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Purity: ≥98%
CP 376395 is a novel potent, selective and orally bioactive antagonist of Corticotropin releasing factor 1 (CRF1) receptor. It is a clinical candidate that, when taken orally, significantly improved both the feeding response in humans and dogs. In an effort to resolve the food effect problem, CP 376395, an orally active CRF 1 receptor antagonist, was discovered. It demonstrated enhanced physicochemical properties while maintaining the intended pharmacological properties. It was decided to move CP 376395 to the clinic.
| Targets |
CRFR2; CRFR1
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|---|---|
| ln Vitro |
CP 376395 fully antagonizes oCRF-stimulated adenylyl cyclase activity in the antivascular cerebral cortex and human CRF1 receptors with an apparent Ki value of 12 nM, indicating highly selective antagonist functional activity. It has an affinity greater than 1 µM for 40 neurotransmitter mass receptors and ion channels [1].
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| ln Vivo |
CP 376395 (10-20 mg/kg, i.p., in batch B6 mice) reduces H2O and food acceptance, increases sucrose acceptance, and decreases EtOH acceptance, but does not reduce EtOH preference [2]. Model: Male B6 mice (n=8-9 per group) [2] Dosage: 0.0, 10.0 or 20.0 mg/kg Administration method: intraperitoneal injection Results: H2O and food intake were dose-dependently attenuated, in which H2O intake was particularly affected during the first half of the dosing session.
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| Animal Protocol |
Male B6 mice (n=8-9 per group)
0.0, 10.0, or 20.0 mg/kg Intraperitoneally |
| References |
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| Molecular Formula |
C20H28N2O
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|---|---|---|
| Molecular Weight |
312.46
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| Exact Mass |
312.22
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| Elemental Analysis |
C, 76.88; H, 9.03; N, 8.97; O, 5.12
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| CAS # |
175140-00-8
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| Related CAS # |
CP 376395 hydrochloride; 1013933-37-3
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| Appearance |
Solid powder
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| SMILES |
CCC(CC)NC1=C(C(=NC(=C1)C)OC2=C(C=C(C=C2C)C)C)C
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| InChi Key |
VIZBSVDBNLAVAW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H30N2O/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)
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.66 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2004 mL | 16.0020 mL | 32.0041 mL | |
| 5 mM | 0.6401 mL | 3.2004 mL | 6.4008 mL | |
| 10 mM | 0.3200 mL | 1.6002 mL | 3.2004 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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