CP 376395 (CP-316311)
(Synonyms: CP 316,311) 目录号 : GC30863
A CRF1 antagonist
Cas No.:175140-00-8
Sample solution is provided at 25 µL, 10mM.
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CP 376,395 is an antagonist of corticotropin-releasing factor (CRF) receptor 1 (CRF1; IC50 = 5.1 nM).1 It inhibits adenylate cyclase activity stimulated by ovine CRF in rat cerebral cortex and at human CRF1 receptors. CP 376,395 (17.8 mg/kg) inhibits CRF-induced increases in the acoustic startle response in rats. It increases the percentage of open arm entries and time spent in the open arms of the elevated plus maze in mice when administered via intramedial prefrontal cortical injection at doses of 1.5 and 3 nmol.2 CP 376,395 (10 mg/kg) reduces ethanol consumption in rats trained on an intermittent access schedule.3 It increases pulmonary ventilation in rats under normocapnic and hypercapnic conditions when injected into the locus coeruleus at a dose of 5 nmol/0.1 μl.4
1.Chen, Y.L., Obach, R.S., Braselton, J., et al.2-Aryloxy-4-alkylaminopyridines: Discovery of novel corticotropin-releasing factor 1 antagonistsJ. Med. Chem.51(5)1385-1392(2008) 2.Miguel, T.T., Gomes, K.S., and Nunes-de-Souza, R.L.Tonic modulation of anxiety-like behavior by corticotropin-releasing factor (CRF) type 1 receptor (CRF1) within the medial prefrontal cortex (mPFC) in male mice: Role of protein kinase A (PKA)Horm. Behav.66(2)247-256(2014) 3.Simms, J.A., Nielsen, C.K., Li, R., et al.Intermittent access ethanol consumption dysregulates CRF function in the hypothalamus and is attenuated by the CRF-R1 antagonist, CP-376395Addict. Biol.19(4)606-611(2014) 4.Incheglu, J.M., Bicego, K.C., and Gargaglioni, L.H.Corticotropin-releasing factor in the locus coeruleus as a modulator of ventilation in ratsRespir. Physiol. Neurobiol.23373-80(2016)
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 | |
| 别名 | CP 316,311 | ||
| Canonical SMILES | CCC(CC)NC1=C(C)C(OC2=C(C)C=C(C)C=C2C)=NC(C)=C1 | ||
| 分子式 | C21H30N2O | 分子量 | 326.48 |
| 溶解度 | DMSO : ≥ 100 mg/mL (306.30 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 3.063 mL | 15.3149 mL | 30.6297 mL |
| 5 mM | 0.6126 mL | 3.063 mL | 6.1259 mL |
| 10 mM | 0.3063 mL | 1.5315 mL | 3.063 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet