Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Elacridar (formerly GW-120918; GF-120918; GG-918; GW-0918; GF120918; GF120918; GW0918; GG918) is a 3rd generationl and potent P-glycoprotein (P-gp or MDR-1) and BCRP inhibitor that has the potential to overcome P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs such as doxorubicin. Elacridar has been used both in vitro and in vivo as a tool inhibitor of P-gp to investigate the role of transporters in the disposition of various test molecules. In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma.
ln Vitro |
Elacridar (0.001-1 μM; 2 h) reduces the viability of 786-O cells [2]. Elacridar (5 μM; 24 h) modulates P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines [2]. Elacridar (5 μM; 24 h) impacts 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells [2].
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ln Vivo |
Elacridar (100 mg/kg; intraperitoneally) distributes differently in the brain and plasma[1]. 1.19 Elacridar Plasma Pharmacokinetic Parameters in Mice[1]. AUC0-inf (μg·min/ml) 1460 90.3 161.4 F 0.22 0.013 1 Mice PO 100 mg/kg Mice IP 100 mg/kg Mice IV 2.5 mg/ kg CL/F (ml/min) 2.05 33.2 0.46 Vd/F (liter) 3.5 12.3 0.17 t1/2 (h) 20 4.3 4.4
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Cell Assay |
Cell Viability Assay[2]
Cell Types: 786-O cells Tested Concentrations: 2.5 and 5 μM Incubation Duration: 2 hrs (hours) Experimental Results: Dose-dependently inhibited cell viability of 786-O cells and demonstrated better inhibitory effect with sunitnib adding Western Blot Analysis[2] Cell Types: MCF-7, Caki-1, and 786-O cell lines Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dreased P-glycoprotein protein expression level in 786-O cells and increased ABCG2 protein expression level in Caki-1 cells. Cell Viability Assay[2] Cell Types: MCF-7 and 786-O cell lines Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependently increased 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells. |
Animal Protocol |
Animal/Disease Models: FVB wild-type mice[1].
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip)injection; 100 mg/kg once Experimental Results: Showd a higher concertation in brain than plasma except at 4 h after the dose. |
References |
[1]. Sane R, et al. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.
[2]. Sato H, et al. Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells. Eur J Pharmacol. 2015 Jan 5;746:258-66. |
Molecular Formula |
C34H33N3O5
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Molecular Weight |
563.64
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CAS # |
143664-11-3
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Related CAS # |
143851-98-3
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SMILES |
O(C([H])([H])[H])C1=C(C([H])=C2C(=C1[H])C([H])([H])N(C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C1=C([H])C([H])=C([H])C3C(C4C([H])=C([H])C([H])=C(C=4N([H])C=31)OC([H])([H])[H])=O)=O)C([H])([H])C2([H])[H])OC([H])([H])[H]
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (2.96 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 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. Solubility in Formulation 2: ≥ 0.5 mg/mL (0.89 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 5.0 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. View More
Solubility in Formulation 3: ≥ 0.25 mg/mL (0.44 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.25 mg/mL (0.44 mM) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. Solubility in Formulation 5: 0.05 mg/mL (0.09 mM) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: 4% DMSO+30% PEG 300+5% Tween 80+ddH2O:1 mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7742 mL | 8.8709 mL | 17.7418 mL | |
5 mM | 0.3548 mL | 1.7742 mL | 3.5484 mL | |
10 mM | 0.1774 mL | 0.8871 mL | 1.7742 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.