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Lasmiditan
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lasmiditan图片
CAS NO:439239-90-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Cas No.439239-90-4
别名拉米地坦
化学名2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl]benzamide
Canonical SMILESCN1CCC(CC1)C(=O)C2=NC(=CC=C2)NC(=O)C3=C(C=C(C=C3F)F)F
分子式C19H18F3N3O2
分子量377.36
溶解度DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:20): 0.04 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Lasmiditan is a selective agonist of 5-HT1F receptor with Ki value of 2.21nM [1].

Lasmiditan shows great selectivity against 5-HT1F over other human recombinant 5-HT receptor subtypes as well as other members of 5-HT1 family. The Ki values for 5-HT2A-2C, 5-HT6 and 5-HT7 are all above 2μM. In the in vitro functional assay, lasmiditan shows high functional selectivity for 5-HT1F with EC50 value of 43.1nM. Moreover, oral administration of lasmiditan potently decreases the dural plasma protein extravasation with ID50 value of 2×104μg/kg in the migraine models. It also inhibits trigeminal stimulation-induced c-fos expression in the nucleus caudalis. Furthermore, lasmiditan is proved to be an effective treatment in acute migraine after the phase II trials. And the oral administration is found to be better than the intravenous administration [1, 2]

References:
[1] Nelson D L, Phebus L A, Johnson K W, et al. Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia, 2010, 30(10): 1159-1169.
[2] Tfelt-Hansen P C, Olesen J. The 5-HT1F receptor agonist lasmiditan as a potential treatment of migraine attacks: a review of two placebo-controlled phase II trials. The journal of headache and pain, 2012, 13(4): 271-275.