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Quinine HCl Dihydrate Potassium Channel inhibitor

Cat.No.S2502

Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria.
Quinine HCl Dihydrate Potassium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 396.91

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 396.91 Formula

C20H24N2O2.HCl.2H2O

Storage (From the date of receipt)
CAS No. 6119-47-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC2=C(C=CN=C2C=C1)C(C3CC4CCN3CC4C=C)O.O.O.Cl

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (199.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 79 mg/mL

Water : 43 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
Potassium channel [1]
In vitro
Quinine blocks Cx36 and Cx50 junctional currents in a reversible and concentration-dependent manner with half maximal blocking concentrations of 32 mM and 73 mM, respectively. Quinine induces slow transitions between open and fully closed states that decreased open probability of the channel. Quinine thus offers a potentially useful method to block certain types of gap junction channels, including those between neurons that are formed by Cx36. [1] Quinine, a K+ channel blocker, prevents formation of tumor necrosis factor (TNF) as well as the subsequent hepatic DNA fragmentation and liver enzyme leakage. [2] Quinine elicits Fos-like immunoreactivity (FLI) concentrated in the medial third of the nucleus; acid elicited more broadly distributed FLI concentrated farther laterally. [3] Quinine has a relatively weak effect on doxorubicin accumulation but was able to completely restore doxorubicin sensitivity in the resistant cells. Quinine also modifies the intracellular tolerance to doxorubicin, which suggests that it is able to modify drug distribution within the cells. [4] Quinine primarily blocks the whole cell potassium currents (IK) in a voltage-dependent manner. Quinine also reduces the size of sodium currents (INa) in a use-dependent manner, while leaving calcium currents (ICa) relatively unaffected. [5]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/7628869/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9582223/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04873011 Unknown status
Obesity
Universitaire Ziekenhuizen KU Leuven
October 29 2020 Phase 1
NCT02817919 Completed
Malaria
African Collaborating Centre for Pharmacovigilance|Kintampo Health Research Centre Ghana|University of Health and Allied Sciences
May 2016 --
NCT02598713 Recruiting
Pneumonia|Aspiration
Massachusetts General Hospital
December 2015 Phase 1

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