Verucerfont-GSK561679-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVerucerfontCat. No.: HY-14875CAS No.: 885220-61-1Synonyms: GSK561679分式: CHNO分量: 406.48作靶點(diǎn): CRFR作通路: GPCR/G Protein儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 86.7 mg/mL (213.29 mM; Need

2、 ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.4601 mL 12.3007 mL 24.6015 mL5 mM 0.4920 mL 2.4601 mL 4.9203 mL10 mM 0.2460 mL 1.2301 mL 2.4601 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Verucerfont促腎上腺質(zhì)激素釋放因受體 1 (CRF1) 的拮抗劑，對(duì)于 CRF1，CRF2 和 CRF-B

3、P 的 IC50 值分別為 6.1，1000 和 1000 nM。IC50 & Target IC50: 6.1 nM (CRF1), 1000 nM (CRF2), 1000 nM (CRF-BP) 1體內(nèi)研究Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEVerucerfont are both significantly differe

4、nt from vehicle, CP-316311, and pexacerfont (PPost hoc analysisshows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6h ofmeasurement (P 1.PROTOCOLAnimal Male Sprague-Dawley rats are received at 175 to 200g and housed in a 12 to 12 light cycle for 1 weekAdministratio

5、n 1 before adrenalectomy. Rats are adrenalectomized at Neurocrine Biosciences, and NaCl is replenished.Adrenalectomy is verified by plasma corticosterone measurements. Seven days after adrenalectomy, rats areimplanted with femoral vein catheters. After 4 days, rats are prepared for blood sampling by

6、 attaching theircatheters to PE50 tubing and a syringe, and acclimated to individual opaque sampling cages for 1h. Thesecages allow sampling to occur without disturbance to the rat. Blood samples (0.3mL) are taken afteracclimation and blood volumes are replaced with 5U/mL heparinized saline. Blood s

7、amples are stored on icewith EDTA. After a baseline blood sample, rats receive oral doses of either vehicle at 5mL/kg or therespective drug (including Verucerfont) in the same volume of vehicle. In each case, the dose is 10mg/kg,based on prior pharmacokinetic studies showing that this dose results i

8、n adequate and comparableexposure. Blood samples are taken 1, 2, 3, 4, and 6h later. Plasma is separated by centrifugation at 4C andstored at -80C for subsequent measurement of ACTH by radioimmunoassay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Schwandt ML, et al. The CRF1 Antagonist Verucerfont in Anxious Alcohol-Dependent Women: Translation of Neuroendocrine, But not ofAnti-Craving Effects. Neuropsychopharmacology. 2016 Nov;41(12):2818-2829.McePdfHeightCaution: Product has not been fully validated for medical a