R121919 (NBI30775)
(Synonyms: 3-(6-(二甲基氨基)-4-甲基吡啶-3-基)-2,5-二甲基-N,N-二丙基吡唑并[1,5-A]嘧啶-7-胺,NBI30775) 目录号 : GC30792
R121919 (NBI30775) (NBI30775) 是一种有效的小分子 CRF1 受体拮抗剂，对 CRF1 受体的 Ki 为 2 至 5 nM，对 CRF2 受体、CRF 结合蛋白或 70 种其他受体类型的活性弱 1000 倍以上.
Cas No.:195055-03-9
Sample solution is provided at 25 µL, 10mM.
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R121919 is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
R121919 is a potent small-molecule CRF1 receptor antagonistwith high affinity for the CRF1 receptor (Ki=2-5 nM) and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types[1].
R121919 reduces measures of both anxiety and depression in the depressed patients. R121919 dose dependently decreases adrenocorticopin hormone and corticosterone responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively[1]. R121919 reduces levels of anxiety in mice with a steep dose-response curve. Molecules such as GR, MR, BAG-1 and AP-1 have been identified as some of the drug's intracellular targets[2].
[1]. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80. [2]. Post A, et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8.
Animal experiment: | Rats: For the restraint stress,R121919 is dissolved in an aqueous 70% (v/v) polyethylene glycol 400 solution, and serially diluted in this vehicle to the appropriate concentrations. The drug is injected i.v. in a volume of 1 mL/kg to Male Sprague-Dawley rats. For the defensive withdrawal experiments, R121919 solutions are made fresh the night before each experiment. R121919 is dissolved in a vehicle consisting of 5% (v/v) polyethoxylated castor oil[1]. Mice: R121919 is dissolved in an aqueous. The drug is administered orally (1 mL/100 g bodyweight) via a feeding tube to six to ten mice per group; the doses applied are 0.5, 1.0 and 5.0 mg/kg for the DBA/2NCRL mice and 1.0, 5.0, and 30 mg/kg for the DBA/2Ola strain; an additional (vehicle) group of mice receives water, while a further group of mice (untreated controls) are spared the aforementioned manipulations[2]. |
References: [1]. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80. | |
| Cas No. | 195055-03-9 | SDF | |
| 别名 | 3-(6-(二甲基氨基)-4-甲基吡啶-3-基)-2,5-二甲基-N,N-二丙基吡唑并[1,5-A]嘧啶-7-胺,NBI30775 | ||
| Canonical SMILES | CCCN(C1=CC(C)=NC2=C(C3=CN=C(N(C)C)C=C3C)C(C)=NN21)CCC | ||
| 分子式 | C22H32N6 | 分子量 | 380.53 |
| 溶解度 | DMSO : 6.2 mg/mL (16.29 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 | 2.6279 mL | 13.1396 mL | 26.2791 mL |
| 5 mM | 0.5256 mL | 2.6279 mL | 5.2558 mL |
| 10 mM | 0.2628 mL | 1.314 mL | 2.6279 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。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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