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Verucerfont

MCE 国际站：Verucerfont

品牌：MedChemExpress (MCE)

货号：HY-14875

CAS 号：885220-61-1

生物活性： Verucerfont 是一种促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂，对 CRF1、CRF2 和 CRF-BP 的 IC50 分别为 ~6.1、>1000 和 >1000 nM。

体内研究(In Vivo)：Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and Verucerfont are both significantly different from vehicle, CP-316 311, and pexacerfont (Pother. A differential effect of treatments over time is also shown by a significant treatment×time interaction (F[20,140]=6.4, PPost hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6 h of measurement (P[1]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：406.48

Formula：C22H26N6O2

性状：固体

颜色：White to off-white

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：粉末 -20°C 3年

Animal Administration [1]：Male Sprague-Dawley rats are received at 175 to 200 g and housed in a 12 to 12 light cycle for 1 week before adrenalectomy. Rats are adrenalectomized at Neurocrine Biosciences, and NaCl is replenished. Adrenalectomy is verified by plasma corticosterone measurements. Seven days after adrenalectomy, rats are implanted with femoral vein catheters. After ~4 days, rats are prepared for blood sampling by attaching their catheters to PE50 tubing and a syringe, and acclimated to individual opaque sampling cages for 1 h. These cages allow sampling to occur without disturbance to the rat. Blood samples (0.3 mL) are taken after acclimation and blood volumes are replaced with 5 U/mL heparinized saline. Blood samples are stored on ice with EDTA. After a baseline blood sample, rats receive oral doses of either vehicle at 5 mL/kg or the respective drug (including Verucerfont) in the same volume of vehicle. In each case, the dose is 10 mg/kg, based on prior pharmacokinetic studies showing that this dose results in adequate and comparable exposure. Blood samples are taken 1, 2, 3, 4, and 6 h later. Plasma is separated by centrifugation at 4°C and stored at -80 °C for subsequent measurement of ACTH by radioimmunoassay[1]. MCE尚未独立确认这些方法的准确性。 仅供参考。

提供质量检测报告：Data Sheet、SDS、COA、HNMR、LCMS、产品使用指南

产品活性：Verucerfont 是促肾上腺皮质激素释放因子受体 1 (CRF1) 的拮抗剂，对于 CRF1，CRF2 和 CRF-BP 的 IC50 值分别为 6.1，>1000 和 >1000 nM。

IC50 & Target：CRFR1

相关产品：Corticosterone | Corticosterone (Standard) | Galanin (1-30), human | Liproxstatin-1 | SEW​2871 | TRAP-6 | Eglumegad | Prostaglandin D2 | GLP-1(9-36)amide | Daunorubicin hydrochloride | Liquiritin | BODIPY 581/591 C11

热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类

Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides

参考文献：
[1]. Schwandt ML, et al. The CRF1 Antagonist Verucerfont in Anxious Alcohol-Dependent Women: Translation of Neuroendocrine, But not of Anti-Craving Effects. Neuropsychopharmacology. 2016 Nov;41(12):2818-2829.