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LY334370

LY334370

产品编号 T4266   CAS 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。

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LY334370 Chemical Structure
LY334370, CAS 182563-08-2
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
其他形式的 LY334370:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: LY334370 (T4266)
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纯度: 98.48%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (142.28 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Shepheard S, et al. Possible antimigraine mechanisms of action of the 5HT1F receptor agonist LY334370. Cephalalgia. 1999 Dec;19(10):851-8.

TargetMol Library Books文献引用

1. Xu Z, Guo L, Yu J, et al.Ligand recognition and G protein coupling of trace amine receptor TAAR1.Nature.2023: 1-3.
Lumateperone Hesperetin Org-13011 fumarate Vabicaserin hydrochloride Vilazodone Hydrochloride Pardoprunox (±)-Fabesetron hydrochloride 5-HT3 antagonist 3

相关化合物库

该产品包含在如下化合物库中:
膜蛋白靶向化合物库 神经退行性疾病化合物库 GPCR靶点分子库 神经递质受体化合物库 含氟化合物库 ReFRAME 相关化合物库 表型筛选靶点鉴定库 神经信号分子库 血管生成库 5-羟色胺分子库

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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。

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Keywords

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

 

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