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R121919

Cat. No. M29045

All AbMole products are for research use only, cannot be used for human consumption.

R121919 Structure
Synonym:

NBI30775

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Quality Control & Documentation
Biological Activity

R121919 (NBI30775) 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.

Chemical Information
Molecular Weight 380.53
Formula C22H32N6
CAS Number 195055-03-9
Form Solid
Solubility (25°C) Ethanol 100 mg/mL (ultrasonic)
DMSO 6.2 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] David A Gutman, et al. Neuropharmacology. Persistent anxiolytic affects after chronic administration of the CRF₁ receptor antagonist R121919 in rats

[2] David A Gutman, et al. Psychoneuroendocrinology. Behavioral effects of the CRF1 receptor antagonist R121919 in rats selectively bred for high and low activity in the swim test

[3] Kelly H Skelton, et al. Eur J Pharmacol. The CRF1 receptor antagonist, R121919, attenuates the severity of precipitated morphine withdrawal

[4] K Held, et al. J Psychiatr Res. Treatment with the CRH1-receptor-antagonist R121919 improves sleep-EEG in patients with depression

[5] David A Gutman, et al. J Pharmacol Exp Ther. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress

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NBI-27914 hydrochloride 

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K41498 TFA is an antisauvagine-30 (aSvg-30) analog and a strongly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM, and 425 nM for human CRF2α, CRF2β, and CRF1 receptors, respectively.K41498 TFA inhibits sauvagine-stimulated cAMP accumulation in hCRF2α/hCRF2β expressing cells. K41498 TFA can be used in hypotension studies.

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Keywords: R121919, NBI30775 supplier, CRFR, inhibitors, activators

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