Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LY334370 是一种选择性5-HT1F 受体激动剂,Ki 值为 1.6 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 283 | 现货 | ||
2 mg | ¥ 395 | 现货 | ||
5 mg | ¥ 662 | 现货 | ||
10 mg | ¥ 993 | 现货 | ||
25 mg | ¥ 2,230 | 现货 | ||
50 mg | ¥ 3,290 | 现货 | ||
100 mg | ¥ 4,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
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 has no vasoconstrictor effects on human cerebral arteries in vitro until up to a dose of 10-5 M, at which it produces a contraction of 8.5±5.7%; however, this is not significant |
体内活性 | Following intravenous administration of LY334370 at 3 mg/kg (n=3) or 10 mg/kg (n=6) electrical stimulation evokes an increase in dural blood vessel diameter of 135±6% and 106±11%, respectively, which is not significantly different from the respective control values. LY334370 has no effect on dural blood vessel diameter per se because the actual dural blood vessel diameter is 43±4 arbitrary units before drug and 43±4 arbitrary units 15 min after injection of LY334370 (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 |
分子量 | 351.42 |
分子式 | C21H22FN3O |
CAS No. | 182563-08-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (142.28 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8456 mL | 14.228 mL | 28.456 mL | 71.1399 mL |
5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL | 14.228 mL | |
10 mM | 0.2846 mL | 1.4228 mL | 2.8456 mL | 7.114 mL | |
20 mM | 0.1423 mL | 0.7114 mL | 1.4228 mL | 3.557 mL | |
50 mM | 0.0569 mL | 0.2846 mL | 0.5691 mL | 1.4228 mL | |
100 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.7114 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LY334370 182563-08-2 GPCR/G Protein Neuroscience 5-HT Receptor LY-334370 inhibit Inhibitor 5-hydroxytryptamine Receptor Serotonin Receptor 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 inhibitor