Quinidine gluconic acid
Based on 24 publication(s) in Google Scholar
Quinidine gluconic acid is an orally active antiarrhythmic agent. Quinidine gluconic acid reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine gluconic acid exerts sustained block and open-channel block effects on IK(f). Quinidine gluconic acid alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine gluconic acid can be used in studies related to uterine sarcoma and seizures.
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- CAS No.: 7054-25-3
- Formule: C26H36N2O9
- Masse moléculaire:520.57
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Publications Citing Use of MedChemExpress (MCE) Quinidine gluconic acid
More- Nat Commun. 2024 Jun 19;15(1):5230. [Abstract]
- Adv Sci (Weinh). 2025 Aug 19:e05666. [Abstract]
- J Hazard Mater. 2021 Aug 15:416:125764. [Abstract]
- Environ Int. 2019 Jun:127:694-703. [Abstract]
- Anal Chem. 2025 Nov 18;97(45):25158-25167. [Abstract]
- J Med Chem. 2021 Mar 11;64(5):2725-2738. [Abstract]
- J Med Chem. 2020 Oct 8;63(19):11085-11099. [Abstract]
- Environ Pollut. 2024 Aug 15:355:124214. [Abstract]
- Pharmaceutics. 2025 Mar 26;17(4):423. [Abstract]
- J Agric Food Chem. 2022 Mar 2;70(8):2520-2528. [Abstract]
- Cell Mol Life Sci. 2025 Nov 25;82(1):419. [Abstract]
- RSC Adv. 2019 May 23;9(28):16136-16146. [Abstract]
- Front Pharmacol. 2020 Jul 31:11:1038. [Abstract]
- Cell Calcium. 2026 Mar:134:103125. [Abstract]
- Virol J. 2024 Aug 8;21(1):181. [Abstract]
- J Anim Sci. 2022 Apr 1;100(4):skac069. [Abstract]
- Andrology. 2025 Oct;13(7):1805-1815. [Abstract]
- AAPS J. 2021 Jun 28;23(4):91. [Abstract]
- Food Chem Toxicol. 2022 Nov:169:113431. [Abstract]
- Vet Microbiol. 2026 May:316:110992. [Abstract]
- Pharmacol Res Perspect. 2021 Oct;9(5):e00879. [Abstract]
- Pharmacol Res Perspect. 2020 Apr;8(2):e00575. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2022 Sep;47(5):639-652. [Abstract]
- Chemosphere. 2021 Dec:284:131347. [Abstract]
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Activité biologique
Description
IC50 & Target
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Caspase 3 |
In Vitro
Quinidine (10 μM; 24 h) gluconic acid potentiates Paclitaxel (HY-B0015)-induced cytotoxicity in P-gp-positive MES-SA/DX5 uterine sarcoma cells (reducing paclitaxel IC50 to 80.56 nM) but does not alter paclitaxel cytotoxicity in P-gp-negative MES-SA uterine sarcoma cells[1].
Quinidine (10 μM; 24 h) gluconic acid significantly increases the sub-G1 apoptotic portion in paclitaxel-treated P-gp-positive MES-SA/DX5 uterine sarcoma cells, enhancing paclitaxel-induced apoptosis[1].
Quinidine inhibits the in vitro metabolism of Debrisoquine in rat liver microsomes, with lower potency than observed in human liver microsomes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:P-gp-negative MES-SA uterine sarcoma cells, P-gp-positive MES-SA/DX5 uterine sarcoma cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Did not significantly alter the cytotoxicity of paclitaxel in MES-SA cells, with paclitaxel IC50 remaining comparable to paclitaxel alone (19 nM vs. 18 nM).
Strongly potentiated paclitaxel-induced cytotoxicity in MES-SA/DX5 cells, reducing the IC50 of paclitaxel from 13851 nM to 81 nM.
Showed no significant cytotoxicity up to 100 μM in either cell line.\nShowed concentration-dependent cytotoxicity with docetaxel against MES-SA cells.
Enhanced docetaxel-induced cytotoxicity in MES-SA/DX5 cells more potently than hydrocinchonine, alongside cinchonine.
Showed no significant cytotoxicity up to 100 μM in either cell line.
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Cell Line:P-gp-positive MES-SA/DX5 uterine sarcoma cells (paclitaxel-treated)
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly increased the sub-G1 apoptotic portion (G0 = 27.19) in paclitaxel-treated MES-SA/DX5 cells, whereas paclitaxel alone induced minimal sub-G1 accumulation (G0 = 0.05).
In Vivo
Quinidine (10-30 mg/kg; intraperitoneal injection; single administration) gluconic acid significantly elevates the threshold of pentylenetetrazol-induced tonic convulsions in male NMRI mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis (male, 175-225 g)[3]
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Dosage:80 mg/kg
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Administration:p.o.; single dose
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Result:Reduced urinary excretion of p-hydroxyamphetamine to 7.2% of vehicle-control levels in the 0-24 h collection period.
Reduced urinary excretion of p-hydroxyamphetamine to 24.1% of vehicle-control levels in the 24-48 h collection period.
Increased amphetamine excretion to 542% of control levels in the 24-48 h period.
Excreted an average of 0.40 μmol p-hydroxyamphetamine and 7.80 μmol amphetamine in the 0-24 h period.
Excreted an average of 3.60 μmol amphetamine and a significantly reduced amount of p-hydroxyamphetamine relative to controls in the 24-48 h period.
Achieved total combined excretion of amphetamine and p-hydroxyamphetamine over 48 h equal to 79.7% of the administered dose, which was not significantly different from control groups.
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Animal Model:NMRI (male, 5-6 weeks old, 25-30 g)[4]
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Dosage:10 mg/kg; 20 mg/kg; 30 mg/kg
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Administration:i.p.; single dose
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Result:Did not alter the pentylenetetrazole threshold dose for onset of myoclonic twitch.
Significantly increased the pentylenetetrazole threshold dose for onset of tonic hind limb extension compared to saline-treated controls (p < 0.05).
Chemical Information
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CAS No. 7054-25-3
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Masse moléculaire 520.57
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Formule C26H36N2O9
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SMILES
C=C[C@H]1C[N@](CC[C@H]1C2)[C@@]2([H])[C@@H](O)C3=CC=NC4=CC=C(OC)C=C34.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (24)
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Journal Impact Factor
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Most Recent
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Nat Commun
Small molecule in situ resin capture provides a compound first approach to natural product discovery. [Abstract]2024 Jun 19;15(1):5230. PMID: 38898025 -
Adv Sci (Weinh)
LPS-Induced Mitochondrial Damage via SLC41A1-Mediated Magnesium Ion Efflux Leads to the Pyroptosis of Dental Stem Cells. [Abstract]2025 Aug 19:e05666. PMID: 40831212
Quinidine gluconic acid purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 19:e05666. [Abstract]
Quinidine rescued [Mg2⁺]i levels in LPS‐treated or TRPM7‐silenced DPSCs and SCAP.
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J Hazard Mater
Stereostructure-activity mechanism of cyproconazole by cytochrome P450 in rat liver microsomes: A combined experimental and computational study. [Abstract]2021 Aug 15:416:125764. PMID: 33827004
Quinidine gluconic acid purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2021 Aug 15:416:125764. [Abstract]
Effects of CYP enzymes inhibitors on metabolic rates of cyproconazole stereoisomers in the in vitro incubation mixtures with RLMs. The asterisks (*) indicates the significant difference in metabolic rates under inhibition compared to the control.
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Environ Int
2019 Jun:127:694-703. PMID: 30991225
Quinidine gluconic acid purchased from MedChemExpress. Usage Cited in: Environ Int. 2019 Jun:127:694-703. [Abstract]
CYP2D6 has contributed in the enantioselectivity of IFP and ICPO because the EF value of the KND-supplemented group follows a doseeffect relationship and the difference in the EF values was over 10% relative to the DMSO control group.
