Revefenacin (TD-4208)
(Synonyms: 雷芬那辛,TD-4208; GSK1160724) 目录号 : GC31761
Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.
Cas No.:864750-70-9
Sample solution is provided at 25 µL, 10mM.
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Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.
Revefenacin is a high affinity competitive antagonist at human recombinant mAChRs with kinetic functional selectivity for M3 over M2 mAChRs and a potent, slowly reversible antagonist in rat, guinea pig, and human airway tissues expressing native mAChRs[1].
[1] Hegde SS, et al. Pharmacol Res Perspect. 2018, 6(3):e00400.
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Animal experiment: |
Rats: To determine the bronchoprotective and antisialagogue potency after a single dose, rats are exposed by inhalation to a nebulized solution of revefenacin (3–3000 µg/mL), tiotropium (0.3–300 µg/mL), glycopyrronium (1–1000 µg/mL), or vehicle (sterile water). Bronchoprotective activity is assessed 24 hours postdose. For the antisialagogue effect, inhibition of Pilo is assessed 1, 6, or 12 hours after inhalation of an efficacious dose of test compound to determine the time point at which peak effect occurred. All subsequent doses are measured at this time point[2]. |
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References: [1]. Steinfeld T, et al. In vitro characterization of TD-4208, a lung-selective and long-acting muscarinic antagonist bronchodilator (Abstract). Am J Respir Crit Care Med 179:A4553. |
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| Cas No. | 864750-70-9 | SDF | |
| 别名 | 雷芬那辛,TD-4208; GSK1160724 | ||
| Canonical SMILES | O=C(OC1CCN(CCN(C(C2=CC=C(CN3CCC(C(N)=O)CC3)C=C2)=O)C)CC1)NC4=CC=CC=C4C5=CC=CC=C5 | ||
| 分子式 | C35H43N5O4 | 分子量 | 597.75 |
| 溶解度 | DMSO : ≥ 125 mg/mL (209.12 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 | 1.6729 mL | 8.3647 mL | 16.7294 mL |
| 5 mM | 0.3346 mL | 1.6729 mL | 3.3459 mL |
| 10 mM | 0.1673 mL | 0.8365 mL | 1.6729 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet