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Flibanserin

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纯度: 99.93%

货号 T4297Cas号 167933-07-5

别名 氟立班丝氨, Girosa, BIMT-17BS, BIMT-17

Flibanserin (Girosa) 一种具有口服活性的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂,Ki 值分别为 1 和 49 nM。它与多巴胺 D4 受体结合,Ki 值在 4 到 24 nM 之间。它是一种血清素能抗抑郁药,用于治疗性欲减退症。

Flibanserin
其他形式的 “Flibanserin”:

Flibanserin

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Rating icon 很棒

纯度: 99.93%

货号 T4297 别名 氟立班丝氨, Girosa, BIMT-17BS, BIMT-17Cas号 167933-07-5

Flibanserin (Girosa) 一种具有口服活性的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂,Ki 值分别为 1 和 49 nM。它与多巴胺 D4 受体结合,Ki 值在 4 到 24 nM 之间。它是一种血清素能抗抑郁药,用于治疗性欲减退症。

规格价格库存数量
1 mg
¥ 169
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5 mg
¥ 372
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10 mg
¥ 619
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25 mg
¥ 1,090
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50 mg
¥ 1,790
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100 mg
¥ 2,680
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200 mg
¥ 3,920
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1 mL x 10 mM (in DMSO)
¥ 397
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产品介绍


生物活性
产品描述
Flibanserin (Girosa) is a serotonergic antidepressant used to treat hypoactive sexual desire disorder. Flibanserin has been associated with a low rate of minor serum aminotransferase elevations during treatment but has not been linked to instances of clinically apparent acute liver injury.
靶点活性
D4 receptor:4-24 nM(Ki), 5-HT1A:1 nM(Ki), 5-HT2A:49 nM(Ki)
别名氟立班丝氨, Girosa, BIMT-17BS, BIMT-17
化学信息
分子量390.4
分子式C20H21F3N4O
CAS No.167933-07-5
SmilesC(CN1CCN(CC1)C2=CC(C(F)(F)F)=CC=C2)N3C=4C(NC3=O)=CC=CC4
密度1.292 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 50 mg/mL (128.07 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.12 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.5615 mL12.8074 mL25.6148 mL128.0738 mL
5 mM0.5123 mL2.5615 mL5.1230 mL25.6148 mL
10 mM0.2561 mL1.2807 mL2.5615 mL12.8074 mL
20 mM0.1281 mL0.6404 mL1.2807 mL6.4037 mL
50 mM0.0512 mL0.2561 mL0.5123 mL2.5615 mL
100 mM0.0256 mL0.1281 mL0.2561 mL1.2807 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20g,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%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/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 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | 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。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
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
% Saline/PBS/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

TargetMol AI Summary
Flibanserin exhibits a multifaceted bioactivity profile, notably including strong interactions with serotonin-related receptors and antiviral properties. It shows a high binding affinity to the human 5-HT1A receptor with a Ki of 11.75 nM and functions as an agonist with an EC50 of 630.96 nM and an Emax of 72.0% relative to 5-hydroxytryptamine. In vivo, it demonstrates antidepressant-like activity in rats, with an ED50 greater than 320 mg/kg in a forced swimming test and inducing forepaw treading and flat body posture at ED50 values greater than 40 mg/kg and 20 mg/kg, respectively. In the context of antiviral activity, Flibanserin inhibits SARS-CoV-2 cytotoxicity in Caco-2 and VERO-6 cells at 10 µM, with a notable inhibition of 56.47% cytotoxicity in Caco-2 cells after 48 hours. It also shows activity against the SARS-CoV-2 3CL-Pro protease at 20 µM via FRET assay, although the inhibition percentages are relatively modest (16.04% and 13.86%). The compound's effect on the USA-WA1/2020 strain of SARS-CoV-2, with a hit score of 0.2785 in HRCE cells, underscores its potential as an antiviral agent. Furthermore, Flibanserin demonstrates inhibitory activity against human HDAC6 with stronger effects observed using commercial peptide substrates (18.44% inhibition). It also binds to various other receptors, including DRD1, DRD3, OPRM1, ADRA2A, showing its potential involvement in multiple signaling pathways. Its complex pharmacological profile includes activities as both an agonist and antagonist across different receptors and enzymes. Overall, Flibanserin is a compound of significant interest for its diverse biological activities and therapeutic potential..
Note: Summary generated by AI, AI may be wrong some times, we do not provide any medical advice and only sell our product to accredited institution, Please cross-check with other sources, data source: chembl
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