MK 571

Research use only, not for human use.

MK 571 is an orally active antagonist of CysLT1 receptor .

MK 571 is an orally active antagonist of CysLT1 receptor.

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.

Animal Model:Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3μg/kg methysergide, 5 min before antigen chdlenge)Dosage:0.5, 0.15, and 0.05 mg/kgAdministration:Orally, once, 1 or 4 h before challengeResult: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 antigenResult: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 days)Dosage:0, 5, and 25 mg/kg Administration:Orally, daily, for 2 more weeks, maintain in hypoxic conditionsResult:Showed reversal of hypoxic pulmonary hypertension (PH), and mice were protected from hypoxic PH. MK-571-treated mice displayed lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles.

L-660711 | L660711 | MK-571

Immunology/Inflammation

LTR

CysLTR1

——

——

115104-28-4

515.09

C26H26ClN2NaO3S2

>98% (HPLC)

——

CN(C)C(=O)CCSC(SCCC(O)=O)c1cccc(\C=C\c2ccc3ccc(Cl)cc3n2)c1

——

(-20℃)

With Ice Pack

≥ 2 years