LCMS (300 KB)

Handling Instructions (2659 KB)

References

[1]. Mamedova LK, et al. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem Pharmacol, 2004, 67(9), 1763-1770. [Content Brief]

[2]. Nishida M, et al. P2Y6 receptor-Galpha12/13 signalling in cardiomyocytes triggers pressure overload-induced cardiacfibrosis. EMBO J. 2008 Dec 3;27(23):3104-15. [Content Brief]

[3]. Riegel AK, et al. Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation. Blood, 2011, 117(8), 2548-2555. [Content Brief]

[4]. Vieira RP, et al. Purinergic receptor type 6 contributes to airway inflammation and remodeling in experimental allergic airway inflammation. Am J Respir Crit Care Med, 2011, 184(2), 215-223. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1156 mL	10.5782 mL	21.1564 mL	52.8910 mL
	5 mM	0.4231 mL	2.1156 mL	4.2313 mL	10.5782 mL
	10 mM	0.2116 mL	1.0578 mL	2.1156 mL	5.2891 mL
	15 mM	0.1410 mL	0.7052 mL	1.4104 mL	3.5261 mL
	20 mM	0.1058 mL	0.5289 mL	1.0578 mL	2.6446 mL
	25 mM	0.0846 mL	0.4231 mL	0.8463 mL	2.1156 mL
	30 mM	0.0705 mL	0.3526 mL	0.7052 mL	1.7630 mL
	40 mM	0.0529 mL	0.2645 mL	0.5289 mL	1.3223 mL
	50 mM	0.0423 mL	0.2116 mL	0.4231 mL	1.0578 mL
	60 mM	0.0353 mL	0.1763 mL	0.3526 mL	0.8815 mL
	80 mM	0.0264 mL	0.1322 mL	0.2645 mL	0.6611 mL
	100 mM	0.0212 mL	0.1058 mL	0.2116 mL	0.5289 mL

MRS 2578 Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MRS 2578711019-86-2MRS2578MRS-2578P2Y ReceptorApoptosisInhibitorinhibitorinhibit

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MRS 2578

Customer Review

MRS 2578 Related Antibodies

6 Publications Citing Use of MCE MRS 2578

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All P2Y Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

MRS 2578 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

MRS 2578 Related Classifications

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