1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. HIF-2α agonist 2

HIF-2α agonist 2 (compound 10) is a HIF-2α agonist with an EC50 value of 1.68 μM at the dose of 20 μM. HIF-2α agonist 2 is non-cytotoxic against 786-O-HRE-Luc cells. HIF-2α agonist 2 can be used for oxygen metabolism research.

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HIF-2α agonist 2 Chemical Structure

HIF-2α agonist 2 Chemical Structure

CAS No. : 2750141-15-0

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Description

HIF-2α agonist 2 (compound 10) is a HIF-2α agonist with an EC50 value of 1.68 μM at the dose of 20 μM. HIF-2α agonist 2 is non-cytotoxic against 786-O-HRE-Luc cells. HIF-2α agonist 2 can be used for oxygen metabolism research[1].

In Vitro

HIF-2α agonist 2 (0.001-100 μM; 24 h) dose-dependently activates HIF-2 with an EC50 value of 1.68 μM at the dose of 20 μM[1].
HIF-2α agonist 2 (0.003-20 μM; 24 h) shows no cytotoxicity against 786-O-HRE-Luc cells[1].

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

Cell Viability Assay[1]

Cell Line: 786-O-HRE-Luc cell line
Concentration: 0.003-20 μM
Incubation Time: 24 hours
Result: Showed no cytotoxicity to 786-O-Luc cells.
Molecular Weight

416.09

Formula

C13H8Br2N2O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S1(N=C(C2=C1C=CC=C2)NC3=CC(Br)=CC(Br)=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.33 mM; ultrasonic and warming and heat to 60°C; 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 2.4033 mL 12.0166 mL 24.0333 mL
5 mM 0.4807 mL 2.4033 mL 4.8067 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

  • Dilution Calculator

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

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 2.4033 mL 12.0166 mL 24.0333 mL 60.0832 mL
5 mM 0.4807 mL 2.4033 mL 4.8067 mL 12.0166 mL
10 mM 0.2403 mL 1.2017 mL 2.4033 mL 6.0083 mL
15 mM 0.1602 mL 0.8011 mL 1.6022 mL 4.0055 mL
20 mM 0.1202 mL 0.6008 mL 1.2017 mL 3.0042 mL
25 mM 0.0961 mL 0.4807 mL 0.9613 mL 2.4033 mL
30 mM 0.0801 mL 0.4006 mL 0.8011 mL 2.0028 mL
40 mM 0.0601 mL 0.3004 mL 0.6008 mL 1.5021 mL
50 mM 0.0481 mL 0.2403 mL 0.4807 mL 1.2017 mL
60 mM 0.0401 mL 0.2003 mL 0.4006 mL 1.0014 mL
80 mM 0.0300 mL 0.1502 mL 0.3004 mL 0.7510 mL
100 mM 0.0240 mL 0.1202 mL 0.2403 mL 0.6008 mL
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  • 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.

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HIF-2α agonist 2
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