206873-63-4 | Tariquidar

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$35.00	$24.00
5mg	95%	in stock	$78.00	$54.00
10mg	95%	in stock	$112.00	$78.00
25mg	95%	in stock	$180.00	$126.00
100mg	95%	in stock	$569.00	$398.00

Description

• Catalog Number: AB17381
• Chemical Name: Tariquidar
• CAS Number: 206873-63-4
• Molecular Formula: C38H38N4O6
• Molecular Weight: 646.7315
• MDL Number: MFCD09837824
• SMILES: COc1cc(C(=O)Nc2ccc(cc2)CCN2CCc3c(C2)cc(c(c3)OC)OC)c(cc1OC)NC(=O)c1cnc2c(c1)cccc2

Computed Properties

• Complexity: 1040
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 48
• Hydrogen Bond Acceptor Count: 8
• Hydrogen Bond Donor Count: 2
• Rotatable Bond Count: 11
• XLogP3: 6.1

Literature

• P-Glycoprotein on Blood-Brain Barrier Plays a Vital Role in Fentanyl Brain Exposure and Respiratory Toxicity in Rats.

  Toxicological sciences : an official journal of the Society of Toxicology 20180701

• Increasing nerve agent treatment efficacy by P-glycoprotein inhibition.

  Chemico-biological interactions 20161125

• Inhibition of P-glycoprotein Gene Expression and Function Enhances Triptolide-induced Hepatotoxicity in Mice.

  Scientific reports 20150101

• Behavioral effects and central nervous system levels of the broadly available κ-agonist hallucinogen salvinorin A are affected by P-glycoprotein modulation in vivo.

  The Journal of pharmacology and experimental therapeutics 20120601

• Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.

  Journal of medicinal chemistry 20120412

• [Evaluation of P-glycoprotein mediated in vitro loperamide biliary excretion with sandwich-cultured rat hepatocytes model].

  Yao xue xue bao = Acta pharmaceutica Sinica 20120401

• Alteration in P-glycoprotein functionality affects intrabrain distribution of quinidine more than brain entry-a study in rats subjected to status epilepticus by kainate.

  The AAPS journal 20120301

• Pgp-mediated interaction between (R)-[11C]verapamil and tariquidar at the human blood-brain barrier: a comparison with rat data.

  Clinical pharmacology and therapeutics 20120201

• A comparative small-animal PET evaluation of [11C]tariquidar, [11C]elacridar and (R)-[11C]verapamil for detection of P-glycoprotein-expressing murine breast cancer.

  European journal of nuclear medicine and molecular imaging 20120101

• Genetic knockdown and pharmacological inhibition of parasite multidrug resistance transporters disrupts egg production in Schistosoma mansoni.

  PLoS neglected tropical diseases 20111201

• Increasing oxime efficacy by blood-brain barrier modulation.

  Toxicology letters 20110925

• Synthesis and structure-activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein.

  Journal of medicinal chemistry 20110825

• Collateral sensitivity of multidrug-resistant cells to the orphan drug tiopronin.

  Journal of medicinal chemistry 20110728

• Solid phase synthesis of tariquidar-related modulators of ABC transporters preferring breast cancer resistance protein (ABCG2).

  Bioorganic & medicinal chemistry letters 20110615

• A novel positron emission tomography imaging protocol identifies seizure-induced regional overactivity of P-glycoprotein at the blood-brain barrier.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20110615

• The third-generation P-glycoprotein inhibitor tariquidar may overcome bacterial multidrug resistance by increasing intracellular drug concentration.

  The Journal of antimicrobial chemotherapy 20110401

• Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP).

  Bioorganic & medicinal chemistry 20110315

• A pharmacodynamic study of docetaxel in combination with the P-glycoprotein antagonist tariquidar (XR9576) in patients with lung, ovarian, and cervical cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20110201

• Synthesis and in vivo evaluation of ¹⁸F-fluoroethyl GF120918 and XR9576 as positron emission tomography probes for assessing the function of drug efflux transporters.

  Bioorganic & medicinal chemistry 20110115

• Specific inhibitors of the breast cancer resistance protein (BCRP).

  ChemMedChem 20100903

• Synthesis and evaluation of [11C]XR9576 to assess the function of drug efflux transporters using PET.

  Annals of nuclear medicine 20100601

• Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET.

  European journal of nuclear medicine and molecular imaging 20100501

• P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide.

  Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20100401

• Assessment of regional differences in tariquidar-induced P-glycoprotein modulation at the human blood-brain barrier.

  Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 20100301

• Uptake and binding of the serotonin 5-HT1A antagonist [18F]-MPPF in brain of rats: effects of the novel P-glycoprotein inhibitor tariquidar.

  NeuroImage 20100115

• Novel lead for potent inhibitors of breast cancer resistance protein (BCRP).

  Bioorganic & medicinal chemistry letters 20100101

• A pilot study to assess the efficacy of tariquidar to inhibit P-glycoprotein at the human blood-brain barrier with (R)-11C-verapamil and PET.

  Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20091201

• Nanoparticle-mediated simultaneous and targeted delivery of paclitaxel and tariquidar overcomes tumor drug resistance.

  Journal of controlled release : official journal of the Controlled Release Society 20090521

• A phase I study of the P-glycoprotein antagonist tariquidar in combination with vinorelbine.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20090515

• Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators.

