Treprostinil
Based on 1 publication(s) in Google Scholar
Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 81846-19-7
- Formula: C23H34O5
- Molecular Weight:390.51
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Treprostinil
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Biological Activity
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IP Receptor 1.9 nM (EC50) |
TP Receptor 919 nM (EC50) |
IP Receptor 32.1 nM (Ki) |
FP Receptor 4680 nM (Ki) |
Treprostinil has high affinity for the DP1, EP2 and IP receptors (Ki=4.4, 3.6 and 32 nM, respectively), low affinity for EP1 and EP4 receptors and even lower affinity for EP3, FP and TP receptors. Activation of IP, DP1 and EP2 receptors, as with treprostinil, can all result in vasodilatation of human pulmonary arteries[1].Treprostinil inhibits viability of cultured endothelial colony forming cells. Endothelial colony forming cells proliferation is stimulated by conditioned media from Treprostinil pretreated mesenchymal stem cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 81846-19-7
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Appearance Solid
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Molecular Weight 390.51
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Formula C23H34O5
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Color White to off-white
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SMILES
OC(COC1=CC=CC2=C1C[C@](C[C@@H](O)[C@@H]3CC[C@@H](O)CCCCC)([H])[C@]3([H])C2)=O
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Synonyms
UT-15
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell
2023 Dec 7;186(25):5500-5516.e21. PMID: 38016470
Solvent & Solubility
DMSO : ≥ 125 mg/mL (320.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Human or murine hematopoietic stem and progenitor cells are incubated in the presence of vehicle or the combination of 10 μM Treprostinil and 30 μM forskolin at 37°C for 1 hour and 24 hours. After washing with phosphate-buffered saline at 4°C, cells are stained for externalized phosphatidylserine with the apoptosis kit[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[3]
Male Lewis rats weighing 200-300 g are used in the study. Donor animals receive treprostinil or placebo 24 h before hepatectomy and the corresponding recipient animal receive the similar treatment until the time of sacrifice. The surgeon is blinded to treatment. Recipients are sacrificed at 1, 3, 6, 24 and 48 h post-transplantation to examine the early events after IRI. Treprostinil (100 ng/kg/min) or placebo is administered subcutaneously via an Alzet implantable osmotic pump. This dose is selected to achieve a steady-state plasma concentration in the range of 5-20 ng/mL[3].
Mice[6]
Bone marrow transplanted (BMT) mice are divided into five different groups with each group consisting of 6 to 10 mice. One group of mice is exposed to hypoxia (10% inspired oxygen fraction) in a normobaric chamber whereas the second group (control BMT) of animals are placed in a normoxic chamber with a normal oxygen environment (21% inspired O2 fraction) for 28 days. Sham group mice receive saline treatment whereas two other groups of mice receive Treprostinil infusions of different dose levels (14 ng/kg and 70 ng/kg per minitue) and are exposed to hypoxia for 4 weeks. For comparison, human infusion rates in PAH therapy vary from 10 to 60 ng/kg per min[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Whittle BJ, et al. Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist. Biochem Pharmacol. 2012 Jul 1;84(1):68-75. [Content Brief]
[2]. Ferrantino M, et al. Inhaled treprostinil sodium for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2011 Nov;12(16):2583-93. [Content Brief]
[3]. Ghonem N, et al. Treprostinil, a prostacyclin analog, ameliorates ischemia-reperfusion injury in rat orthotopic liver transplantation. Am J Transplant. 2011 Nov;11(11):2508-16. [Content Brief]
[4]. Smadja DM, et al. Treprostinil indirectly regulates endothelial colony forming cell angiogenic properties by increasing VEGF-A produced by mesenchymal stem cells. Thromb Haemost. 2015 Oct;114(4):735-47. [Content Brief]
[5]. Kazemi Z, et al. Repurposing Treprostinil for Enhancing Hematopoietic Progenitor Cell Transplantation. Mol Pharmacol. 2016 Jun;89(6):630-44. [Content Brief]
[6]. Nikam VS, et al. Treprostinil inhibits the recruitment of bone marrow-derived circulating fibrocytes in chronic hypoxic pulmonary hypertension. Eur Respir J. 2010 Dec;36(6):1302-14. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5608 mL | 12.8038 mL | 25.6075 mL | 64.0188 mL |
| 5 mM | 0.5122 mL | 2.5608 mL | 5.1215 mL | 12.8038 mL | |
| 10 mM | 0.2561 mL | 1.2804 mL | 2.5608 mL | 6.4019 mL | |
| 15 mM | 0.1707 mL | 0.8536 mL | 1.7072 mL | 4.2679 mL | |
| 20 mM | 0.1280 mL | 0.6402 mL | 1.2804 mL | 3.2009 mL | |
| 25 mM | 0.1024 mL | 0.5122 mL | 1.0243 mL | 2.5608 mL | |
| 30 mM | 0.0854 mL | 0.4268 mL | 0.8536 mL | 2.1340 mL | |
| 40 mM | 0.0640 mL | 0.3201 mL | 0.6402 mL | 1.6005 mL | |
| 50 mM | 0.0512 mL | 0.2561 mL | 0.5122 mL | 1.2804 mL | |
| 60 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0670 mL | |
| 80 mM | 0.0320 mL | 0.1600 mL | 0.3201 mL | 0.8002 mL | |
| 100 mM | 0.0256 mL | 0.1280 mL | 0.2561 mL | 0.6402 mL |
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