| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.6 μM (hTGase) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | LDN-27219 (0.1-2 mg/kg; i.v. once) affects vivo arterial pressure and shows larger effects on older rats[2]. Animal Model: | ||||||||||||
| Name | LDN-27219 | ||||||||||||
| CAS | 312946-37-5 | ||||||||||||
| Formula | C20H16N4O2S2 | ||||||||||||
| Molar Mass | 408.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| 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. |
LDN-27219
CAS: 312946-37-5 F: C20H16N4O2S2 W: 408.50
LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.