R121919 (NBI30775) |
| Catalog No.GC30792 |
R121919(NBI30775)(NBI30775)는 CRF1 수용체에 대해 2~5nM의 Ki를 갖고 CRF2 수용체, CRF-결합 단백질 또는 70가지 다른 수용체 유형에서 1000배 이상 더 약한 활성을 갖는 강력한 소분자 CRF1 수용체 길항제입니다. .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 195055-03-9
Sample solution is provided at 25 µL, 10mM.
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R121919 is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
R121919 is a potent small-molecule CRF1 receptor antagonistwith high affinity for the CRF1 receptor (Ki=2-5 nM) and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types[1].
R121919 reduces measures of both anxiety and depression in the depressed patients. R121919 dose dependently decreases adrenocorticopin hormone and corticosterone responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively[1]. R121919 reduces levels of anxiety in mice with a steep dose-response curve. Molecules such as GR, MR, BAG-1 and AP-1 have been identified as some of the drug's intracellular targets[2].
[1]. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80. [2]. Post A, et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8.
Animal experiment: | Rats: For the restraint stress,R121919 is dissolved in an aqueous 70% (v/v) polyethylene glycol 400 solution, and serially diluted in this vehicle to the appropriate concentrations. The drug is injected i.v. in a volume of 1 mL/kg to Male Sprague-Dawley rats. For the defensive withdrawal experiments, R121919 solutions are made fresh the night before each experiment. R121919 is dissolved in a vehicle consisting of 5% (v/v) polyethoxylated castor oil[1]. Mice: R121919 is dissolved in an aqueous. The drug is administered orally (1 mL/100 g bodyweight) via a feeding tube to six to ten mice per group; the doses applied are 0.5, 1.0 and 5.0 mg/kg for the DBA/2NCRL mice and 1.0, 5.0, and 30 mg/kg for the DBA/2Ola strain; an additional (vehicle) group of mice receives water, while a further group of mice (untreated controls) are spared the aforementioned manipulations[2]. |
References: [1]. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80. | |
| Cas No. | 195055-03-9 | SDF | |
| Canonical SMILES | CCCN(C1=CC(C)=NC2=C(C3=CN=C(N(C)C)C=C3C)C(C)=NN21)CCC | ||
| Formula | C22H32N6 | M.Wt | 380.53 |
| Solubility | DMSO : 6.2 mg/mL (16.29 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6279 mL | 13.1396 mL | 26.2791 mL |
| 5 mM | 0.5256 mL | 2.6279 mL | 5.2558 mL |
| 10 mM | 0.2628 mL | 1.314 mL | 2.6279 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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