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hGPR91 antagonist 1
🥰Excellent
Catalog No. T11560Cas No. 1314796-00-3
hGPR91 antagonist 1 is a potent and selective hGPR91 antagonist (IC50: 7 μM).
hGPR91 antagonist 1
🥰Excellent
Purity: 98.89%
Catalog No. T11560Cas No. 1314796-00-3
hGPR91 antagonist 1 is a potent and selective hGPR91 antagonist (IC50: 7 μM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $87 | In Stock | |
| 5 mg | $213 | In Stock | |
| 10 mg | $313 | In Stock | |
| 25 mg | $533 | In Stock | |
| 50 mg | $728 | In Stock | |
| 100 mg | $987 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $235 | In Stock |
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Purity:98.89%
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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.Product Introduction
Bioactivity
Chemical Properties
| Description | hGPR91 antagonist 1 is a potent and selective hGPR91 antagonist (IC50: 7 μM). |
| Targets&IC50 | GPR91 (human):7 μM |
| In vivo | GPR91, a 7TM G-Protein-Coupled Receptor, has been recently deorphanized with succinic acid as its endogenous ligand.Current literature indicates that GPR91 plays role in various pathophysiology including renal hypertension, autoimmune disease and retinal angiogenesis.Starting from a small molecule high-throughput screening hit 1 (hGPR91 IC(50): 0.8 μM)-originally synthesized in Merck for Bradykinin B(1) Receptor (BK(1)R) program, systematic structure-activity relationship study led us to discover potent and selective hGPR91 antagonists e.g. 2c, 4c, and 5 g (IC(50): 7-35 nM;>1000 fold selective against hGPR99, a closest related GPCR;>100 fold selective in Drug Matrix screening).Led to identification of two structurally distinct and orally bio-available lead compounds: 5g (%F: 26) and 7e (IC(50): 180 nM;>100 fold selective against hGPR99;%F: 87). |
| Molecular Weight | 529.53 |
| Formula | C31H23F4N3O |
| Cas No. | 1314796-00-3 |
| Smiles | C(C(N[C@@H](C)C1=CC=C(C=C1)C2=CC(C(F)(F)F)=C(F)C=C2)=O)C3=CC=C(C4=NC5=C(C=C4)C=CC=N5)C=C3 |
| Relative Density. | 1.286 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 25 mg/mL (47.21 mM)  | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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