1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Taprenepag isopropyl

Taprenepag isopropyl (Synonyms: PF-04217329)

Cat. No.: HY-19998 Purity: 98.77%
Handling Instructions

Taprenepag isopropyl is a highly selective EP2 receptor agonist.

For research use only. We do not sell to patients.

Taprenepag isopropyl Chemical Structure

Taprenepag isopropyl Chemical Structure

CAS No. : 1005549-94-9

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10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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10 mg USD 145 In-stock
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25 mg USD 300 In-stock
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50 mg USD 500 In-stock
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100 mg USD 800 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Taprenepag isopropyl is a highly selective EP2 receptor agonist.

IC50 & Target

EP2 Receptor

 

In Vivo

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 no ocular findings occur for animals in the low-dose group (0.75 mg/day)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

520.60

Formula

C₂₇H₂₈N₄O₅S

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (384.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 5 mg/mL (9.60 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (9.60 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (9.60 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

Taprenepag isopropylPF-04217329PF04217329PF 04217329Prostaglandin ReceptorInhibitorinhibitorinhibit

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Product Name:
Taprenepag isopropyl
Cat. No.:
HY-19998
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