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R121919

Name: R121919
Brand: TargetMol
SKU: T16713
Price: 89 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.75%

Catalog No. T16713Alias NBI30775Cas No. 195055-03-9

Pack Size	Price	USA Warehouse	Global Warehouse
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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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.75%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

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

Chemical Properties

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

	1mg	5mg	10mg	50mg
1 mM	2.6279 mL	13.1396 mL	26.2791 mL	131.3957 mL
5 mM	0.5256 mL	2.6279 mL	5.2558 mL	26.2791 mL
10 mM	0.2628 mL	1.3140 mL	2.6279 mL	13.1396 mL

Ethanol

	1mg	5mg	10mg	50mg
20 mM	0.1314 mL	0.6570 mL	1.3140 mL	6.5698 mL
50 mM	0.0526 mL	0.2628 mL	0.5256 mL	2.6279 mL
100 mM	0.0263 mL	0.1314 mL	0.2628 mL	1.3140 mL

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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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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