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LY334370

产品编号 T4266Cas号 182563-08-2
别名 4-氟-N-(3-(1-甲基哌啶-4-基)-1H-吲哚-5-基)苯甲酰胺盐酸盐, LY 334370

LY334370 是一种选择性5-HT1F 受体激动剂,Ki 值为 1.6 nM。

LY334370

LY334370

纯度: 98.48%
产品编号 T4266 别名 4-氟-N-(3-(1-甲基哌啶-4-基)-1H-吲哚-5-基)苯甲酰胺盐酸盐, LY 334370Cas号 182563-08-2

LY334370 是一种选择性5-HT1F 受体激动剂,Ki 值为 1.6 nM。

规格价格库存数量
1 mg¥ 170现货
5 mg¥ 397现货
10 mg¥ 596现货
25 mg¥ 1,330现货
50 mg¥ 1,970现货
100 mg¥ 2,870现货
200 mg¥ 3,970现货
1 mL x 10 mM (in DMSO)¥ 437现货
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纯度:98.48%
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产品介绍

生物活性
产品描述
LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM
靶点活性
5-HT1F:Ki: 1.6 nM
体外活性
LY334370在体外对人脑动脉不表现出血管收缩效应,直至剂量达到10^-5 M,此时可触发8.5±5.7%的收缩率,但此结果并不显著。
体内活性
经静脉注射LY334370后,以3 mg/kg (n=3) 或10 mg/kg (n=6) 剂量进行电刺激,可以观察到硬脑膜血管直径分别增加至135±6%和106±11%,这与各自的对照值无显著差异。LY334370本身对硬脑膜血管直径无影响,因为在药物注射前后15分钟,硬脑膜血管的实际直径分别为43±4任意单位和43±4任意单位(10 mg/kg)。
激酶实验
AlphaScreen Assay: All reagents are diluted in 50 mM HEPES, 0.1% BSA, pH 7.5 supplemented with 0.01% Tween20 and allowed to equilibrate to room temperature prior to addition to plates. Catalytic turnover assays are run in 10 μL volumes in lowvolume 384-well plates at RT. The reaction consisted of enzyme (5 nM), biotinylated substrate peptide (30 nM), Fe(II) (1 μM), ascorbate (100 μM), 2OG (10 μM) and run at RT. For PHD2, the reaction consisted of enzyme (5 nM), biotinylated substrate peptide (60 nM), Fe(II) (20 μM), ascorbate (200 μM), 2OG (2 μM) and run at RT. EDTA is used to quench the reaction (5 μL), AlphaScreen donor (Streptavidin-conjugated) and acceptor (Protein A-conjugated) beads preincubated with peptide product antibodies are added (5 μL). Plates are foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. The final bead concentration in 20 μL reaction is 20 μg/mL. IC50 values are calculated in Prism 6 after normalisation against corresponding DMSO controls.
细胞实验
For in vitro studies, LY334370 is dissolved in buffer solution.Human cerebral artery is used in this study. Segments are prepared as previously described, but briefly they are placed in a buffer solution containing (mM) NaCl 119, NaHCo3 15, KCl 4.6, CaCl2 1.5, NaH2PO4 1.2, MgCl2 1.2, and glucose 5.5. Sections of vessel about 0.5 mm in diameter and 1 to 2 mm in length are mounted in a temperature-controlled tissue bath (37°C) containing buffer solution bubbled with 95% O2 and 5% CO2. The vessel segments are given a tension of 4 mN and allowed to stabilize at this tension for 1 to 1.5 h. Vessel reactivity is tested by exposure to 60 mM KCl. This is done twice for each segment and only if the response is similar to the segment used for LY334370 testing. Responses to LY334370 is calculated as a percentage of the maximum KC1 response.
动物实验
LY334370 is dissolved in 0.9% saline and is administered at a volume of 1 mL/kg. Male Sprague-Dawley rats (300 to 400 g) are treated with LY334370 (3 or 10 mg/kg, iv.).
别名4-氟-N-(3-(1-甲基哌啶-4-基)-1H-吲哚-5-基)苯甲酰胺盐酸盐, LY 334370
化学信息
分子量351.42
分子式C21H22FN3O
CAS No.182563-08-2
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (142.28 mM)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.8456 mL14.2280 mL28.4560 mL142.2799 mL
5 mM0.5691 mL2.8456 mL5.6912 mL28.4560 mL
10 mM0.2846 mL1.4228 mL2.8456 mL14.2280 mL
20 mM0.1423 mL0.7114 mL1.4228 mL7.1140 mL
50 mM0.0569 mL0.2846 mL0.5691 mL2.8456 mL
100 mM0.0285 mL0.1423 mL0.2846 mL1.4228 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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