Ingliforib是一种glycogenphosphorylase抑制剂，对肝脏、肌肉和大脑glycogenphosphorylase的IC50值分别为52，352和150nM，具有心脏保护的作用。
货号:ajcx12850
CAS:186392-65-4
分子式:C23H24ClN3O5
分子量：457.91
溶解度:DMSO : 130 mg/mL (283.90 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Ingliforib is a glycogen phosphorylase inhibitor, with IC50s of 52, 352 and 150 nM for liver, muscle and brain glycogen phosphorylase, and has cardioprotective activity.

Ingliforib is a glycogen phosphorylase inhibitor, and inhibits the myocardial GP isoforms (muscle and brain) with IC50s of 352 and 150 nM, respectively, also a potent inhibitor of the liver isoform (IC50 of 52 nM). Ingliforib (0.1, 1, 10 μM) dose-dependently reduces infarct size in the isolated rabbit hearts[1].

Ingliforib (15 mg/kg) potently reduces infarct size by 52%, and decreases plasma glucose and lactate concentrations in openchest anesthetized rabbits. Ingliforib (15 mg/kg) also inhibits myocardial glycogen phosphorylase a (GPa) and total glycogen phosphorylase (GP) activity in anesthetized rabbits[1].

[1]. Tracey WR, et al. Cardioprotective effects of ingliforib, a novel glycogen phosphorylase inhibitor. Am J Physiol Heart Circ Physiol. 2004 Mar;286(3):H1177-84.

Protocol:

Animal experiment:

Rabbits[1]Male New Zealand White rabbits (3 to 4 kg) are used in the assay. At least 1 h after surgery, when arterial pressure, heart rate (HR), and rate-pressure product (RPP) have stabilized for at least 30 min (baseline), the rabbits receive a bolus of either 15.4 mg/kg of Ingliforib or vehicle (administered in 15 s), followed by a constant infusion of 23.1 mg/kg/h Ingliforib or vehicle at the same dose volume for a total of 3.5 h.

参考文献: [1]. Tracey WR, et al. Cardioprotective effects of ingliforib, a novel glycogen phosphorylase inhibitor. Am J Physiol Heart Circ Physiol. 2004 Mar;286(3):H1177-84.