| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
Apoptosis is induced and HCC cells become more sensitive to sorafenib (2 μM) when exposed to maprotiline (10 μM) [2]. In HepG2 and Huh7 cells, maprotiline (0, 10 or 20 μM, 72 hours) suppresses the phosphorylation of SREBP2 by acting on the ERK pathway [2]. In HCC cells, maprotiline may regulate cholesterol production by targeting CRABP1 [2]. Test for cell invasion [2]
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|---|---|
| ln Vivo |
Neuropathic pain can be effectively reduced by combining the synthetic cannabinoid WIN 55,212-2 with maprotiline (3, 10, or 30 mg/kg; i.p.) [1]. Low toxicity to organs, immune system, and hematopoiesis is observed with maprotiline (0, 20, or 40 mg/kg); intraperitoneally; twice weekly; 3 weeks [2]. By blocking cholesterol production and interacting with CRABP1, maprotiline (0, 20, or 40 mg/kg; i.p.; twice weekly; 3 weeks) suppresses the development and metastasis of HCC cells [2].
|
| Cell Assay |
Cell invasion test [2]
Cell Types: human liver cancer cell lines Huh7 and HepG2 Tested Concentrations: 0, 10, 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of liver cancer cell migration and epithelial-mesenchymal transition (EMT). Cell viability assay [2] Cell Types: human liver cancer cell lines Huh7 and HepG2 Tested Concentrations: 0, 10, 20 μM Incubation Duration: 0, 24, 48, 72, 96, 120 hrs (hours) Experimental Results: Triggered cell apoptosis and inhibited cell viability Huh7 and HepG2 cells in a dose- and time-dependent manner. Western Blot Analysis [2] Cell Types: Human liver cancer cell lines Huh7 and HepG2 Tested Concentrations: 0, 10, 20 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of cholesterol biosynthesis in liver cancer cells. |
| Animal Protocol |
Animal/Disease Models: Male Balb-c mouse (25-30 g) [1]
Doses: 3, 10, 30 mg/kg Route of Administration: intraperitoneal (ip) injection; assessment 30 minutes after treatment Experimental Results: Pain-related behaviors in neuropathic mice weaken. Animal/Disease Models: Nude mice (BALB/C nu/nu, 4-6 weeks old, female) [2] Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a week; 3-week Experimental Results: diminished serum and tumor cholesterol levels, inhibited the growth of Huh7-derived tumor xenografts without obvious toxic effects. |
| References |
[1]. Gunduz O, et al. Analysis of the anti-allodynic effects of combination of a synthetic cannabinoid and a selective noradrenaline re-uptake inhibitor in nerve injury-induced neuropathic mice. Eur J Pain. 2016 Mar. 20(3):465-71.
[2]. Zheng C, et al. Maprotiline Suppresses Cholesterol Biosynthesis and Hepatocellular Carcinoma Progression Through Direct Targeting of CRABP1. Front Pharmacol. 2021 May 20. 12:689767. |
| Molecular Formula |
C20H23N
|
|---|---|
| Molecular Weight |
277.40332
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| CAS # |
10262-69-8
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| Related CAS # |
Maprotiline hydrochloride;10347-81-6
|
| SMILES |
CNCCCC12CCC(C3=CC=CC=C31)C4=CC=CC=C42
|
| 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)
|
| 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6049 mL | 18.0245 mL | 36.0490 mL | |
| 5 mM | 0.7210 mL | 3.6049 mL | 7.2098 mL | |
| 10 mM | 0.3605 mL | 1.8025 mL | 3.6049 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.
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