MK-571 sodium salt

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效且特异性的 LTD4 受体拮抗剂，Ki 为 0.22 nM。

A potent and specific LTD4 receptor antagonist with Ki of 0.22 nM; effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors; also is an inhibitor of multidrug resistance protein-1 (MRP1) mediated transportorally active.Asthma Phase 2 Clinical(In Vitro):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.(In Vivo):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 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 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 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 sodium salt

GPCR/G Protein

Leukotriene Receptor

CysLTR1

Inflammation/Immunology

Asthma

115103-85-0

537.069

C26H26ClN2NaO3S2

>98% (HPLC)

DMSO: ≥ 33 mg/mL

CN(C)C(=O)CCSC(C1=CC=CC(=C1)C=CC2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)[O-].[Na+]

Propanoic acid, 3-[[[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]-, sodium salt, (E)- (9CI)

(-20℃)

With Ice Pack

≥ 2 years