A CRF1 antagonist
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CP 376,395

Item No. 29188

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1-ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-4-pyridinamine
CAS Number
175140-00-8
Synonyms
  • CP 316,311
Molecular Formula
C21H30N2O
Formula Weight
326.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 15 mg/mlEthanol: 30 mg/ml
λmax
216, 252 nm
SMILES
CC1=C(OC2=NC(C)=CC(NC(CC)CC)=C2C)C(C)=CC(C)=C1
InChi Code
InChI=1S/C21H30N2O/c1-8-18(9-2)23-19-12-16(6)22-21(17(19)7)24-20-14(4)10-13(3)11-15(20)5/h10-12,18H,8-9H2,1-7H3,(H,22,23)
InChi Key
VIZBSVDBNLAVAW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $128

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    5 mg

    $440

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    10 mg

    $685

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    Product Description

    CP 376,395 is an antagonist of corticotropin-releasing factor (CRF) receptor 1 (CRF1; IC50 = 5.1 nM).1 It inhibits adenylate cyclase activity stimulated by ovine CRF in rat cerebral cortex and at human CRF1 receptors. CP 376,395 (17.8 mg/kg) inhibits CRF-induced increases in the acoustic startle response in rats. It increases the percentage of open arm entries and time spent in the open arms of the elevated plus maze in mice when administered via intramedial prefrontal cortical injection at doses of 1.5 and 3 nmol.2 CP 376,395 (10 mg/kg) reduces ethanol consumption in rats trained on an intermittent access schedule.3 It increases pulmonary ventilation in rats under normocapnic and hypercapnic conditions when injected into the locus coeruleus at a dose of 5 nmol/0.1 μl.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, Y.L., Obach, R.S., Braselton, J., et al. 2-Aryloxy-4-alkylaminopyridines: Discovery of novel corticotropin-releasing factor 1 antagonists. J. Med. Chem. 51(5), 1385-1392 (2008).

    2. Miguel, T.T., Gomes, K.S., and Nunes-de-Souza, R.L. Tonic modulation of anxiety-like behavior by corticotropin-releasing factor (CRF) type 1 receptor (CRF1) within the medial prefrontal cortex (mPFC) in male mice: Role of protein kinase A (PKA). Horm. Behav. 66(2), 247-256 (2014).

    3. Simms, J.A., Nielsen, C.K., Li, R., et al. Intermittent access ethanol consumption dysregulates CRF function in the hypothalamus and is attenuated by the CRF-R1 antagonist, CP-376395. Addict. Biol. 19(4), 606-611 (2014).

    4. Incheglu, J.M., Bicego, K.C., and Gargaglioni, L.H. Corticotropin-releasing factor in the locus coeruleus as a modulator of ventilation in rats. Respir. Physiol. Neurobiol. 233, 73-80 (2016).