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Ingliforib (Synonyms: CP 368296; GPi 296)

Cat. No.: HY-19396
Handling Instructions

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.

For research use only. We do not sell to patients.

Ingliforib Chemical Structure

Ingliforib Chemical Structure

CAS No. : 186392-65-4

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

IC50: 52 nM (liver Glycogen phosphorylase), 352 nM (Muscle Glycogen phosphorylase), 150 nM (Barin Glycogen phosphorylase)[1]

In Vitro

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].

In Vivo

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1838 mL 10.9192 mL 21.8384 mL
5 mM 0.4368 mL 2.1838 mL 4.3677 mL
10 mM 0.2184 mL 1.0919 mL 2.1838 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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. Sixty minutes after starting the infusion, regional ischemia is produced by tightening the coronary artery snare for 30 min. The snare is released, and the heart is reperfused for an additional 120 min. Myocardial ischemia is confirmed by regional cyanosis and ST segment elevation; reperfusion is confirmed by reactive hyperemia and rapid decline of the ST elevation. At the end of either the ischemic period or reperfusion period, each rabbit is euthanized with an intravenous overdose of pentobarbital sodium (100 mg/kg). The heart is quickly excised and prepared for measurement of glycogen phosphorylase activity and glycogen content, or mounted and perfused with physiological saline at 38.5°C for subsequent determination of infarct size[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

457.91

Formula

C₂₃H₂₄ClN₃O₅

CAS No.

186392-65-4

SMILES

O=C(C(N1)=CC2=C1C=CC(Cl)=C2)N[[email protected]@H](CC3=CC=CC=C3)[[email protected]@H](O)C(N4C[[email protected]@H](O)[[email protected]@H](O)C4)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Ingliforib
Cat. No.:
HY-19396
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Ingliforib

Cat. No.: HY-19396