CP 376395

SKU: orb1302946

Description

CP 376395 (CP-316311) is a potent and selective antagonist of the corticotropin-releasing factor receptor 1 (CRF1). This small molecule is a valuable research tool for investigating the CRF system in stress-related disorders, utilized in both in vitro binding assays and in vivo behavioral models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 175140-00-8
• MW: 326.48
• Purity: 99.83% (May vary between batches)
• Formula: C₂₁H₃₀N₂O
• SMILES: O(C1=C(C)C=C(C)C=C1C)C2=C(C)C(NC(CC)CC)=CC(C)=N2
• Target: CRFR
• Solubility: H2O:< 0.1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (12.25 mM);DMSO:100 mg/mL (306.3 mM)

Bioactivity

• In Vivo:
  Pretreatment with CP 376395 (ID50=17.8 mg/kg, p.o.) reverses the excitation of locus coeruleus neurons induced by icv CRF (3 μg) completely blocked the enhanced startle response, while pretreatment with CP 376395(10 mg/kg, p.o.) induced by icv CRF (1 μg) is partially blocked.
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• In Vitro:
  It is highly selective for the human CRF1 receptor subtype,and exhibits affinities against 40 neurotransmitter receptor and ion channels(>1 μM).
• Animal Research:
  Beagle dogs weighing between 8 and 15 kg are administered with CP 376395 hydrochloride salt (1.0 mg/kg) into the cephalic vein of the foreleg. Beagle dogs are treated with CP 376395(10 mg/mL) prepared in 0.1% methyl cellulose at pH 2 by oral.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, CRF, CRFR, CP376395, CP-376395, CP316311, CP-316311, Corticotropin-releasing Factor Receptor, CP 316311, CP 376395

Compound Identifiers

PubChem CID

9862166