Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
sigma (σ) receptor[1] dopamine transporter[1]
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ln Vitro |
HCT-116p53+/+ cell counts are lowered concentration-dependently by rimcazole (1–50 μM; 24-48 hours) [2]. In cancer cells (HCT-116p53+/+ and MDA-MB-231 cells), rimcazole (50 μM; 1–24 hours) causes a transitory increase of HIF-1α protein, but not in normal human dermal fibroblasts [2].
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Cell Assay |
Western Blot Analysis[2]
Cell Types: HCT-116p53+/+ cells Tested Concentrations: 50 μM Incubation Duration: 1, 2, 3, 5, 6, 24 hrs (hours) Experimental Results: Accumulation of HIF-1α protein, maximal at 6 h. No change in p53 protein levels. HIF-1α protein levels returned to normal steady-state levels within 24 h. |
References |
[1]. Gilmore DL, et, al. Review of the pharmacological and clinical profile of rimcazole. CNS Drug Rev. Spring 2004;10(1):1-22.
[2]. Achison M, et, al. HIF-1alpha contributes to tumour-selective killing by the sigma receptor antagonist rimcazole. Oncogene. 2007 Feb 22;26(8):1137-46. [3]. Matsumoto RR, et, al. Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters. Neuropharmacology. 2001 Dec;41(7):878-86. [4]. Job MO, et, al. A behavioral economic analysis of the effects of rimcazole on reinforcing effects of cocaine injection and food presentation in rats. Psychopharmacology (Berl). 2019 Dec;236(12):3601-3612. |
Molecular Formula |
C21H29CL2N3
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Molecular Weight |
394.38
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CAS # |
75859-03-9
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Related CAS # |
Rimcazole;75859-04-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
Cl.Cl.CC1NC(C)CN(CCCN2C3=CC=CC=C3C3=CC=CC=C23)C1
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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) |
DMSO: 12.5 mg/mL (31.70 mM)
H2O: < 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5356 mL | 12.6781 mL | 25.3563 mL | |
5 mM | 0.5071 mL | 2.5356 mL | 5.0713 mL | |
10 mM | 0.2536 mL | 1.2678 mL | 2.5356 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.