LDN-27219
Based on 1 publication(s) in Google Scholar
LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease.
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- Pureza: 99.76%
- No. CAS: 312946-37-5
- Fòrmula: C20H16N4O2S2
- Peso molecular:408.50
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) LDN-27219
More
Actividad biológica
IC50: 0.6 μM (hTGase)[1]
LDN-27219 (30 μM; 12 min) promotes the closed conformation of TGase 2 to activates calcium-activated potassium channels in smooth muscle cells[2]. LDN-27219 (30 μM; 20-25 min) increases the response to acetylcholine in phenylephrine-contracted human subcutaneous arteries[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:12 to 14-week-old male Wistar rats[2]
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Dosage:0.1, 1 and 2 mg/kg
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Administration:Intravenous injection; 0.1, 1 and 2 mg/kg once
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Result:Dose-dependently decreased mean arterial pressure of mice.
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Animal Model:12 to 14- and 35 to 40-week-old male Wistar rats
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Dosage:0.1, 1 and 2 mg/kg
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Administration:Intravenous injection; 0.1, 1 and 2 mg/kg once
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Result:Decreased mean arterial pressure in old group more significant than young group.
Chemical Information
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No. CAS 312946-37-5
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Appearance Solid
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Peso molecular 408.50
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Fòrmula C20H16N4O2S2
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Color White to off-white
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SMILES
O=C1N(C2=CC=CC=C2)C(SCC(NN)=O)=NC3=C1C(C4=CC=CC=C4)=CS3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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JCI Insight
RhoA vesicle trafficking-mediated transglutaminase 2 membrane translocation promotes IgA1 mesangial deposition in IgA nephropathy. [Abstract]2023 Oct 9;8(19):e160374. PMID: 37811653
Solvente y solubilidad
DMSO : 100 mg/mL (244.80 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.12 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.12 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Case A, et al. Kinetic analysis of the interaction of tissue transglutaminase with a nonpeptidic slow-binding inhibitor. Biochemistry. 2007 Jan 30;46(4):1106-15. [Content Brief]
[2]. Pinilla E, et al. Transglutaminase 2 Inhibitor LDN 27219 Age-Dependently Lowers Blood Pressure and Improves Endothelium-Dependent Vasodilation in Resistance Arteries. Hypertension. 2021 Jan;77(1):216-227. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4480 mL | 12.2399 mL | 24.4798 mL | 61.1995 mL |
| 5 mM | 0.4896 mL | 2.4480 mL | 4.8960 mL | 12.2399 mL | |
| 10 mM | 0.2448 mL | 1.2240 mL | 2.4480 mL | 6.1200 mL | |
| 15 mM | 0.1632 mL | 0.8160 mL | 1.6320 mL | 4.0800 mL | |
| 20 mM | 0.1224 mL | 0.6120 mL | 1.2240 mL | 3.0600 mL | |
| 25 mM | 0.0979 mL | 0.4896 mL | 0.9792 mL | 2.4480 mL | |
| 30 mM | 0.0816 mL | 0.4080 mL | 0.8160 mL | 2.0400 mL | |
| 40 mM | 0.0612 mL | 0.3060 mL | 0.6120 mL | 1.5300 mL | |
| 50 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2240 mL | |
| 60 mM | 0.0408 mL | 0.2040 mL | 0.4080 mL | 1.0200 mL | |
| 80 mM | 0.0306 mL | 0.1530 mL | 0.3060 mL | 0.7650 mL | |
| 100 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6120 mL |
LDN-27219 Related Classifications
HY-16693 Related Classifications
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