RG7713 (RO5028442) (Synonyms: RO5028442) |
| Katalog-Nr.GC30890 |
RG7713 (RO5028442) (RO5028442) ist ein hochwirksamer und selektiver Brain-Penetrant Vasopressin 1a (V1a)-Rezeptorantagonist mit einem Kis von 1 nM (hV1a) und 39 nM (mV1a).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 920022-47-5
Sample solution is provided at 25 µL, 10mM.
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RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
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].
[1]. Ratni H, et al. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. J Med Chem. 2015 Mar 12;58(5):2275-89.
Cell experiment: | 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 fluorometricimaging plate reader, compound dilution series added to the cells, and agonist activity measured[1]. |
References: [1]. Ratni H, et al. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. J Med Chem. 2015 Mar 12;58(5):2275-89. | |
| Cas No. | 920022-47-5 | SDF | |
| Überlieferungen | RO5028442 | ||
| Canonical SMILES | O=C(C1=CN(CCN(C)C)C2=C1C=CC(Cl)=C2)N3CCC4(C(C=CC=C5)=C5CO4)CC3 | ||
| Formula | C25H28ClN3O2 | M.Wt | 437.96 |
| Löslichkeit | DMSO : 20 mg/mL (45.67 mM) | 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 | 2.2833 mL | 11.4166 mL | 22.8331 mL |
| 5 mM | 456.7 μL | 2.2833 mL | 4.5666 mL |
| 10 mM | 228.3 μL | 1.1417 mL | 2.2833 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 25 reference(s) in Google Scholar.)
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