| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Treprostinil sodium (LRX-15; Remodulin for infusion, Orenitram for oral, and Tyvaso for inhalation), a synthetic analog of prostacyclin (PGI2), is a novel and potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively. Treprostinil is a vasodilator that is applied to the management of hypertension in the lungs. The FDA approved treprostinil inhalation form in July 2009; it is sold under the trade name Tyvaso.
| Targets |
IP Receptor ( EC50 = 1.9 nM ); TP Receptor ( EC50 = 919 nM ); IP Receptor ( Ki = 32.1 nM ); FP Receptor ( Ki = 4680 nM ); DP1 ( EC50 = 0.6±0.1 nM ); EP2 ( EC50 = 6.2±1.2 nM ); DP1 ( EC50 = 4.4 nM ); EP2 ( EC50 = 3.6 nM ); EP4 ( EC50 = 826 nM ); EP3 ( EC50 = 2505 nM ); EP1 ( Ki = 212 nM ); EP1 ( EC50 = 285 nM ); EP3 ( EC50 = 68.9 nM ); EP4 ( EC50 = 181 nM )
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| ln Vitro |
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| ln Vivo |
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| Cell Assay |
Hematopoietic stem and progenitor cells from humans or mice are cultured for one hour and twenty-four hours at 37°C either in the presence of vehicle or in combination with 10 μM Treprostinil and 30 μM forskolin. The apoptosis kit is used to stain cells for externalized phosphatidylserine after they have been washed with phosphate-buffered saline at 4°C[5].
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| Animal Protocol |
Rats: For the study, male Lewis rats weighing between 200 and 300 g are employed. 24 hours prior to hepatectomy, donor animals are given treprostinil or a placebo, and the corresponding recipient animal receives the same care until the moment of sacrifice. Treatment is invisible to the surgeon. To study what happens right after IRI, recipients are sacrificed 1, 3, 6, 24 and 48 hours after transplantation. Using an Alzet implantable osmotic pump, subcutaneous administration of treprostinil (100 ng/kg/min) or placebo is performed. This dosage is chosen to produce a plasma concentration that is steady-state and falls between 5 and 20 ng/mL[3].
Mice: Mice that have had bone marrow transplantation (BMT) are split up into five groups, each with six to ten mice. In a normobaric chamber, one group of mice is exposed to hypoxia (10% inspired oxygen fraction), while the other group of mice (control BMT) spends 28 days in a normoxic chamber with a normal oxygen environment (21% inspired O2 fraction). While the two other groups of mice receive four weeks of hypoxic exposure and receive Treprostinil infusions at varying dose levels (14 ng/kg and 70 ng/kg per minute), the sham group mice receive saline treatment. Comparatively, infusion rates for humans in PAH therapy range from 10 to 60 ng/kg per minute[6]. |
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| References |
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| Molecular Formula |
C23H33NAO5
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|---|---|
| Molecular Weight |
412.4949
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| Exact Mass |
412.22
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| Elemental Analysis |
C, 66.97; H, 8.06; Na, 5.57; O, 19.39
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| CAS # |
289480-64-4
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| Related CAS # |
Treprostinil;81846-19-7; Treprostinil diethanolamine; 830354-48-8
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| Appearance |
Solid powder
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| SMILES |
CCCCC[C@@H](CC[C@H]1[C@@H](C[C@H]2[C@@H]1CC3=C(C2)C(=CC=C3)OCC(=O)[O-])O)O.[Na+]
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| InChi Key |
IQKAWAUTOKVMLE-ZSESPEEFSA-M
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| InChi Code |
InChI=1S/C23H34O5.Na/c1-2-3-4-7-17(24)9-10-18-19-11-15-6-5-8-22(28-14-23(26)27)20(15)12-16(19)13-21(18)25;/h5-6,8,16-19,21,24-25H,2-4,7,9-14H2,1H3,(H,26,27);/q;+1/p-1/t16-,17-,18+,19-,21+;/m0./s1
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| Chemical Name |
sodium;2-[[(1R,2R,3aS,9aS)-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[g]naphthalen-5-yl]oxy]acetate
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| Synonyms |
UT-15; LRX 15 sodium; UT 15; LRX15 sodium; UT15; LRX-15 sodium; BW 15AU sodium; U-62840 sodium; Uniprost; Treprostinil; Orenitram; Remodulin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~82 mg/mL (~198.8 mM)
Water: 82 mg/mL Ethanol: 82 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (121.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4243 mL | 12.1215 mL | 24.2430 mL | |
| 5 mM | 0.4849 mL | 2.4243 mL | 4.8486 mL | |
| 10 mM | 0.2424 mL | 1.2122 mL | 2.4243 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03045029 | Active Recruiting |
Drug: Oral treprostinil | Pulmonary Arterial Hypertension | United Therapeutics | July 18, 2017 | N/A |
| NCT05176951 | Active Recruiting |
Drug: Treprostinil Palmitil Drug: Placebo |
Pulmonary Hypertension | Insmed Incorporated | December 22, 2022 | Phase 2 |
| NCT05060315 | Active Recruiting |
Combination Product: Remunity Pump for Remodulin |
Pulmonary Arterial Hypertension | United Therapeutics | July 5, 2023 | N/A |
| NCT03835676 | Recruiting | Drug: Treprostinil | Pulmonary Hypertension | Magdi H. Yacoub | May 1, 2019 | Phase 4 |
| NCT04005469 | Recruiting | Drug: Treprostinil | Ischemia Reperfusion Injury Delayed Graft Function |
Rhode Island Hospital | November 13, 2020 | Phase 1 Phase 2 |
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