1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Treprostinil sodium

Treprostinil sodium (Synonyms: UT-15)

Cat. No.: HY-16504 Purity: ≥98.0%
Handling Instructions

Treprostinil sodium 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.

Treprostinil sodium Chemical Structure

Treprostinil sodium Chemical Structure

CAS No. : 289480-64-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 240 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 240 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
25 mg USD 960 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Treprostinil sodium:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

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Description

Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.

IC50 & Target

DP/DP1 Receptor

0.6 nM (EC50)

IP Receptor

1.9 nM (EC50)

EP2 Receptor

6.2 nM (EC50)

EP3 Receptor

68.9 nM (EC50)

EP4 Receptor

181 nM (EC50)

EP1 Receptor

285 nM (EC50)

TP Receptor

919 nM (EC50)

EP2 Receptor

3.6 nM (Ki)

EP1 Receptor

212 nM (Ki)

EP4 Receptor

826 nM (Ki)

EP3 Receptor

2505 nM (Ki)

DP/DP1 Receptor

4.4 nM (Ki)

IP Receptor

32.1 nM (Ki)

FP Receptor

4680 nM (Ki)

In Vitro

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].

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

In Vivo

Inhaled treprostinil sodium, a prostacyclin analog, is the most recent agent to receive FDA approval for the treatment of a fatal orphan disease: pulmonary arterial hypertension (PAH)[2]. Treprostinil preserves the sinusoidal endothelial cell lining and reduces platelet deposition early post-transplantation compared to placebo. Hepatic tissue blood flow is significantly compromised in the placebo group, whereas treprostinil maintains blood flow similar to normal levels[3].Treprostinil treatment significantly increases the vessel-forming ability of endothelial colony forming cells combined with mesenchymal stem cells in Matrigel implanted in nude mice. Silencing VEGF-A gene in mesenchymal stem cells also blocks the pro-angiogenic effect of Treprostinil[4]. Treprostinil is most efficacious in raising intracellular cAMP levels in murine and human hematopoietic stem and progenitor cells[5]. Treatment with Treprostinil significantly reduces the recruitment of cells compared to normoxic mice. Treprostinil also reduces right ventricular systolic pressure and slightly reduces the vascular remodelling but fails to reverse the right ventricular hypertrophy[6].

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

Clinical Trial
Molecular Weight

412.49

Formula

C₂₃H₃₃NaO₅

CAS No.
SMILES

O=C(O[Na])COC1=C2C[[email protected]@]3([H])C[[email protected]@H](O)[[email protected]](CC[[email protected]@H](O)CCCCC)[[email protected]@]3([H])CC2=CC=C1

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 : ≥ 26 mg/mL (63.03 mM)

H2O : 16.67 mg/mL (40.41 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*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: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[5]

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].

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

Animal Administration
[3][6]

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].

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

References
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Keywords:

TreprostinilUT-15UT15UT 15Prostaglandin ReceptorInhibitorinhibitorinhibit

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Treprostinil sodium
Cat. No.:
HY-16504
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