2. GPCR/G Protein
  3. Vasopressin Receptor
  4. Terlipressin

Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Terlipressin diacetate) that retains the same biological activity.

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

Terlipressin Chemical Structure

Terlipressin Chemical Structure

CAS No. : 14636-12-5

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Other Forms of Terlipressin:

Terlipressin Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Terlipressin

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V1a Receptor  V1b Receptor  V2 Receptor 

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research[1][2][3][4][5].

IC50 & Target

Vasopressin V1 receptor[1]
In Vitro

Terlipressin (25 nM; 24-72 hours; IEC-6 cells) treatment significantly improves cell viability, proliferation and apoptosis in IEC-6 cells[1].
Terlipressin inhibits the secretion of TNF-α and 15-F2t-isoprostane from IEC-6 cells following oxygen and glucose deprivation/re-oxygenation (OGD/R). Terlipressin administration following OGD attenuates OGD/R-induced cell damage via the PI3K signaling pathway[1].

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

Terlipressin Related Antibodies

Cell Proliferation Assay[1]

Cell Line: IEC-6 cells induced by oxygen and glucose deprivation/re-oxygenation (OGD/R)
Concentration: 25 nM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Significantly increased the proliferation of IEC-6 cells.
In Vivo

Using a mouse nonlethal hepatic ischemia-reperfusion (IR) model, Terlipressin administration significantly ameliorates IR-induced liver apoptosis, necrosis and inflammation[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

1227.37

Formula

C52H74N16O15S2
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Gly-Gly-Gly-Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Lys-Gly-NH2 (Disulfide bridge: Cys4-Cys9)
Sequence Shortening

GGGCYFQNCPKG-NH2 (Disulfide bridge: Cys4-Cys9)
SMILES

O=C([C@H](CSSC[C@@H](C(N[C@H](C1=O)CC2=CC=C(O)C=C2)=O)NC(CNC(CNC(CN)=O)=O)=O)NC([C@@H](NC([C@@H](NC([C@](N1)([H])CC3=CC=CC=C3)=O)CCC(N)=O)=O)CC(N)=O)=O)N(CCC4)[C@@H]4C(N[C@@H](CCCCN)C(NCC(N)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (81.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8148 mL 4.0738 mL 8.1475 mL
5 mM 0.1630 mL 0.8148 mL 1.6295 mL
View the Complete Stock Solution Preparation Table

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (2.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (2.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8148 mL 4.0738 mL 8.1475 mL 20.3688 mL
5 mM 0.1630 mL 0.8148 mL 1.6295 mL 4.0738 mL
10 mM 0.0815 mL 0.4074 mL 0.8148 mL 2.0369 mL
15 mM 0.0543 mL 0.2716 mL 0.5432 mL 1.3579 mL
20 mM 0.0407 mL 0.2037 mL 0.4074 mL 1.0184 mL
25 mM 0.0326 mL 0.1630 mL 0.3259 mL 0.8148 mL
30 mM 0.0272 mL 0.1358 mL 0.2716 mL 0.6790 mL
40 mM 0.0204 mL 0.1018 mL 0.2037 mL 0.5092 mL
50 mM 0.0163 mL 0.0815 mL 0.1630 mL 0.4074 mL
60 mM 0.0136 mL 0.0679 mL 0.1358 mL 0.3395 mL
80 mM 0.0102 mL 0.0509 mL 0.1018 mL 0.2546 mL
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Terlipressin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Terlipressin14636-12-5Vasopressin ReceptorVasoconstrictorvasopressinvasoconstrictionV1-receptorsacutevaricealbleedinghepatorenalanti-inflammatoryanti-oxidativeInhibitorinhibitorinhibit

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