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CRF1 receptor antagonist-1

Cat. No. M42172
CRF1 receptor antagonist-1 Structure
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Biological Activity

CRF1 receptor antagonist-1 is a CRF1 receptor antagonist.

Chemical Information
Molecular Weight 499.04
Formula C27H28ClFN2O2S
CAS Number 2635364-30-4
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ana Cláudia Cipriano et al. Horm Behav. CRF receptor type 1 (but not type 2) located within the amygdala plays a role in the modulation of anxiety in mice exposed to the elevated plus maze

[2] Courtney L Williams et al. J Neurosci. CRF-R2 and the heterosynaptic regulation of VTA glutamate during reinstatement of cocaine seeking

[3] Vineet C Chitravanshi et al. Am J Physiol Heart Circ Physiol. Mechanisms of cardiovascular actions of urocortins in the hypothalamic arcuate nucleus of the rat

[4] Yuhpyng L Chen et al. J Med Chem. 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists

[5] Shoshiro Okada et al. Eur J Pharmacol. Extrahypothalamic corticotropin-releasing hormone mediates (-)-nicotine-induced elevation of plasma corticosterone in rats

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