| 產(chǎn)品描述： | MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release |
| 靶點(diǎn)： |
LTD4:0.22±0.15 nM (Ki, In guinea pig lung);LTD4:2.1±1.8 nM (Ki, In human lung);LTD4:10.5 (pA2);LTE4:10.4 (pA2);LeukotrieneReceptor;LTR |
| 體外研究： |
MK571 (15 μM, 1 h) sodium markedly suppresses constitutive and Ag-stimulated S1P secretion from RBL-2H3 cells and mast cells, and inhibits Fluo-3 efflux. Cell Viability Assay Cell Line: RBL-2H3 cells, human LAD2 mast cells Concentration: 15 μM Incubation Time: 1 h Result: Inhibited S1P secretion by vector and SphK1 transfected RBL-2H3 cells, whereas it did not affect uptake and intracellular conversion of [3H]Sph to S1P. Inhibited Fluo-3 efflux, inhibited S1P export by LAD2 cells, and blocked Ag-stimulated release of S1P. |
| 體內(nèi)研究： |
MK-571 sodium (0-0.5 mg/kg, orally, once) produces dose-dependent inhibition of the duration of antigen-induced dyspnea in conscious sensitized rats treated with methysergide (3 μg/kg). MK-571 sodium (0-1 mg/kg, orally, once) blocks LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys. MK-571 sodium (0-25 mg/kg, Orally, daily, for 2 more weeks) shows reversal of hypoxic pulmonary hypertension (PH), and protects mice from hypoxic PH. Animal Model: Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/kg methysergide, 5 min before antigen chdlenge) Dosage: 0.5, 0.15, and 0.05 mg/kg Administration: Orally, once, 1 or 4 h before challenge Result: Produced dose-dependent inhibition of the duration of antigen-induced dyspnea, with ED50 values of 0.13 (95% confidence interval (CI), 0.03-0.62) and 0.11 (95% CI, 0.009-1.47) mg/kg, respectively. MK-571 was even more active when administered orally as a suspension in 1% Methocel (4 h pretreatment), with an ED50 of 0.068 (95% CI, 0.83-0.14) mg/kg. Animal Model: Csnscisus squirrel msnkeys Dosage: 0.1, 0.5, and 1 mg/kg Administration: Orally, once, 2 h prior to challenge with Ascaris antigen Result: Produced significant inhibition of the bronchoconstriction at 0.5 mg/kg, produced significant inhibition of the increases in RL and decreases in Cdyn at 1 mg/kg. Animal Model: FVB (Friend virus B-type) mice (Mrp4–/– and WT, 6 weeks old, exposed to chronic hypoxia (10% O2) in a ventilated chamber for 28 day |
| 參考文獻(xiàn)： |
1. Jones TR, et al. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol. 1989 Jan;67(1):17-28. 2. Hara Y, et al. Inhibition of MRP4 prevents and reverses pulmonary hypertension in mice. J Clin Invest. 2011 Jul;121(7):2888-97. 3. Mitra P, et al. Role of ABCC1 in export of sphingosine-1-phosphate from mast cells. Proc Natl Acad Sci U S A. 2006 Oct 31;103(44):16394-9. |
| 溶解性： |
Soluble in H2O |
| 保存條件： |
-20℃ 充氮保存 |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.862 ml |
9.31 ml |
18.62 ml |
| 5 mM |
0.372 ml |
1.862 ml |
3.724 ml |
| 10 mM |
0.186 ml |
0.931 ml |
1.862 ml |
| 50 mM |
0.037 ml |
0.186 ml |
0.372 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。 |
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