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Cat. No. M1888
Tariquidar Structure


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10mg USD 130 In stock
50mg USD 380 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Tariquidar is a highly selective, potent non-competitive inhibitor of P-glycoprotein. P-glycoprotein actively transports structurally unrelated compounds out of cells, conferring the multidrug resistance phenotype in cancer. P-gp is also expressed in normal tissues like blood brain barrier, gastrointestinal track, liver, spleen and kidney. Tariquidar profoundly inhibited P-glycoprotein in lymphocytes by 93.7% (95% confidence interval, 92.0-95.3%). Tariquidar (XR9576) inhibits the ATPase activity of P-glycoprotein, suggesting that the modulating effect is derived from both inhibition of substrate binding and inhibition of ATP hydrolysis or each of them.

Cell Experiment
Cell lines HEK 293 cells
Preparation method A sample of the isolated histidine-tagged P-gp was mixed with an equal volume of 10 mg/ml of sheep brain phosphatidylethanolamine that had been washed and suspended in TBS. ATPase activity was measured in the presence of various concentrations of tariquidar.
Concentrations 0.25 µM, 0.5 µM, 1 µM,
Incubation time 24 h
Animal Experiment
Animal models Balb/C mice
Formulation water with 5% glucose
Dosages 10 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 646.73
Formula C38H38N4O6
CAS Number 206873-63-4
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source J Biol Chem (2015). Figure 3. Tariquidar
Method Disulfide Cross-linking Analysis
Cell Lines HEK 293 cells
Concentrations 0.5 μM
Incubation Time 16 h
Results Accordingly, we screened the rescue of 223 G251V processing mutants in which each position in the TM segment was replaced with arginine. HEK293 cells were transfected with each mutant and expressed for 16 h in the absence or presence of 0.5 μM tariquidar.
Source J Biol Chem (2015). Figure 2. Tariquidar
Method Expression and Maturation of G251V Arginine Mutants
Cell Lines HEK 293 cells
Concentrations 500, 1000 nM
Incubation Time 16 h
Results By contrast, a higher concentration (1000 nM) of tariquidar did not significantly inhibit cross-linking of the ICL (L175C(ICL1)/N820C(ICL3), A259C(ICL2)/W803C(ICL3), A266C(ICL2/F1086C(NBD2)) (Fig. 2B) or the NBD (C431(NBD1)/L1176C(NBD2), L531C(NBD1)/C1074(NBD2), and P517C(NBD1)/I1050C(NBD2)) mutants (Fig. 2C).

Reversal of multidrug resistance by co-delivery of tariquidar (XR9576) and paclitaxel using long-circulating liposomes.
Patel NR, et al. Int J Pharm. 2011 Sep 15;416(1):296-9. PMID: 21703341.

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Keywords: Tariquidar, XR9576 supplier, P-gp, inhibitors

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