MK 886 (L 663536) 是一种有效的、细胞渗透性和口服活性的 FLAP（IC50 为 30 nM）和白三烯生物合成（完整白细胞和人全血中的 IC50 分别为 3 nM 和 1.1 μM）抑制剂。 MK 886 也是一种非竞争性 PPARα 拮抗剂，可诱\u200b\u200b导细胞凋亡。
| Cas No. | 118414-82-7 |
| 别名 | 3-[1-(4-氯苄基)-3-叔丁基硫代-5-异丙基吲哚-2-基]-2,2-二甲基丙酸,L 663536 |
| 化学名 | 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid |
| Canonical SMILES | ClC1=CC=C(C=C1)CN(C2=CC=C(C(C)C)C=C32)C(CC(C)(C(O)=O)C)=C3SC(C)(C)C |
| 分子式 | C27H34ClNO2S |
| 分子量 | 472.08 |
| 溶解度 | DMF: 15 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml,DMSO: 5 mg/ml,Ethanol: 0.14 mg/ml |
| 储存条件 | Store at 2-8℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | MK-886 (L 663536) is a 5-lipoxygenase-activating protein inhibitor and a leukotriene biosynthesis inhibitor (IC50=2.5 nM). References:
[1]. [1] Kehrer JP et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochem J. 2001 Jun 15.
[2]. [2] Gillard J et al. L-663,536 (MK-886) (3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2 - dimethylpropanoic acid), a novel, orally active leukotriene biosynthesis inhibitor. Can J Physiol Pharmacol. 1989 May;67(5):456-64.
[3]. [3] Dixon RA et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature, 1990 Jan 18, 343(6255):282-4.http://www.ncbi.nlm.nih.gov/pubmed/2300173 |
