hGPR91 antagonist 3
Based on 1 Customer Validation
hGPR91 antagonist 3 (Compound 5g) is a potent and orally active GPR91 antagonist with IC50s of 35 nM and 135 nM, for human GPR91 and rat GPR91, respectively.
For research use only. We do not sell to patients.
- Purity: 99.01%
- CAS No.: 1314796-31-0
- Formula: C23H18F4N4O2
- Molecular Weight:458.41
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 35 nM (human GPR91) and 135 nM (rat GPR91)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
>30 μM
Compound: 5g
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Antagonist activity at human GPR99 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level at by FLIPR assay
Antagonist activity at human GPR99 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level at by FLIPR assay
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[PMID: 21571530] |
| CHO-K1 | IC50 |
135 nM
Compound: 5g
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Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
|
[PMID: 21571530] |
| CHO-K1 | IC50 |
35 nM
Compound: 5g
|
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
|
[PMID: 21571530] |
Chemical Information
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CAS No. 1314796-31-0
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Appearance Solid
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Molecular Weight 458.41
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Formula C23H18F4N4O2
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Color Off-white to light yellow
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SMILES
O=C(CCCC1=CC=C2C=CC=NC2=N1)NCC3=CC(C4=CC(C(F)(F)F)=C(F)C=C4)=NO3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (218.15 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (269 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
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 (stored under nitrogen). 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 | 2.1815 mL | 10.9073 mL | 21.8145 mL | 54.5363 mL |
| 5 mM | 0.4363 mL | 2.1815 mL | 4.3629 mL | 10.9073 mL | |
| 10 mM | 0.2181 mL | 1.0907 mL | 2.1815 mL | 5.4536 mL | |
| 15 mM | 0.1454 mL | 0.7272 mL | 1.4543 mL | 3.6358 mL | |
| 20 mM | 0.1091 mL | 0.5454 mL | 1.0907 mL | 2.7268 mL | |
| 25 mM | 0.0873 mL | 0.4363 mL | 0.8726 mL | 2.1815 mL | |
| 30 mM | 0.0727 mL | 0.3636 mL | 0.7272 mL | 1.8179 mL | |
| 40 mM | 0.0545 mL | 0.2727 mL | 0.5454 mL | 1.3634 mL | |
| 50 mM | 0.0436 mL | 0.2181 mL | 0.4363 mL | 1.0907 mL | |
| 60 mM | 0.0364 mL | 0.1818 mL | 0.3636 mL | 0.9089 mL | |
| 80 mM | 0.0273 mL | 0.1363 mL | 0.2727 mL | 0.6817 mL | |
| 100 mM | 0.0218 mL | 0.1091 mL | 0.2181 mL | 0.5454 mL |
hGPR91 antagonist 3 Related Classifications
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