Lasmiditan (COL-144; LY573144)
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发布时间: 2024-07-15 12:35:18
CAS号:439239-90-4
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纯度: 98.0%
备货期: 10天
库存: 现货
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用途: Lasmiditan (COL-144; LY573144) is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.IC50 value: 2.1 nM (Ki, 5-HT1F); >1000 nM (Ki, 5-HT1B/5-HT1D) [1]Target: 5-HT1F receptorin vitro: In vitro binding studies Lasmiditan showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor, compared with K(i) values of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively, a selectivity ratio greater than 470-fold. Lasmiditan showed higher selectivity for the 5-HT(1F) receptor relative to other 5-HT(1) receptor subtypes than the first generation 5-HT(1F) receptor agonist LY334370. Unlike the 5-HT(1B/1D) receptor agonist sumatriptan, lasmiditan did not contract rabbit saphenous vein rings, a surrogate assay for human coronary artery constriction, at concentrations up to 100 μM [1].in vivo: In two rodent models of migraine, oral administration of lasmiditan potently inhibited markers associated with electrical stimulation of the trigeminal ganglion (dural plasma protein extravasation, and induction of the immediate early gene c-Fos in the trigeminal nucleus caudalis) [1]. Two RCTs in the phase II development of lasmiditan was reviewed. In the intravenous placebo-controlled RCT, lasmiditan doses of 2.5-45 mg were used, and there was a linear association between headache relief (HR) rates and dose levels (P 物理化学性质: CAS号:439239-90-4 常用中文名:2,4,6-三氟-N-[6-[(1-甲基-4-哌啶基)羰基]-2-吡啶基]苯甲酰胺 常用英文名:Lasmiditan 分子式:C19H18F3N3O2 分子量:377.360 密度:1.4±0.1 g/cm3 沸点:433.3±45.0 °C at 760 mmHg 熔点:N/A 闪点:215.9±28.7 °C 储存条件:2-8℃
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公司名:上海念兴实业有限公司 推荐
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地址: 2222 Huancheng Road, Juyuan New District, Jiading District, Shanghai
地区: 上海市普陀区
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公司名:上海化源世纪贸易有限公司
区域:上海市普陀区
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2024-07-15 价格:需询单
2021-02-06 价格:¥2869.0
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Lasmiditan (COL-144; LY573144)价格为, 由Lasmiditan (COL-144; LY573144)生产厂家上海念兴实业有限公司提供,供应信息包括纯度,备货期/库存,供货能力等。>>电脑版:Lasmiditan (COL-144; LY573144)_价格_生产厂家【上海念兴实业有限公司】
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