CP 376395 hydrochlorideCAS# 1013933-37-3 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1013933-37-3 | SDF | Download SDF |
| PubChem ID | 24806455 | Appearance | Powder |
| Formula | C21H31ClN2O | M.Wt | 362.94 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in water and to 100 mM in DMSO | ||
| Chemical Name | 3,6-dimethyl-N-pentan-3-yl-2-(2,4,6-trimethylphenoxy)pyridin-4-amine;hydrochloride | ||
| SMILES | CCC(CC)NC1=CC(=NC(=C1C)OC2=C(C=C(C=C2C)C)C)C.Cl | ||
| Standard InChIKey | UDIOZDHQQNYISB-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H30N2O.ClH/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);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent and selective CRF1 receptor antagonist (Ki values are 12 and >10000 nM for CRF1 and CRF2 receptors respectively). Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active. |
CP 376395 hydrochloride Dilution Calculator
CP 376395 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7553 mL | 13.7764 mL | 27.5528 mL | 55.1055 mL | 68.8819 mL |
| 5 mM | 0.5511 mL | 2.7553 mL | 5.5106 mL | 11.0211 mL | 13.7764 mL |
| 10 mM | 0.2755 mL | 1.3776 mL | 2.7553 mL | 5.5106 mL | 6.8882 mL |
| 50 mM | 0.0551 mL | 0.2755 mL | 0.5511 mL | 1.1021 mL | 1.3776 mL |
| 100 mM | 0.0276 mL | 0.1378 mL | 0.2755 mL | 0.5511 mL | 0.6888 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Structure of class B GPCR corticotropin-releasing factor receptor 1.[Pubmed:23863939]
Nature. 2013 Jul 25;499(7459):438-43.
Structural analysis of class B G-protein-coupled receptors (GPCRs), cell-surface proteins that respond to peptide hormones, has been restricted to the amino-terminal extracellular domain, thus providing little understanding of the membrane-spanning signal transduction domain. The corticotropin-releasing factor receptor type 1 is a class B receptor which mediates the response to stress and has been considered a drug target for depression and anxiety. Here we report the crystal structure of the transmembrane domain of the human corticotropin-releasing factor receptor type 1 in complex with the small-molecule antagonist CP-376395. The structure provides detailed insight into the architecture of class B receptors. Atomic details of the interactions of the receptor with the non-peptide ligand that binds deep within the receptor are described. This structure provides a model for all class B GPCRs and may aid in the design of new small-molecule drugs for diseases of brain and metabolism.
2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists.[Pubmed:18288792]
J Med Chem. 2008 Mar 13;51(5):1385-92.
An orally active clinical candidate of corticotropin-releasing factor 1 (CRF 1) antagonist 1 showed a significant positive food effect in dog and human after oral administration. Efforts to address the food effect issue led us to explore and discover compounds in series 2 as orally active CRF 1 receptor antagonists, in which some compounds showed improved physicochemical properties while retaining desired pharmacological properties. Compound 3a (CP-376395) was selected for further development, due not only to its reduced food effects but also its greater efficacy in CNS models. Compound 3a was advanced to the clinic. The synthesis of representative potential candidates and their in vitro, ex vivo, and in vivo data are described.
