1. GPCR/G Protein
  2. Vasopressin Receptor
  3. 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.

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Terlipressin

Terlipressin 構造式

CAS 番号 : 14636-12-5

容量 価格(税別) 在庫状況
1 mg $25 見積もりとリードタイムを求めるのご確認
5 mg $50 見積もりとリードタイムを求めるのご確認

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

Other 在庫あり Forms of Terlipressin:

Other Forms of Terlipressin:

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Vasopressin Receptor アイソフォーム固有の製品をすべて表示:

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製品説明

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]

体外実験

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.

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.
体内実験

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.

分子量

1227.37

分子式

C52H74N16O15S2

CAS 番号
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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

溶剤 & 溶解度
体外: 

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
10 mM 0.0815 mL 0.4074 mL 0.8148 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)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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.
純度とドキュメンテーション
参考文献

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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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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.

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Inquiry Information

製品名:
Terlipressin
製品番号:
HY-12554
数量:
MCE 日本正規代理店: