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Etavopivat

Name: Etavopivat
Brand: TargetMol
SKU: T39753
Rating: 4.5 (1 reviews)

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Catalog No. T39753Cas No. 2245053-57-8

Alias FT-4202, FT4202, FT 4202

Etavopivat is a potent, selective, and orally active activator of erythrocyte pyruvate kinase (PKR) that enhances red blood cell glycolytic flux and energy metabolism, exhibiting strong antisickling effects by improving erythrocyte deformability and reducing hemoglobin polymerization. Etavopivat is therefore widely applied in translational and mechanistic studies of sickle cell disease and other inherited haemoglobinopathies.

Etavopivat

😃Good

Catalog No. T39753Alias FT-4202, FT4202, FT 4202Cas No. 2245053-57-8

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$448	Inquiry	Inquiry
10 mg	$788	Inquiry	Inquiry

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

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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Product Introduction

Bioactivity

Description	Etavopivat is a potent, selective, and orally active activator of erythrocyte pyruvate kinase (PKR) that enhances red blood cell glycolytic flux and energy metabolism, exhibiting strong antisickling effects by improving erythrocyte deformability and reducing hemoglobin polymerization. Etavopivat is therefore widely applied in translational and mechanistic studies of sickle cell disease and other inherited haemoglobinopathies.
In vitro	In human red blood cells (RBCs), treatment with Etavopivat (20 μM) for 4 hours resulted in a significant improvement in hemoglobin-oxygen affinity and a reduction in the Point of Sickling (PoS) metric[1].
In vivo	In a mouse model of Sickle Cell Anemia (SCA), oral administration of Etavopivat (500-1000 mg/kg, daily for 2 weeks) demonstrated robust therapeutic efficacy, significantly improving red blood cell survival rates and increasing hemoglobin levels [1]. Additionally, in a pharmacodynamic study involving Cynomolgus monkeys, oral administration of Etavopivat (3-22 mg/kg) for 5 days exhibited dose-dependent activity. Specifically, at doses of 8 mg/kg and 22 mg/kg, it induced a marked increase in intracellular ATP levels and a reduction in 2,3-DPG levels, confirming its mechanism of action in a non-human primate model [2].
Synonyms	FT-4202, FT4202, FT 4202

Chemical Properties

Molecular Weight	457.5
Formula	C₂₂H₂₃N₃O₆S
Cas No.	2245053-57-8
Smiles	S(=O)(=O)(N1CC2=C(C1)CN(C([C@H](CO)C3=CC=CC=C3)=O)C2)C=4C=C5C(=NC4)OCCO5

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 40 mg/mL (87.43 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1858 mL	10.9290 mL	21.8579 mL	109.2896 mL
5 mM	0.4372 mL	2.1858 mL	4.3716 mL	21.8579 mL
10 mM	0.2186 mL	1.0929 mL	2.1858 mL	10.9290 mL
20 mM	0.1093 mL	0.5464 mL	1.0929 mL	5.4645 mL
50 mM	0.0437 mL	0.2186 mL	0.4372 mL	2.1858 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

Keywords

Etavopivat