| Size | Price | Stock | Qty |
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| Targets |
NBI-30775 targets the corticotropin-releasing factor 1 receptor (CRF1R), a G protein-coupled receptor that mediates the effects of corticotropin-releasing factor (CRF), a key regulator of the hypothalamic-pituitary-adrenal (HPA) axis and stress responses. The compound is a highly selective antagonist with a Ki of 2 to 5 nM.
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| ln Vitro |
Strong CRF1 receptor antagonist R121919 is a tiny chemical that exhibits high affinity for CRF1 receptors (Ki=2–5 nM) and 1000-fold lower activity when it comes to CRF2 receptors, CRF binding proteins, or the 70 other receptor types listed above [1].
NBI-30775 is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM for the CRF1 receptor. It exhibits over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types. The compound's high selectivity and potency make it a valuable tool for studying CRF1 receptor function. |
| ln Vivo |
In rats under restraint stress, R121919 dose-dependently lowers corticosterone and adrenocortical hormone responses. Peak plasma concentrations of corticosterone and adrenocortical hormone were 25% and 9%, respectively, at a dose of 10 mg/kg R121919 [1]. R121919 has a high dose-response curve that lowers anxiety in rats. Some of the intracellular targets of this medication have been discovered, including GR, MR, BAG-1, and AP-1 [2].
NBI-30775 has demonstrated antidepressant and anxiolytic effects in vivo. As a CRF1R antagonist, it modulates the HPA axis and stress responses, showing potential for the treatment of depression, anxiety, and stress-related disorders. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources. |
| Enzyme Assay |
NBI-30775's binding affinity to the CRF1 receptor can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant human CRF1 receptors. Competition binding experiments are performed with increasing concentrations of NBI-30775 against a fixed concentration of a radiolabeled CRF receptor ligand (e.g., [¹²⁵I]sauvagine). Non-specific binding is determined in the presence of an excess of unlabeled CRF. Ki values are calculated from competition curves.
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| Cell Assay |
The functional activity of NBI-30775 at the CRF1 receptor is evaluated in vitro using cells expressing recombinant CRF1 receptors. Cells are treated with increasing concentrations of NBI-30775, and CRF1 receptor-mediated signaling pathways (e.g., cAMP accumulation or calcium mobilization) are measured. Antagonist activity is assessed by the compound's ability to block CRF-induced signaling.
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| Animal Protocol |
NBI-30775 is administered orally or intraperitoneally in animal models of depression and anxiety. In rodent models (e.g., forced swim test, tail suspension test, elevated plus maze, or open field test), NBI-30775 is given at various doses. Behavioral responses are assessed to evaluate antidepressant and anxiolytic effects.
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| ADME/Pharmacokinetics |
NBI-30775 has a molecular formula of C22H32N6 and a molecular weight of 380.53 g/mol. Its chemical name is 5-[7-(dipropylamino)-2,5-dimethylpyrazolo[1,5-a]pyrimidin-3-yl]-N,N,4-trimethylpyridin-2-amine. Specific pharmacokinetic parameters are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of NBI-30775 is not extensively documented. As a CRF1 receptor antagonist, potential adverse effects may include those related to HPA axis modulation. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
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| Additional Infomation |
NBI-30775 (CAS# 195055-03-9) is also known as R121919. It is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM and over 1000-fold selectivity over CRF2 receptor. NBI-30775 has demonstrated antidepressant and anxiolytic effects.
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| Molecular Formula |
C22H32N6
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| Molecular Weight |
380.54
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| Exact Mass |
380.269
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| CAS # |
195055-03-9
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| PubChem CID |
9821250
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| Appearance |
White to off-white solid powder
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| Density |
1.114g/cm3
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| Index of Refraction |
1.595
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| LogP |
4.408
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
480
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ANNRUWYFVIGKHA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H32N6/c1-8-10-27(11-9-2)20-13-16(4)24-22-21(17(5)25-28(20)22)18-14-23-19(26(6)7)12-15(18)3/h12-14H,8-11H2,1-7H3
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| Chemical Name |
3-[6-(dimethylamino)-4-methylpyridin-3-yl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine
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| Synonyms |
R 121919; R-121919; R121919
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Ethanol : ~100 mg/mL (~262.79 mM)
DMSO : ~6.2 mg/mL (~16.29 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 1.79 mg/mL (4.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: 1.79 mg/mL (4.70 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 1.79 mg/mL (4.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6278 mL | 13.1392 mL | 26.2784 mL | |
| 5 mM | 0.5256 mL | 2.6278 mL | 5.2557 mL | |
| 10 mM | 0.2628 mL | 1.3139 mL | 2.6278 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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