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Leukotriene receptor ligand
A potent, selective, orally active leukotriene D4 antagonist. Ki=2.1 nM for inhibition of [3H]-LTD4 binding to human lung membranes. Competitively antagonizes contractions of guinea pig trachea and ileum and human trachea induced by LTD4. Blocks LTD4 and ascaris-induced bronchoconstriction in conscious squirrel monkeys.
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Product Details
| Alternative Name |
L660,711 |
|---|---|
| Appearance |
Off-white solid. |
| CAS |
115104-28-4 |
| Couple Target |
Leukotriene receptor, Prostanoid receptor |
| Couple Type |
Ligand |
| Formula |
C26H26ClN2O3S2 . Na |
| MW |
537 |
| Purity |
≥90% (HPLC) |
| Solubility |
Soluble in water (20mg/ml), aqueous buffers, 100% ethanol (10mg/ml) or DMSO. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 2 months at -20°C. |
|---|---|
| Long Term Storage |
-20°C |
| Shipping |
Blue Ice |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Alisertib shows negligible potential for perpetrating pharmacokinetic drug-drug interactions on ABCB1, ABCG2 and cytochromes P450, but acts as dual-activity resistance modulator through the inhibition of ABCC1 transporter: D. Vagiannis, et al.; Toxicol. Appl. Pharmacol. 434, 115823 (2022), Abstract
- A reversal in sensory processing accompanies ongoing ecological divergence and speciation in Rhagoletis pomonella: C.Tait, et al.; Proc. Biol. Sci. 288, 192 (2021), Abstract
- Resolving different presynaptic activity patterns within single olfactory glomeruli of Xenopus laevis larvae: R. Topci, et al.; Sci. Rep. 11, 14258 (2021), Abstract
- Chemical effects on dye efflux activity in live zebrafish embryos and on zebrafish Abcb4 ATPase activity: F. Bieczynski, et al.; FEBS Lett. 595, 828 (2021), Application(s): Treatment of zebrafish embryos, Abstract
- Overexpression of ABCC1 Confers Drug Resistance to Betulin: X. Chen, et al.; Front. Oncol. 11, 640656 (2021), Application(s): Cell treatment (carcinoma cell lines: HEK293), Abstract — Full Text
- Uptake and metabolism of sulphated steroids by the blood–brain barrier in the adult male rat: M.Z. Qaiser, et al.; J. Neurochem. 142, 672 (2017), Abstract — Full Text
- G protein-coupled KISS1 receptor is overexpressed in triple negative breast cancer and promotes drug resistance: Blake, A., Dragan, M., et al.; Sci. Rep. 7, 46525 (2017), Abstract
- Glycol porphyrin derivatives and temoporfin elicit resistance to photodynamic therapy by different mechanisms: Kralova, J., Kolár, M., et al.; Sci. Rep. 7, 44497 (2017), Abstract
- Increased Systemic Exposure of Methotrexate by a Polyphenol-Rich Herb via Modulation on Efflux Transporters Multidrug Resistance-Associated Protein 2 and Breast Cancer Resistance Protein: C.P. Yu, et al.; J. Pharm. Sci. 105, 343 (2016), Application(s): Positive control, Abstract
- The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters: J.P. Rigalli, et al.; Cancer Lett. 376, 165 (2016), Application(s): Cell culture, Abstract
- The Interactions of P-Glycoprotein with Antimalarial Drugs, Including Substrate Affinity, Inhibition and Regulation: S.M. Senarathna, et al.; PLoS One 11, e0152677 (2016), Application(s): Cell culture, Abstract — Full Text
- Chemotherapy induces Notch1-dependent MRP1 up-regulation, inhibition of which sensitizes breast cancer cells to chemotherapy: Kim, B., Stephen, S. L., et al.; BMC Cancer 15, 634 (2015), Abstract
