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100mg | ||
250mg | ||
500mg |
ln Vitro |
Rabbit aldehyde oxidase is inhibited by quinacrine, with IC50 values of 3.3 μM and 10 μM, respectively[2]. Voltage sodium channels are inhibited by quinacrine (IC50: 3.3 μM)[3]. Quinacrine (0–20 μM, 24 h) stimulates and suppresses the development of SGC-7901 cells [7]. Quinacrine (100 μM) is also a PLA2 Bragg channel.
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ln Vivo |
Triglycerides can cause acute renal injury, however quinacrine (3–30 mg/kg, intraperitoneal injection, once day for three days) can prevent this damage [5]. Quinacrine (intraperitoneal injection, 2.5–10 mg/kg, once day for three days in a row).
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Cell Assay |
Cell viability assay [7]
Cell Types: SGC-7901 Cell Tested Concentrations: 0, 5, 10, 15, 20 μM Incubation Duration: 24 h Experimental Results: Inhibited cell growth, IC50 value was 16.18 μM. |
Animal Protocol |
Animal/Disease Models: Acute kidney injury rat model [5]
Doses: 3-30 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Attenuated glycerol-induced structural and renal toxicity. Changes in kidney function. |
References |
[1]. Vogtherr M, et al. Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein. J Med Chem. 2003 Aug 14;46(17):3563-4.
[2]. Pryde DC, et al. Aldehyde oxidase: an enzyme of emerging importance in drug discovery. J Med Chem. 2010 Dec 23;53(24):8441-60. [3]. McNeal ET, et al. [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. J Med Chem. 1985 Mar;28(3):381-8. [4]. Caro AA,et al. Role of phospholipase A2 activation and calcium in CYP2E1-dependent toxicity in HepG2 cells. J Biol Chem. 2003 Sep 5;278(36):33866-77. [5]. Al Asmari AK, et al. Protective effect of quinacrine against glycerol-induced acute kidney injury in rats. BMC Nephrol. 2017 Jan 28;18(1):41. [6]. al Khader A, et al. Quinacrine attenuates cyclosporine-induced nephrotoxicity in rats. Transplantation. 1996 Aug 27;62(4):427-35. [7]. Wu X, et al. Quinacrine Inhibits Cell Growth and Induces Apoptosis in Human Gastric Cancer Cell Line SGC-7901. Curr Ther Res Clin Exp. 2012 Feb;73(1-2):52-64. |
Molecular Formula |
C23H30CLN30
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Molecular Weight |
399.21
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Exact Mass |
399.2077
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CAS # |
83-89-6
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Related CAS # |
Quinacrine dihydrochloride;69-05-6;l-Atabrine dihydrochloride;56100-42-6;d-Atabrine dihydrochloride;56100-41-5;Quinacrine hydrochloride hydrate;6151-30-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CCN(CC)CCCC(C)N=C1C2=C(C=C(C=C2)Cl)NC3=C1C=C(C=C3)OC
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Synonyms |
Haffkinine; Erion
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5049 mL | 12.5247 mL | 25.0495 mL | |
5 mM | 0.5010 mL | 2.5049 mL | 5.0099 mL | |
10 mM | 0.2505 mL | 1.2525 mL | 2.5049 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.