Terlipressin diacetate
Based on 2 publication(s) in Google Scholar
Terlipressin diacetate is a vasopressin analogue with potent vasoactive properties. Terlipressin diacetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin diacetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin diacetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.17%
- CAS No.: 1884420-36-3
- 화학식: C56H82N16O19S2
- 분자량:1347.48
-
보관:
Stored under nitrogen, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Terlipressin diacetate
MoreAll Vasopressin Receptor Isoforms
More
Biological Activity
제품 설명
IC50 & Target
|
V1b Receptor |
In Vitro
Terlipressin diacetate (25 nM; 24-72 hours; IEC-6 cells) treatment significantly improves cell viability, proliferation and apoptosis in IEC-6 cells[1].
Terlipressin diacetate inhibits the secretion of TNF-α and 15-F2t-isoprostane from IEC-6 cells following oxygen and glucose deprivation/re-oxygenation (OGD/R). Terlipressin diacetate 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. Further protocols information, click here.
-
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
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1884420-36-3
-
Appearance Solid
-
분자량 1347.48
-
화학식 C56H82N16O19S2
-
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)
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Stored under nitrogen, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Sci Rep
An investigation of reconstituted terlipressin infusion stability for use in hepatorenal syndrome. [Abstract]2020 Dec 3;10(1):21037. PMID: 33273555 -
Anal Bioanal Chem
Understanding the chemical stability of peptidomimetic therapeutics using high-resolution mass spectrometry: a study of terlipressin and its degradation products. [Abstract]2025 Aug;417(19):4311-4329. PMID: 40518483
용액&용해도
In Vitro:
H2O : 100 mg/mL (74.21 mM; Need ultrasonic)
DMSO : 50 mg/mL (37.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.86 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (74.21 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
-
Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
순도&문서
-
Data Sheet (282 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
References
[1]. Zi-Meng Liu, et al. Terlipressin Protects Intestinal Epithelial Cells Against Oxygen-Glucose Deprivation/Re-Oxygenation Injury via the Phosphatidylinositol 3-kinase Pathway. Exp Ther Med. 2017 Jul;14(1):260-266. [Content Brief]
[2]. Yeun Tarl Fresner Ng Jao, et al. Refractory Torsade De Pointes Induced by Terlipressin (Glypressin). Int J Cardiol. 2016 Nov 1;222:135-140. [Content Brief]
[3]. Xiqiang Liu, et al. Signaling Through Hepatocyte Vasopressin Receptor 1 Protects Mouse Liver From Ischemia-Reperfusion Injury. Oncotarget. 2016 Oct 25;7(43):69276-69290. [Content Brief]
[4]. Xinmiao Zhou, et al. Terlipressin for the Treatment of Acute Variceal Bleeding: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Medicine (Baltimore). 2018 Nov;97(48):e13437. [Content Brief]
[5]. Alastair O'Brien, et al. Terlipressin for Norepinephrine-Resistant Septic Shock. Lancet. 2002 Apr 6;359(9313):1209-10. [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 (stored under nitrogen, away from moisture). 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 / H2O | 1 mM | 0.7421 mL | 3.7106 mL | 7.4213 mL | 18.5532 mL |
| 5 mM | 0.1484 mL | 0.7421 mL | 1.4843 mL | 3.7106 mL | |
| 10 mM | 0.0742 mL | 0.3711 mL | 0.7421 mL | 1.8553 mL | |
| 15 mM | 0.0495 mL | 0.2474 mL | 0.4948 mL | 1.2369 mL | |
| 20 mM | 0.0371 mL | 0.1855 mL | 0.3711 mL | 0.9277 mL | |
| 25 mM | 0.0297 mL | 0.1484 mL | 0.2969 mL | 0.7421 mL | |
| 30 mM | 0.0247 mL | 0.1237 mL | 0.2474 mL | 0.6184 mL | |
| H2O | 40 mM | 0.0186 mL | 0.0928 mL | 0.1855 mL | 0.4638 mL |
| 50 mM | 0.0148 mL | 0.0742 mL | 0.1484 mL | 0.3711 mL | |
| 60 mM | 0.0124 mL | 0.0618 mL | 0.1237 mL | 0.3092 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.