- Fast neuronal labeling in live tissue using a biocytin conjugated fluorescent probe: M. Harsløf, et al.; J. Neurosci. Methods 253, 101 (2015), Application(s): Cell Culture, Abstract
- Phospholipase C and diacylglycerol mediate olfactory responses to amino acids in the main olfactory epithelium of an amphibian: Sansone, A., Hassenklöver, T., et al.; PLoS One 9, e87721 (2014), Abstract
- Screening compounds with a novel high-throughput ABCB1-mediated efflux assay identifies drugs with known therapeutic targets at risk for multidrug resistance interference: Ansbro, M. R., Shukla, S., et al.; PLoS One 8, e60334 (2013), Abstract
- (R)-[(11)C]verapamil is selectively transported by murine and human P-glycoprotein at the blood-brain barrier, and not by MRP1 and BCRP: Römermann, K., Wanek, T., et al.; Nucl. Med. Biol. 40, 873 (2013), Abstract
- Bimodal processing of olfactory information in an amphibian nose: odor responses segregate into a medial and a lateral stream: Gliem, S., Syed, A. S., et al.; Cell. Mol. Life Sci. 70, 1965 (2013), Abstract
- Leukotrienes target F-actin/cofilin-1 to enhance alveolar macrophage anti-fungal activity: Morato-Marques, M., Campos, M. R., et al.; J. Biol. Chem. 286, 28902 (2011), Abstract
- Purinergic receptor-mediated Ca signaling in the olfactory bulb and the neurogenic area of the lateral ventricles: Hassenklöver, T., Schulz, P., et al.; Purinergic Signal. 6, 429 (2010), Abstract
- Olfactory coding with patterns of response latencies: Junek, S., Kludt, E., et al.; Neuron 67, 872 (2010), Abstract
- The endocannabinoid 2-arachidonoyl-glycerol controls odor sensitivity in larvae of Xenopus laevis: Breunig, E., Manzini, I., et al.; J. Neurosci. 30, 8965 (2010), Abstract
- Estradiol induces export of sphingosine 1-phosphate from breast cancer cells via ABCC1 and ABCG2: K. Takabe, et al.; J. Biol. Chem. 285, 10477 (2010), Abstract
- Sensitivity to sodium arsenite in human melanoma cells depends upon susceptibility to arsenite-induced mitotic arrest: McNeely, S. C., Belshoff, A. C., et al.; Toxicol. Appl. Pharmacol. 229, 252 (2008), Abstract
- Cannabinoid action in the olfactory epithelium: Czesnik, D., Schild, D., et al.; PNAS 104, 2967 (2007), Abstract
- Classes and narrowing selectivity of olfactory receptor neurons of Xenopus laevis tadpoles: Manzini, I., Schild, D., et al.; J. Gen. Physiol. 123, 99 (2004), Abstract
- Impact of BCRP/MXR, MRP1 and MDR1/P-Glycoprotein on thermoresistant variants of atypical and classical multidrug resistant cancer cells: U. Stein, et al.; Int. J. Cancer 97, 751 (2002), Abstract
- P-Glycoprotein and transporter MRP1 reduce HIV protease inhibitor uptake in CD4 cells: potential for accelerated viral drug resistance?: K. Jones, et al.; Aids 15, 1353 (2001), Abstract
- Overexpression of glutathione S-transferase II and multidrug resistance transport proteins is associated with acquired tolerance to inorganic arsenic: J. Liu, et al.; Mol. Pharmacol. 60, 302 (2001), Abstract
- Resistance of human multidrug resistance-associated protein 1-overexpressing lung tumor cells to the anticancer drug arsenic trioxide: L. Vernhet, et al.; Biochem. Pharmacol. 61, 1387 (2001), Abstract
- The leukotriene LTD4 receptor antagonist MK571 specifically modulates MRP associated multidrug resistance: V. Gekeler, et al.; Biochem. Biophys. Res. Commun. 208, 345 (1995), Abstract
- Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist: T.R. Jones, et al.; Can. J. Physiol. Pharmacol. 67, 17 (1989), Abstract
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