CP 154526
CP 154526 is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 has anxiolytic activities.
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- CAS No.: 157286-86-7
- 화학식: C23H32N4
- 분자량:364.53
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.011 μM
Compound: 8, CP-154,526
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Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
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[PMID: 21414781] |
CP 154526 displaces [125I][Tyr0]CRF from rat hippocampal CRF receptors (IC50 = 0.5 nM) and from pituitary CRF receptors (IC50 = 0.04 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley rats[2]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:i.p.; once
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Result:Exhibited signs of anxiolytic-like activity.
Chemical Information
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CAS No. 157286-86-7
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분자량 364.53
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화학식 C23H32N4
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SMILES
CC1=C(N2C=C(C)C3=C(N(CCCC)CC)N=C(C)N=C32)C(C)=CC(C)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. J Lundkvist, et al. A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity. Eur J Pharmacol. 1996 Aug 8;309(2):195-200. [Content Brief]
[2]. D W Schulz, et al. CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors. Proc Natl Acad Sci U S A. 1996 Sep 17;93(19):10477-82. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)