CP 316311 is a potent and selectiveCRF1 receptorantagonist with anIC₅₀value of 6.8 nM.

IC50: 6.8 nM (CRF1 receptor)^[1]

CP 316311 fully antagonizes CRF-stimulated adenylate cyclase activity in rat cortex and at human CRF1 receptors endogenously expressed in IMR32 cells with apparent K_ivalues of 7.6 and 8.5 nM, respectively^[1].

CP 316311 (3.2 mg/kg) inhibits¹²⁵I-oCRF binding by >80% in rats. CP 316311 significantly attenuates activation of the hypothalamic–pituitary–adrenal (HPA) axis, with an MED value of 10 mg/kg, p.o. CP 316311 blocks the effects of both the exogenous and endogenous CRF in the CNS. CP 316311 blocks the effects induced by the exogeneous or endogeneous CRF in the brain in rat models^[1].

327.46

C₂₁H₂₉NO₂

175139-41-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.