RG7713
Based on 2 publication(s) in Google Scholar
RG7713 (RO5028442) is a highly potent, selective and brain-penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
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- Pureté: 99.92%
- CAS No.: 920022-47-5
- Formule: C25H28ClN3O2
- Masse moléculaire:437.96
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) RG7713
MoreVoir tous les produits spécifiques à Isoform Vasopressin Receptor
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Activité biologique
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V1a Receptor |
RG7713 (RO5028442) (compound 8) has excellent binding in and functional affinity for hV1a, moderate mouse affinity, and excellent selectivity versus human V2 (hV2) and human oxytocin (hOT) receptors. RG7713 (RO5028442) shows high solubility. RG7713 (RO5028442) is found to be highly selective against a panel of 89 targets. Finally, RG7713 (RO5028442) is identified as a suitable compound for clinical studies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 920022-47-5
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Appearance Solid
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Masse moléculaire 437.96
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Formule C25H28ClN3O2
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Color White to off-white
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SMILES
O=C(C1=CN(CCN(C)C)C2=C1C=CC(Cl)=C2)N3CCC4(C(C=CC=C5)=C5CO4)CC3
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Synonyms
RO5028442
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Mol Med (Berl)
Vasopressin-stimulated ORAI1 expression and store-operated Ca2+ entry in aortic smooth muscle cells. [Abstract]2021 Mar;99(3):373-382. PMID: 33409552 -
Solvant et solubilité
DMSO : 20 mg/mL (45.67 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (4.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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.
Protocole
CHO cells are stably transfected with expression plasmids encoding human V1a and grown in F-12 K, containing 10% fetal bovine serum, 1% penicillin-streptomycin, 1% glutamate, and 200 μg/mL geneticin at 37 °C in a 10% CO2 incubator at 95% humidity. Cells are plated for 24 h at 50,000 cells/well in clear bottomed 96 well plates and are dye loaded for 60 min with 2 μM Fluo-4-AM in assay buffer. After cell washing, the plate is loaded on a fluorometric imaging plate reader, compound dilution series added to the cells, and agonist activity measured[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2833 mL | 11.4166 mL | 22.8331 mL | 57.0828 mL |
| 5 mM | 0.4567 mL | 2.2833 mL | 4.5666 mL | 11.4166 mL | |
| 10 mM | 0.2283 mL | 1.1417 mL | 2.2833 mL | 5.7083 mL | |
| 15 mM | 0.1522 mL | 0.7611 mL | 1.5222 mL | 3.8055 mL | |
| 20 mM | 0.1142 mL | 0.5708 mL | 1.1417 mL | 2.8541 mL | |
| 25 mM | 0.0913 mL | 0.4567 mL | 0.9133 mL | 2.2833 mL | |
| 30 mM | 0.0761 mL | 0.3806 mL | 0.7611 mL | 1.9028 mL | |
| 40 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.4271 mL |
RG7713 Related Classifications
HY-12981 Related Classifications
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