产品描述:
LDN-27219 is an inhibitor of tissue transglutaminase 2 (TG2; IC50 = 0.25 µM) that promotes its closed conformation.{58277,58278} LDN-27219 induces relaxation of isolated rat mesenteric arteries precontracted with the thromboxane receptor agonist U-46619 (Item No. 16450) in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase (NOS) inhibitor Nω-nitro-L-arginine.{58279} It also activates large-conductance calcium-activated potassium (KCa1.1/BKCa) channels in isolated rat smooth muscle cells when used at a concentration of 30 µM. LDN-27219 (0.1, 1, and 2 mg/kg, i.v.) decreases blood pressure in anesthetized rats.