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Anal Chem
A Computational Integration Strategy Driven by Chemical Similarity Uncovers Comprehensive Metabolic Profiles of Small Bioactive Peptides via UHPLC-HRMS for Doping Control. [Abstract]2025 Nov 18;97(45):25158-25167. PMID: 41202118 -
J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
J Med Chem
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. [Abstract]2020 Oct 8;63(19):11085-11099. PMID: 32886512 -
Environ Pollut
Assessing environmental and human health risks: Insight from the enantioselective metabolism and degradation of fenpropidin. [Abstract]2024 Aug 15:355:124214. PMID: 38801883 -
Pharmaceutics
Plasma Protein Binding, Biostability, Metabolite Profiling, and CYP450 Phenotype of TPB15 Across Different Species: A Novel Smoothened Inhibitor for TNBC Therapy. [Abstract]2025 Mar 26;17(4):423. PMID: 40284418 -
J Agric Food Chem
Enantioselective Metabolic Mechanism and Metabolism Pathway of Pydiflumetofen in Rat Liver Microsomes: In Vitro and In Silico Study. [Abstract]2022 Mar 2;70(8):2520-2528. PMID: 35184556 -
Cell Mol Life Sci
2025 Nov 25;82(1):419. PMID: 41288707 -
RSC Adv
Identification of key transporters mediating uptake of aconitum alkaloids into the liver and kidneys and the potential mechanism of detoxification by active ingredients of liquorice. [Abstract]2019 May 23;9(28):16136-16146. PMID: 35521419 -
Front Pharmacol
Eye Drops of Metformin Prevents Fibrosis After Glaucoma Filtration Surgery in Rats via Activating AMPK/Nrf2 Signaling Pathway. [Abstract]2020 Jul 31:11:1038. PMID: 32903813
Quinidine gluconic acid purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Jul 31:11:1038. [Abstract]
Cell cycle relative proteins/genes (CyclinD1, CDK4, P21 and P27) level were assessed in HConFs after Quinidine treatment by western blot.
Quinidine gluconic acid purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Jul 31:11:1038. [Abstract]
Cell cycle relative proteins/genes (CyclinD1, CDK4, P21 and P27) level were assessed in HConFs after Atropine/Quinidine treatment by qRT-PCR.
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Cell Calcium
MONNA alleviates MPTP-induced Parkinson's disease in zebrafish by activating TFEB dependently on ER Calcium. [Abstract]2026 Mar:134:103125. PMID: 41637953 -
Virol J
2024 Aug 8;21(1):181. PMID: 39118175 -
J Anim Sci
2022 Apr 1;100(4):skac069. PMID: 35247050 -
Andrology
Pharmacological inhibition of KSper impairs flagellar pH homeostasis of human spermatozoa. [Abstract]2025 Oct;13(7):1805-1815. PMID: 39498893 -
AAPS J
Cannabinoid Interactions with Cytochrome P450 Drug Metabolism: a Full-Spectrum Characterization. [Abstract]2021 Jun 28;23(4):91. PMID: 34181150 -
Food Chem Toxicol
The "steric-like" inhibitory effect and mechanism of doxycycline on florfenicol metabolism: Interaction risk. [Abstract]2022 Nov:169:113431. PMID: 36116547 -
Vet Microbiol
The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]2026 May:316:110992. PMID: 41865607 -
Pharmacol Res Perspect
Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [Abstract]2021 Oct;9(5):e00879. PMID: 34628723 -
Pharmacol Res Perspect
Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats. [Abstract]2020 Apr;8(2):e00575. PMID: 32266794 -
Eur J Drug Metab Pharmacokinet
Evaluation of an Ussing Chamber System Equipped with Rat Intestinal Tissues to Predict Intestinal Absorption and Metabolism in Humans. [Abstract]2022 Sep;47(5):639-652. PMID: 35733077 -
Chemosphere
A proposed "steric-like effect" for the slowdown of enrofloxacin antibiotic metabolism by ciprofloxacin, and its mechanism. [Abstract]2021 Dec:284:131347. PMID: 34323809
Pureté et documentation
Références
[1]. Lee SY, et al. Hydrocinchonine, cinchonine, and quinidine potentiate paclitaxel-induced cytotoxicity and apoptosis via multidrug resistance reversal in MES-SA/DX5 uterine sarcoma cells. Environ Toxicol. 2011 Aug;26(4):424-31. [Content Brief]
[2]. Kehl SJ, et al. Quinidine-induced inhibition of the fast transient outward K+ current in rat melanotrophs. Br J Pharmacol. 1991;103(3):1807-1813. [Content Brief]
[3]. Moody DE, et al. Quinidine inhibits in vivo metabolism of amphetamine in rats: impact upon correlation between GC/MS and immunoassay findings in rat urine. J Anal Toxicol. 1990;14(5):311-317. [Content Brief]
[4]. Jamali H, et al. Effect of dextromethorphan/quinidine on pentylenetetrazole- induced clonic and tonic seizure thresholds in mice. Neurosci Lett. 2020;729:134988. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Quinidine gluconic acid Related Classifications
HY-B1751F Related Classifications
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