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(E/Z)-Sivopixant

Name: (E/Z)-Sivopixant
Brand: TargetMol
SKU: T9653
Price: 88 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9653Cas No. 1640808-39-4

Alias (E/Z)-S-600918

(E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM, suitable for respiratory diseases research.

(E/Z)-Sivopixant

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Purity: 99.82%

Catalog No. T9653Alias (E/Z)-S-600918Cas No. 1640808-39-4

(E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM, suitable for respiratory diseases research.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$88	In Stock	In Stock
5 mg	$223	In Stock	In Stock
10 mg	$333	In Stock	In Stock
25 mg	$537	In Stock	In Stock
50 mg	$732	In Stock	In Stock
100 mg	$990	In Stock	In Stock
500 mg	$1,970	-	In Stock
1 mL x 10 mM (in DMSO)	$249	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.82%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

(E/Z)-Sivopixant AI Summary

(E/Z)-Sivopixant exhibits significant bioactivity as a potent antagonist at the P2X3 receptor, with an IC50 of 4.2 nM in human P2X3R and an IC50 of 4.0 nM at the rat P2X3 receptor. It shows functional selectivity for the P2X3 receptor over the P2X2 receptor with a selectivity ratio of 1100.0. In a rat model of neuropathic pain, it provides analgesic effects, evidenced by an ED50 of 0.4 mg/kg and 64.0% efficacy at 3 mg/kg orally (po). The compound demonstrates good oral bioavailability in rats, with F values of 52.8% and 76.8% at 1 mg/kg and 3 mg/kg dosages, respectively. Additionally, it has good solubility in JP2 fluid at pH 6.8 at 458.0 µg/mL and exhibits low protein binding in rat plasma (Fu = 0.01). Pharmacokinetically, it has a half-life of 10.1 hours and a clearance rate of 2.7 mL/min/kg in rats following intravenous (iv) administration at 1 mg/kg. (E/Z)-Sivopixant inhibits CYP enzymes with IC50 values above 20,000 nM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Furthermore, it shows low activity as an antagonist at the P2X1, P2X2, P2X4, and P2X7 receptors with IC50 values above 30,000 nM. In cell viability assays, the compound's effects vary; it promotes growth in HEK293T cells with growth rates from 0.2 to 0.97, but shows mixed results with human fibroblast and U2OS cell viability, ranging from inhibitory to stimulatory effects. Overall, (E/Z)-Sivopixant is a promising candidate for targeting P2X3 receptors with both analgesic and selective properties, favorable pharmacokinetics, and mixed effects on various cell lines' viability..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	(E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM, suitable for respiratory diseases research.
Synonyms	(E/Z)-S-600918

Chemical Properties

Molecular Weight	507.93
Formula	C₂₅H₂₂ClN₅O₅
Cas No.	1640808-39-4
Smiles	C[C@@H](Cn1c(=O)nc(Nc2ccc(Oc3ccccn3)cc2)n(Cc2ccc(Cl)cc2)c1=O)C(O)=O

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 90 mg/mL (177.19 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.5 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9688 mL	9.8439 mL	19.6878 mL	98.4388 mL
5 mM	0.3938 mL	1.9688 mL	3.9376 mL	19.6878 mL
10 mM	0.1969 mL	0.9844 mL	1.9688 mL	9.8439 mL
20 mM	0.0984 mL	0.4922 mL	0.9844 mL	4.9219 mL
50 mM	0.0394 mL	0.1969 mL	0.3938 mL	1.9688 mL
100 mM	0.0197 mL	0.0984 mL	0.1969 mL	0.9844 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc