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R121919
🥰Excellent
Catalog No. T16713Cas No. 195055-03-9
Alias NBI30775
R121919 (NBI30775) is a potent small molecule antagonist of the adrenocorticotropic hormone-releasing factor receptor 1 (CRF1), demonstrating antidepressant and anxiolytic activity, and inhibiting the CRF1 receptor, CRF2 receptor, and CRF-binding proteins.
R121919
🥰Excellent
Purity: 99.75%
Catalog No. T16713Alias NBI30775Cas No. 195055-03-9
R121919 (NBI30775) is a potent small molecule antagonist of the adrenocorticotropic hormone-releasing factor receptor 1 (CRF1), demonstrating antidepressant and anxiolytic activity, and inhibiting the CRF1 receptor, CRF2 receptor, and CRF-binding proteins.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $89 | In Stock | |
| 10 mg | $143 | In Stock | |
| 25 mg | $297 | In Stock | |
| 50 mg | $488 | In Stock | |
| 100 mg | $783 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $98 | In Stock |
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Purity:99.75%
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Product Introduction
Bioactivity
Chemical Properties
| Description | R121919 (NBI30775) is a potent small molecule antagonist of the adrenocorticotropic hormone-releasing factor receptor 1 (CRF1), demonstrating antidepressant and anxiolytic activity, and inhibiting the CRF1 receptor, CRF2 receptor, and CRF-binding proteins. |
| Targets&IC50 | CRF1 receptor:2-5 nM (Ki) |
| In vitro | R121919 is a potent small-molecule CRF1 receptor antagonist, exhibiting high affinity for the CRF1 receptor with a Ki value in the range of 2–5 nM. Notably, its activity at the CRF2 receptor, CRF-binding protein, and 70 other receptor types is over 1000-fold weaker[2]. |
| In vivo | In rats, R121919 demonstrates a dose-dependent reduction in adrenocorticotropic hormone and corticosterone responses to restraint stress. At a dose of 10 mg/kg R121919, peak plasma concentrations of adrenocorticotropic hormone and corticosterone are decreased by 9% and 25%, respectively[2]. Moreover, R121919 exhibits anxiolytic effects in mice with a steep dose-response curve, leading to reduced anxiety levels. Some of the intracellular targets of the drug include molecules like GR (glucocorticoid receptor), MR (mineralocorticoid receptor), BAG-1 (Bcl-2-associated athanogene-1), and AP-1 (activator protein 1)[1]. |
| Synonyms | NBI30775 |
| Molecular Weight | 380.53 |
| Formula | C22H32N6 |
| Cas No. | 195055-03-9 |
| Smiles | CCCN(CCC)c1cc(C)nc2c(c(C)nn12)-c1cnc(cc1C)N(C)C |
| Relative Density. | 1.31g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (13.14 mM), Sonication is recommended. Ethanol: 80 mg/mL (210.23 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.63 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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