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CP-376395 is a CRF1-selective antagonist. CP-376395 fully antagonizes oCRF-stimulated adenylate cyclase activity in rat cerebral cortex and at human CRF1 receptors with an apparent Ki value of 12 nM, indicating antagonist functional activity. In the CNS, systemically administered CP-376395 blocks the effects of both exogenous and endogenous CRF. CP-376395 treatment reverses the excitation of locus coeruleus neurons induced by icv CRF (3 µg) with an ID50 of completely blocked the enhanced startle response induced by icv CRF (1 µg) at 17.8 mg/kg, p.o. and partially blocked at 10 mg/kg, p.o. without significantly altering baseline startle.
| Molecular Weight | 326.48 |
| Formula | C21H30N2O |
| CAS Number | 175140-00-8 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CRFR Products |
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| DMP 696
DMP 696 is a selective corticotropin-releasing hormone receptor 1 (CRHR1) antagonist, used for the treatment of anxiety and depression. |
| Antalarmin
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. |
| Antisauvagine-30
Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF2 receptor antagonist with Kd values of 1.4 nM and 153.6 nM for mouse CRF2β and rat CRF1 receptors, respectively. |
| NBI-27914 hydrochloride
NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a Ki value of 1.7 nM. |
| K41498 TFA
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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