A selective CRF1 antagonist
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CP 154,526 (hydrochloride)

Item No. 20732

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-butyl-N-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, monohydrochloride
CAS Number
257639-98-8
Molecular Formula
C23H32N4 • HCl
Formula Weight
401.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 20 mg/mlEthanol: 20 mg/ml
λmax
304 nm
SMILES
CC1=NC(N(CCCC)CC)=C2C(N(C3=C(C)C=C(C)C=C3C)C=C2C)=N1.Cl
InChi Code
InChI=1S/C23H32N4.ClH/c1-8-10-11-26(9-2)22-20-18(6)14-27(23(20)25-19(7)24-22)21-16(4)12-15(3)13-17(21)5;/h12-14H,8-11H2,1-7H3;1H
InChi Key
ZWDLBNCJWNENFF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $36

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    1 mg

    $68

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    5 mg

    $103

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    10 mg

    $169

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    Product Description

    CP 154,526 is an antagonist of corticotropin-releasing factor receptor 1 (CRF1; Ki = 2.7 nM).1,2 It is selective for CRF1 over CRF2 (Ki = >10 μM).1 CP 154,526 inhibits CRF-induced increases in adrenocorticotropic hormone (ACTH) levels in rat plasma with an ID50 value of 10 mg/kg. It increases the time spent in the open arms of the elevated plus maze in rats when administered at a dose of 1 mg/kg.3 CP 154,526 (10 mg/kg, twice per day for 14 days) decreases immobility time in the forced swim test in a rat model of depressive-like behavior.4 It also decreases stress-induced reinstatement of cocaine or heroin self-administration in cocaine- and heroin-trained rats, respectively, when administered at doses of 15 and 30 mg/kg.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schulz, D.W., Mansbach, R.S., Sprouse, J., et al. CP-154,526: A potent and selective nonpeptide antagonist of corticotropin releasing factor receptors. Proc. Natl. Acad. Sci. USA 93(19), 10477-10482 (1996).

    2. Seymour, P.A., Schmidt, A.W., and Schulz, D.W. The pharmacology of CP-154,526, a non-peptide antagonist of the CRH1 receptor: A review. CNS Drug Rev. 9(1), 57-96 (2003).

    3. Lundkvist, J., Chai, Z., Teheranian, R., et al. A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity. Eur. J. Pharmacol. 309(2), 195-200 (1996).

    4. Overstreet, D.H., Keeney, A., and Hogg, S. Antidepressant effects of citalopram and CRF receptor antagonist CP-154,526 in a rat model of depression. Eur. J. Pharmacol. 492(2-3), 195-201 (2004).

    5. Feng, S., Liu, D., Feng, W., et al. Allyl fluorescein ethers as promising fluorescent probes for carbon monoxide imaging in living cells. Anal. Chem. 89(6), 3754-3760 (2017).