Taprenepag isopropyl (PF-04217329) (Synonyms: PF-04217329) |
| Catalog No.GC31919 |
Taprenepag isopropÍlico (PF-04217329) es un agonista del receptor EP2 altamente selectivo.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Sinónimos | 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 | ||
| Formula | C27H28N4O5S | M.Wt | 520.6 |
| Solubility | DMSO : 200 mg/mL (384.17 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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