A-317491 sodium salt hydrate

Name: A-317491 sodium salt hydrate
Brand: MedChemExpress
SKU: HY-15568A
Rating: 5.0 (5 reviews)

Cat. No.: HY-15568A Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors, with K_is of 22, 22, 9, and 92 nM for hP2X₃, rP2X₃, hP2X_2/3, and rP2X_2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X₃ and P2X_2/3 receptor-mediated calcium flux.

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

A-317491 sodium salt hydrate Chemical Structure

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 163	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 163	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 122	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 182	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 617	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of A-317491 sodium salt hydrate:

A-317491 In-stock

4 Publications Citing Use of MCE A-317491 sodium salt hydrate

: A-317491 sodium salt hydrate purchased from MedChemExpress. Usage Cited in: Int J Nanomedicine. 2017 Nov 9;12:8171-8183. [Abstract]; PC12 cell fluorescence images of baseline (before ATP stimulation), 0 s (the brightest fluorescence images after ATP stimulation), 50 s, 100 s, 150 s, and 200 s. Ca²⁺ peak increase (∆F/F₀) in PC12 cells incubated with A-317491 salt, CSOSA/NLC, and CSOSA/NLC/A-317491 for predetermined time under 100 μM ATP stimulation.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All P2X Receptor Isoform Specific Products:

View All Isoforms

P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

P2X3 Receptor

In Vitro

A-317491 potently blocks recombinant human and rat P2X₃ and P2X_2/3 receptor-mediated calcium flux (K_i=22-92 nM) ^[1].
A-317491 (1 nM-10 μM) produces a concentration-dependent block of dorsal root ganglion (DRG) currents with an IC₅₀ of 15 nM^[1].

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

In Vivo

A-317491 (0.1-30 mg/kg; a single s.c.) dose-dependently reverses inflammatory mechanical hyperalgesia in rats^[2].
A-317491 (3-30 mg/kg; a single .v.) exhibits the plasma half-life (7.38 h), clearance rate (1.83 L/h/kg), and volume of distribution (0.17 L/kg)^[2].

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

Animal Model:	Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant^[2]
Dosage:	0.1, 1, 3, 10, 30 mg/kg
Administration:	A single s.c.
Result:	Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration.

Molecular Weight

606.57

Formula

C₃₃H₂₉NNaO₉

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O.[Na].O

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:

H₂O : 100 mg/mL (164.86 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6486 mL	8.2431 mL	16.4861 mL
5 mM	0.3297 mL	1.6486 mL	3.2972 mL
10 mM	0.1649 mL	0.8243 mL	1.6486 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (82.43 mM); Clear solution; Need ultrasonic

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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (256 KB) LCMS (262 KB)

Handling Instructions (2659 KB)

References

[1]. Jarvis MF, et, al. A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84. [Content Brief]

[2]. Wu G, et, al. A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats. Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O	1 mM	1.6486 mL	8.2431 mL	16.4861 mL	41.2154 mL
	5 mM	0.3297 mL	1.6486 mL	3.2972 mL	8.2431 mL
	10 mM	0.1649 mL	0.8243 mL	1.6486 mL	4.1215 mL
	15 mM	0.1099 mL	0.5495 mL	1.0991 mL	2.7477 mL
	20 mM	0.0824 mL	0.4122 mL	0.8243 mL	2.0608 mL
	25 mM	0.0659 mL	0.3297 mL	0.6594 mL	1.6486 mL
	30 mM	0.0550 mL	0.2748 mL	0.5495 mL	1.3738 mL
	40 mM	0.0412 mL	0.2061 mL	0.4122 mL	1.0304 mL
	50 mM	0.0330 mL	0.1649 mL	0.3297 mL	0.8243 mL
	60 mM	0.0275 mL	0.1374 mL	0.2748 mL	0.6869 mL
	80 mM	0.0206 mL	0.1030 mL	0.2061 mL	0.5152 mL
	100 mM	0.0165 mL	0.0824 mL	0.1649 mL	0.4122 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.