Verucerfont
(Synonyms: 3-(4-甲氧基-2-甲基苯基)-2,5-二甲基-N-[(1S)-1-(3-甲基-1,2,4-恶二唑-5-基)丙基]吡唑并[1,5-A]嘧啶-7-胺,GSK561679) 目录号 : GC19374
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。
Cas No.:885220-61-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | 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]. |
References: [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. | |
Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.
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 (PPost hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6 h of measurement (P<0.001 vs vehicle at each time-point, and vs the respective pretreatment baseline)[1].
References:
[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.
| Cas No. | 885220-61-1 | SDF | |
| 别名 | 3-(4-甲氧基-2-甲基苯基)-2,5-二甲基-N-[(1S)-1-(3-甲基-1,2,4-恶二唑-5-基)丙基]吡唑并[1,5-A]嘧啶-7-胺,GSK561679 | ||
| Canonical SMILES | CC[C@H](NC1=CC(C)=NC2=C(C3=CC=C(OC)C=C3C)C(C)=NN12)C4=NC(C)=NO4 | ||
| 分子式 | C22H26N6O2 | 分子量 | 406.48 |
| 溶解度 | DMSO : 86.7 mg/mL (213.29 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4601 mL | 12.3007 mL | 24.6015 mL |
| 5 mM | 0.492 mL | 2.4601 mL | 4.9203 mL |
| 10 mM | 0.246 mL | 1.2301 mL | 2.4601 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。