Bioactivity | MK-571 (L-660711) 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 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3]. |
Invitro | MK571(15 μM,1 小时)显着抑制 RBL-2H3 细胞和肥大细胞的组成型和 Ag 刺激的 S1P 分泌,并抑制 Fluo-3 外排[3]。 0 --> MK-571 相关抗体: Cell Viability Assay[3] Cell Line: |
In Vivo | MK-571(0-0.5 mg/kg,口服,一次)对接受美西麦角 (3 μg/kg) 治疗的清醒致敏大鼠中抗原诱导的呼吸困难持续时间产生剂量依赖性抑制[1]。MK-571(0-1 mg/kg,口服,一次)可阻断有意识的松鼠猴中 LTD4- 和蛔虫诱导的支气管收缩[1]。MK-571(0-25 mg/kg,口服,每天,持续 2 周以上)可逆转缺氧性肺动脉高压 (PH),并保护小鼠免受缺氧性 PH 的影响[2]。 Animal Model: |
Name | MK-571 |
CAS | 115104-28-4 |
Formula | C26H27ClN2O3S2 |
Molar Mass | 515.09 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |