TC-S 7009 |
| Catalog No.GC50128 |
High affinity and selective HIF-2α inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1422955-31-4
Sample solution is provided at 25 µL, 10mM.
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High affinity and selective HIF-2α inhibitor (Kd = 81 nM). Binds to the HIF-2α PAS-B domain; disrupts HIF-2α-ARNT heterodimerization. Exhibits >60-fold selectivity for HIF-2α over HIF-1α. Decreases HIF-2α DNA-binding and attenuates expression of HIF-2α target genes in vitro.
Scheuermann et al (2013) Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat.Chem.Biol. 9 271 PMID:23434853 |Rogers et al (2013) Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor. J.Med.Chem. 56 1739 PMID:23363003 |Wu et al (2019) Bidirectional modulation of HIF-2 activity through chemical ligands. Nat.Chem.Biol. 15 367 PMID:30804532
| Cas No. | 1422955-31-4 | SDF | |
| Canonical SMILES | ClC1=CC(F)=CC(NC3=C([N+]([O-])=O)C2=NON=C2C=C3)=C1 | ||
| Formula | C12H6ClFN4O3 | M.Wt | 308.65 |
| Solubility | DMSO: 30 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2399 mL | 16.1996 mL | 32.3992 mL |
| 5 mM | 0.648 mL | 3.2399 mL | 6.4798 mL |
| 10 mM | 0.324 mL | 1.62 mL | 3.2399 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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