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Ingliforib (CP 368296) (Synonyms: CP 368296; GPi 296)

カタログ番号GC32658

Ingliforib (CP 368296) (CP 368296) はグリコーゲン ホスホリラーゼ阻害剤であり、肝臓、筋肉、脳のグリコーゲン ホスホリラーゼに対する IC50 は 52、352、150 nM で、心保護作用があります。

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Ingliforib (CP 368296) 化学構造

Cas No.: 186392-65-4

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$181.00
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1mg
$90.00
在庫あり
5mg
$180.00
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10mg
$288.00
在庫あり
25mg
$518.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of Ingliforib (CP 368296)

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 of Ingliforib (CP 368296)

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.

References:

[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.

Chemical Properties of Ingliforib (CP 368296)

Cas No. 186392-65-4 SDF
同義語 CP 368296; GPi 296
Canonical SMILES O=C(C(N1)=CC2=C1C=CC(Cl)=C2)N[C@@H](CC3=CC=CC=C3)[C@@H](O)C(N4C[C@@H](O)[C@@H](O)C4)=O
Formula C23H24ClN3O5 M.Wt 457.91
溶解度 DMSO : 130 mg/mL (283.90 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Ingliforib (CP 368296)

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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
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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