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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 |
|---|
| Verucerfont
Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively. |
| Antalarmin hydrochloride
Antalarmin hydrochloride is a non-peptide CRF1 corticotropin-releasing factor receptor antagonist with a Ki of 1 nM. |
| CP-154526 hydrochloride
CP-154526 hydrochloride is a selective, non-peptide antagonist of corticotropin releasing factor receptors (CRF1) with a Ki of 2.7 nM. CP 154526 hydrochloride shows selective for CRF1 over CRF2 (Ki = >10 μM). |
| CRF (bovine) TFA
CRF (bovine) TFA is a potent agonist of CRF receptor, and displaces [125I-Tyr]ovine CRF with a Ki of 3.52 nM. |
| Corticotropin-releasing factor (human)
Corticotropin-releasing factor human (Human CRF) stimulates the synthesis and secretion of adrenocorticotropin in the anterior pituitary. |
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