CP 376395 (CP-316311) (Synonyms: CP 316,311) |
| Catalog No.GC30863 |
CP 376395 (CP-316311) est un antagoniste puissant et sélectif du récepteur du facteur de libération de la corticotropine 1 (CRF1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 175140-00-8
Sample solution is provided at 25 µL, 10mM.
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CP 376395 is a potent and selective Corticotropin releasing factor 1 (CRF1) receptor antagonist.
CP 376395 fully antagonizes oCRF-stimulated adenylate cyclase activity in rat cerebral cortex and at human CRF1 receptors with an apparent Ki value of 12 nM, indicating antagonist functional activity. It is highly selective for the human CRF1 receptor subtype; affinity for the CRF2 receptor is >10000 nM. It shows affinities greater than 1 µM against 40 neurotransmitter receptor and ion channels[1].
In the CNS, systemically administered CP 376395 blocks the effects of both exogenous and endogenous CRF. Pretreatment with CP 376395 reverses the excitation of locus coeruleus neurons induced by icv CRF (3 µg) with an ID50 of completely blocked the enhanced startle response induced by icv CRF (1 µg) at 17.8 mg/kg, p.o. and partially blocked at 10 mg/kg, p.o. without significantly altering baseline startle. The attenuation of fear-potentiated startle is statistically significant at lower doses (0.32-3.2 mg/kg, p.o., with 62-83% blockade) and completely reversed by CP 376395 at 10 mg/kg, p.o[1].
[1]. Chen YL, et al. 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J Med Chem. 2008 Mar 13;51(5):1385-92.
Animal experiment: | Dogs: Four beagle dogs (two male and two female) weighing between 8 and 15 kg are administered 1 mesylate salt or CP 376395 hydrochloride salt (1.0 mg/kg) into the cephalic vein of the foreleg. The dosing solution for 1 is neat ethanol (15.4 mg/mL) and for CP 376395 is sterile saline at pH 2 (10 mg/mL). Oral dosing is conducted by gavage with drugs suspended in 0.1% methyl cellulose at pH 2. For the intravenous and fasted oral legs of the study, animals have last eaten approximately 21 h prior to drug administration and are permitted food and water approximately 3.5 h postdose. In the fed oral leg of the study, the animals are given one can of wet dog food 1 h before dosing. Blood samples are collected by venipuncture of the jugular vein prior to drug administration and at time points of 0.083 (i.v. only), 0.25, 0.5, 1.0, 2.0, 3.0, 4.0, 6.0, 8.0, 12, and 24 h postdose, processed to obtain serum and stored frozen until the day of analysis[1]. |
References: [1]. Chen YL, et al. 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J Med Chem. 2008 Mar 13;51(5):1385-92. | |
| Cas No. | 175140-00-8 | SDF | |
| Synonymes | CP 316,311 | ||
| Canonical SMILES | CCC(CC)NC1=C(C)C(OC2=C(C)C=C(C)C=C2C)=NC(C)=C1 | ||
| Formula | C21H30N2O | M.Wt | 326.48 |
| Solubility | DMSO : ≥ 100 mg/mL (306.30 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.063 mL | 15.3149 mL | 30.6297 mL |
| 5 mM | 612.6 μL | 3.063 mL | 6.1259 mL |
| 10 mM | 306.3 μL | 1.5315 mL | 3.063 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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