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.
For research use only. We do not sell to patients.
- CAS No.: 157286-86-7
- Formula: C23H32N4
- Molecular Weight:364.53
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.011 μM
Compound: 8, CP-154,526
|
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
|
[PMID: 21414781] |
In Vitro
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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male Sprague Dawley rats[2]
-
Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
-
Administration:i.p.; once
-
Result:Exhibited signs of anxiolytic-like activity.
Chemical Information
-
CAS No. 157286-86-7
-
Molecular Weight 364.53
-
Formula C23H32N4
-
SMILES
CC1=C(N2C=C(C)C3=C(N(CCCC)CC)N=C(C)N=C32)C(C)=CC(C)=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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)