R 121919 hydrochloride |
| Katalog-Nr.GC50488 |
High affinity CRF1 antagonist; orally bioavailable
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 195055-66-4
Sample solution is provided at 25 µL, 10mM.
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High affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable.
Chen and Grigoriadis (2005) NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev.Res. 65 216 |Jutkiewicz et al (2005) The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 180 215 PMID:15696320 |Gutman et al (2003) The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J.Pharmacol.Exp.Ther. 304 874 PMID:12538845 |Heinrichs et al (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule cortico. releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27 194 PMID:12093593
| Cas No. | 195055-66-4 | SDF | |
| Canonical SMILES | CCCN(C1=CC(C)=NC2=C(C3=CN=C(N(C)C)C=C3C)C(C)=NN12)CCC.Cl | ||
| Formula | C22H32N6.HCl | M.Wt | 416.99 |
| Löslichkeit | Soluble in DMSO | 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. |
||
| 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 | 2.3981 mL | 11.9907 mL | 23.9814 mL |
| 5 mM | 479.6 μL | 2.3981 mL | 4.7963 mL |
| 10 mM | 239.8 μL | 1.1991 mL | 2.3981 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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