[CAS NO. 312946-37-5] LDN-27219
PRODUCTS SPECIFICATIONS [312946-37-5]
DESCRIPTION [312946-37-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 408.50 |
| Molecular Formula | C20H16N4O2S2 |
| SMILES | O=C1N(C2=CC=CC=C2)C(SCC(NN)=O)=NC3=C1C(C4=CC=CC=C4)=CS3 |
Summary
LDN-27219 is a reversible, slow-binding inhibitor of TGase . LDN-27219 inhibits human TGase with an IC 50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease [1] [2] .
IC50 & Target
IC50: 0.6 μM (hTGase) [1]
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LDN-27219 (0.1-2 mg/kg; i.v. once) affects vivo arterial pressure and shows larger effects on older rats [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 12 to 14-week-old male Wistar rats [2] |
| Dosage: | 0.1, 1 and 2 mg/kg |
| Administration: | Intravenous injection; 0.1, 1 and 2 mg/kg once |
| Result: | Dose-dependently decreased mean arterial pressure of mice. |
| Animal Model: | 12 to 14- and 35 to 40-week-old male Wistar rats |
| Dosage: | 0.1, 1 and 2 mg/kg |
| Administration: | Intravenous injection; 0.1, 1 and 2 mg/kg once |
| Result: | Decreased mean arterial pressure in old group more significant than young group. |
Appearance
Solid
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
DMSO : ≥ 125 mg/mL ( 306.00 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4480 mL | 12.2399 mL | 24.4798 mL |
| 5 mM | 0.4896 mL | 2.4480 mL | 4.8960 mL |
| 10 mM | 0.2448 mL | 1.2240 mL | 2.4480 mL |
References
- [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.
- [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.
