CP 376395

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CP 376395 是一种有效且特异性的促肾上腺皮质激素释放因子 1 (CRF1) 受体拮抗剂。

CP 376395 is an effective and specific Corticotropin-releasing factor 1 (CRF1) receptor antagonist.(In Vitro):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. It is highly selective for the human CRF1 receptor subtype; affinity for the CRF2 receptor is >10000 nM. It shows affinities greater than 1 μM against 40 neurotransmitter receptor and ion channels.(In Vivo):In the CNS, systemically administered CP 376395 blocks the effects of both exogenous and endogenous CRF. Pretreatment with CP 376395 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. The attenuation of fear-potentiated startle is statistically significant at lower doses (0.32-3.2 mg/kg, p.o., with 62-83% blockade) and completely reversed by CP 376395 at 10 mg/kg, p.o.

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Animal Model:Male B6 mice (n=8-9 per group)Dosage:0.0, 10.0, or 20.0 mg/kg Administration:Intraperitoneally.Result:Dose-dependently attenuated intake of H2O and food, with H2O intake affected specifically during the first half of the session.

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Others

Other Targets

CRF1

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175140-00-8

326.48

C21H30N2O

>98% (HPLC)

DMSO : ≥ 100 mg/mL 306.30 mM ;H2O : < 0.1 mg/mL

CCC(CC)NC1=CC(=NC(=C1C)OC2=C(C=C(C=C2C)C)C)C

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(-20℃)

With Ice Pack

≥ 2 years