nicorandil

Nicorandil (SG-75) 是一种有效的钾通道激活剂，靶向血管核苷二磷酸依赖性 K+通道和心脏 ATP 敏感 K+通道 (KATP)。Nicorandil 是一种烟酰胺酯，具有血管舒张和心脏保护作用，并具有治疗心绞痛和缺血性心脏病的潜力。

Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B Kir6.2 over the SUR2A Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 = 4.4 µM). It decreases mean blood pressure, coronary resistance, and heart rate, as well as increases coronary sinus outflow, in dogs when administered intravenously at a dose of 1 mg kg. Nicorandil increases survival and decreases infarct size in a rabbit model of myocardial ischemia-reperfusion injury induced by left coronary artery occlusion. Formulations containing nicorandil have been used in the treatment of angina pectoris.

Nicorandil N-oxide, a metabolite of nicorandil, functions as an activator of the ATP-sensitive potassium channel Kir6.2 (SUR2B/Kir6.2) and is associated with the sulfonylurea receptor 2B (SUR2B), while also serving as a nitric oxide donor.

Quizartinib, also know as AC220 and AC010220, is an orally available FLT3 STK1 inhibitor with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3 STK1), colony-stimulating factor 1 receptor (CSF1R FMS), stem cell factor receptor (SCFR KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis. Mutations in FLT3, resulting in constitutive activation, are the most frequent genetic alterations in acute myeloid leukemia (AML) and occur in approximately one-third of AML cases.

SG 209是nicorandil的类似物，可作为K+通道开放剂和无硝酸盐的冠状血管扩张剂。