  Bioorganic & medicinal chemistry 20090315

• Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar.

  Journal of medicinal chemistry 20090226

• Functional and energetic characterization of P-gp-mediated doxorubicin transport in rainbow trout (Oncorhynchus mykiss) hepatocytes.

  Comparative biochemistry and physiology. Toxicology & pharmacology : CBP 20090101

• Influence of the dual ABCB1 and ABCG2 inhibitor tariquidar on the disposition of oral imatinib in mice.

  Journal of experimental & clinical cancer research : CR 20090101

• Tariquidar, a selective P-glycoprotein inhibitor, does not potentiate loperamide's opioid brain effects in humans despite full inhibition of lymphocyte P-glycoprotein.

  Anesthesiology 20081201

• Resistance to antiepileptic drugs and expression of P-glycoprotein in two rat models of status epilepticus.

  Epilepsy research 20081101

• Tariquidar-induced P-glycoprotein inhibition at the rat blood-brain barrier studied with (R)-11C-verapamil and PET.

  Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20080801

• Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice.

  Journal of cancer research and clinical oncology 20080501

• Glutamate is critically involved in seizure-induced overexpression of P-glycoprotein in the brain.

  Neuropharmacology 20080501

• Inhibition of P-glycoprotein (ABCB1)- and multidrug resistance-associated protein 1 (ABCC1)-mediated transport by the orally administered inhibitor, CBT-1((R)).

  Biochemical pharmacology 20080315

• Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.

  Bioorganic & medicinal chemistry 20080301

• Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.

  Bioorganic & medicinal chemistry 20080101

• Region-specific overexpression of P-glycoprotein at the blood-brain barrier affects brain uptake of phenytoin in epileptic rats.

  The Journal of pharmacology and experimental therapeutics 20070701

• In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).

  Bioorganic & medicinal chemistry 20070601

• Differential drug susceptibility of intracellular and extracellular tuberculosis, and the impact of P-glycoprotein.

  Tuberculosis (Edinburgh, Scotland) 20070501

• Development of a humanized in vitro blood-brain barrier model to screen for brain penetration of antiepileptic drugs.

  Epilepsia 20070301

• Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein.

  Neuropharmacology 20070201

• Multidrug-resistance gene 1-type p-glycoprotein (MDR1 p-gp) inhibition by tariquidar impacts on neuroendocrine and behavioral processing of stress.

  Psychoneuroendocrinology 20070101

• In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity at CYP-450.

  Bioorganic & medicinal chemistry 20061201

• Quantification of serotonin 5-HT1A receptors in monkey brain with [11C](R)-(-)-RWAY.

  Synapse (New York, N.Y.) 20061201

• The erythromycin breath test reflects P-glycoprotein function independently of cytochrome P450 3A activity.

  Clinical pharmacology and therapeutics 20060901

• Modulation of multidrug resistance efflux pump activity to overcome chemoresistance in cancer.

  Current opinion in pharmacology 20060801

• Differential in vivo sensitivity to inhibition of P-glycoprotein located in lymphocytes, testes, and the blood-brain barrier.

  The Journal of pharmacology and experimental therapeutics 20060601

• Inhibition of multidrug resistance transporter-1 facilitates neuroprotective therapies after focal cerebral ischemia.

  Nature neuroscience 20060401

• Inhibition of the multidrug transporter P-glycoprotein improves seizure control in phenytoin-treated chronic epileptic rats.

  Epilepsia 20060401

• Structure-activity relationships of a series of tariquidar analogs as multidrug resistance modulators.

  Bioorganic & medicinal chemistry 20060301

• Phase II study of tariquidar, a selective P-glycoprotein inhibitor, in patients with chemotherapy-resistant, advanced breast carcinoma.

  Cancer 20050815

• Identification of OATP1B3 as a high-affinity hepatocellular transporter of paclitaxel.

  Cancer biology & therapy 20050801

• The coupling mechanism of P-glycoprotein involves residue L339 in the sixth membrane spanning segment.

  FEBS letters 20050718

• Modulation of drug resistance transporters as a strategy for treating myelodysplastic syndrome.

  Best practice & research. Clinical haematology 20041201

• P-glycoprotein retains function when reconstituted into a sphingolipid- and cholesterol-rich environment.

  Journal of lipid research 20041001

• Ex vivo reversal of chemoresistance by tariquidar (XR9576).

  Anti-cancer drugs 20041001

• Inhibition of glucosylceramide synthase does not reverse drug resistance in cancer cells.

  The Journal of biological chemistry 20040924

• Inhibition of P-glycoprotein function by XR9576 in a solid tumour model can restore anticancer drug efficacy.

  European journal of cancer (Oxford, England : 1990) 20040301

• Pheophorbide a is a specific probe for ABCG2 function and inhibition.

  Cancer research 20040215

• Pumping of drugs by P-glycoprotein: a two-step process?

  The Journal of pharmacology and experimental therapeutics 20031201

• The histone deacetylase inhibitor FK228 preferentially enhances adenovirus transgene expression in malignant cells.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20031101

• Increased 99mTc-sestamibi accumulation in normal liver and drug-resistant tumors after the administration of the glycoprotein inhibitor, XR9576.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20030201

• In vitro prevention of the emergence of multidrug resistance in a pediatric rhabdomyosarcoma cell line.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20011001

• In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576.

  Cancer research 20010115