LDN-27219

LDN-27219 is an inhibitor of tissue transglutaminase 2 (TG2, IC50 = 0.25 µM) that promotes its closed conformation. LDN-27219 induces relaxation of isolated rat mesenteric arteries precontracted with the thromboxane receptor agonist U-46619 (Cay-16450) in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase (NOS) inhibitor Nomega-nitro-L-arginine. 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.Formal Name: 2-[(3,4-dihydro-4-oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)thio]-acetic acid, hydrazide (ACl). CAS Number: 312946-37-5. Molecular Formula: C20H16N4O2S2. Formula Weight: 408.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 100 mM. SMILES: O=C(CSC1=NC2=C(C(N1C3=CC=CC=C3)=O)C(C4=CC=CC=C4)=CS2)NN. InChi Code: 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). InChi Key: WLBUICQBNZXIDJ-UHFFFAOYSA-N.