For research use only. Not for therapeutic Use.
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[1][2].
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].
LDN-27219 (0.1-2 mg/kg; i.v. once) affects vivo arterial pressure and shows larger effects on older rats[2].
| Catalog Number | I003106 |
| CAS Number | 312946-37-5 |
| Synonyms | 2-(4-oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)sulfanylacetohydrazide |
| Molecular Formula | C20H16N4O2S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H16N4O2S2/c21-23-16(25)12-28-20-22-18-17(15(11-27-18)13-7-3-1-4-8-13)19(26)24(20)14-9-5-2-6-10-14/h1-11H,12,21H2,(H,23,25) |
| InChIKey | WLBUICQBNZXIDJ-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)C2=CSC3=C2C(=O)N(C(=N3)SCC(=O)NN)C4=CC=CC=C4 |
| Reference | [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. |
