2. Metabolic Enzyme/Protease
  3. Pyruvate Kinase
  4. Tebapivat

Tebapivat  (Synonyms: AG-946; PKR activator 2)

Cat. No.: HY-135884 Purity: 99.12%
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Tebapivat (PKR activator 2) is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385.

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

Tebapivat Chemical Structure

Tebapivat Chemical Structure

CAS No. : 2283422-04-6

Size Price Stock Quantity
1 mg USD 900 In-stock
5 mg USD 2000 In-stock
10 mg USD 3400 In-stock
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Based on 1 publication(s) in Google Scholar

Tebapivat Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

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Description

Tebapivat (PKR activator 2) is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385[1].

IC50 & Target

Pyruvate kinase-R (PKR)[1]
In Vitro

Tebapivat (compound 385) activates wild type PKR, PKR K410E or PKR 510Q with AC50 values <0.3 μΜ[1].
Pyruvate kinase deficiency (PKD) is a disease of red blood cells caused by a deficiency of pyruvate kinase R (PKR) enzyme as a result of autosomal recessive mutations of the PKLR gene. PKR activators can be beneficial to treat disorders and conditions such as but not limited to PKD, thalassemia, hereditary elliptocytosis, anemia (e.g. , congenital anemias (e.g., enzymopathies), hemolytic anemia (e.g. hereditary and/or congenital hemolytic anemia, acquired hemolytic anemia, chronic hemolytic anemia caused by phosphoglycerate kinase deficiency, anemia of chronic diseases, non-spherocytic hemolytic anemia or hereditary spherocytosis)[1].

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

Tebapivat Related Antibodies
Molecular Weight

392.44

Formula

C18H16N8OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(N(C)C2=C3SC(CC4=NNC=C4)=N2)=C3C=NN1CC5=NC(N)=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (127.41 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 2.5482 mL 12.7408 mL 25.4816 mL
5 mM 0.5096 mL 2.5482 mL 5.0963 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 5 mg/mL (12.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
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
References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5482 mL 12.7408 mL 25.4816 mL 63.7040 mL
5 mM 0.5096 mL 2.5482 mL 5.0963 mL 12.7408 mL
10 mM 0.2548 mL 1.2741 mL 2.5482 mL 6.3704 mL
15 mM 0.1699 mL 0.8494 mL 1.6988 mL 4.2469 mL
20 mM 0.1274 mL 0.6370 mL 1.2741 mL 3.1852 mL
25 mM 0.1019 mL 0.5096 mL 1.0193 mL 2.5482 mL
30 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1235 mL
40 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5926 mL
50 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2741 mL
60 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0617 mL
80 mM 0.0319 mL 0.1593 mL 0.3185 mL 0.7963 mL
100 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
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Tebapivat Related Classifications

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:

Tebapivat2283422-04-6AG-946 PKR activator 2AG946AG 946PKR activator2PKR activator 2PKR activator-2Pyruvate KinasePKRdeficiencyhemolyticanemiaPKLRautosomalInhibitorinhibitorinhibit

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