RG7713 (RO5028442)
(Synonyms: RO5028442) 目录号 : GC30890
A vasopressin V1a receptor antagonist
Cas No.:920022-47-5
Sample solution is provided at 25 µL, 10mM.
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RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).1 It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 ?M.
1.Ratni, H., Rogers-Evans, M., Bissantz, C., et al.Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approachJ. Med. Chem.58(5)2275-2289(2015)
Cell experiment: | CHO cells are stably transfected with expression plasmids encoding human V1a and grown in F-12 K, containing 10% fetal bovine serum, 1% penicillin-streptomycin, 1% glutamate, and 200 μg/mL geneticin at 37 °C in a 10% CO2 incubator at 95% humidity. Cells are plated for 24 h at 50,000 cells/well in clear bottomed 96 well plates and are dye loaded for 60 min with 2 μM Fluo-4-AM in assay buffer. After cell washing, the plate is loaded on a fluorometricimaging plate reader, compound dilution series added to the cells, and agonist activity measured[1]. |
References: [1]. Ratni H, et al. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. J Med Chem. 2015 Mar 12;58(5):2275-89. | |
| Cas No. | 920022-47-5 | SDF | |
| 别名 | RO5028442 | ||
| Canonical SMILES | O=C(C1=CN(CCN(C)C)C2=C1C=CC(Cl)=C2)N3CCC4(C(C=CC=C5)=C5CO4)CC3 | ||
| 分子式 | C25H28ClN3O2 | 分子量 | 437.96 |
| 溶解度 | DMSO : 20 mg/mL (45.67 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 | 2.2833 mL | 11.4166 mL | 22.8331 mL |
| 5 mM | 0.4567 mL | 2.2833 mL | 4.5666 mL |
| 10 mM | 0.2283 mL | 1.1417 mL | 2.2833 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