Taprenepag isopropyl (PF-04217329)
(Synonyms: PF-04217329) 目录号 : GC31919
Taprenepag isopropyl (PF-04217329) 是一种高度选择性的 EP2 受体激动剂。
Cas No.:1005549-94-9
Sample solution is provided at 25 µL, 10mM.
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Taprenepag isopropyl is a highly selective EP2 receptor agonist.
Taprenepag isopropyl is a highly selective EP2 receptor agonist. Intraocular pressure (IOP) in the left, vehicle-dosed eye typically remains within the normal range. In the right (Taprenepag isopropyl-dosed) eye, IOP is reduced in all dose groups. In the high-dose group, IOP is reduced to the extent that it cannot be measured (<4mm Hg) on Days 22 and 29. There are no clinical signs or changes in body weight observed with any dose of Taprenepag isopropyl administration, and noocular findings occur for animals in the low-dose group (0.75 mg/day)[1].
[1]. Yanochko GM, et al. Investigation of ocular events associated with taprenepag isopropyl, a topical EP2 agonist in development for treatment of glaucoma. J Ocul Pharmacol Ther. 2014 Jun;30(5):429-39.
Animal experiment: | Three year-old, male cynomolgus monkeys with body weights ranging from 2.6 to 5.0 kg are used in this study. Animals are dosed twice daily for 28 days in the right eye with Taprenepag isopropyl (0.75, 12, or 36 mg/day), and an equal volume of vehicle (containing cremophor, boric acid, BAC, and EDTA) is dosed in the left eye. An additional 2 monkeys are included in the high-dose group to assess recovery over a 28 day period. Toxicity outcomes are based on the assessment of clinical signs, body weight, ophthalmic examination, pupillary diameter, corneal staining, pachymetry, and noncontact specular microscopy. IOP is measured once during the predose phase and before dosing on Days 1, 8, 15, 22, and 29 of the dosing phase, then once during each week of the recovery period[1]. |
References: [1]. Yanochko GM, et al. Investigation of ocular events associated with taprenepag isopropyl, a topical EP2 agonist in development for treatment of glaucoma. J Ocul Pharmacol Ther. 2014 Jun;30(5):429-39. | |
| Cas No. | 1005549-94-9 | SDF | |
| 别名 | PF-04217329 | ||
| Canonical SMILES | O=S(C1=CN=CC=C1)(N(CC2=CC(OCC(OC(C)C)=O)=CC=C2)CC3=CC=C(N4C=CC=N4)C=C3)=O | ||
| 分子式 | C27H28N4O5S | 分子量 | 520.6 |
| 溶解度 | DMSO : 200 mg/mL (384.17 mM; Need ultrasonic) | 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 | 1.9209 mL | 9.6043 mL | 19.2086 mL |
| 5 mM | 0.3842 mL | 1.9209 mL | 3.8417 mL |
| 10 mM | 0.1921 mL | 0.9604 mL | 1.9209 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: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet