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AC265347

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货号 T29541Cas号 1253901-26-6

别名 AC-265347

AC265347 是一种有效的钙敏感受体 (CaSR) 激动剂和 ago-PAM 正变构调节剂,具有抗肿瘤活性,通过诱导分化抑制神经母细胞瘤肿瘤生长。AC265347 可用于研究神经母细胞瘤。

AC265347
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AC265347

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货号 T29541 别名 AC-265347Cas号 1253901-26-6

AC265347 是一种有效的钙敏感受体 (CaSR) 激动剂和 ago-PAM 正变构调节剂,具有抗肿瘤活性,通过诱导分化抑制神经母细胞瘤肿瘤生长。AC265347 可用于研究神经母细胞瘤。

规格价格库存数量
1 mg
¥ 458
现货
5 mg
¥ 1,090
现货
10 mg
¥ 1,860
现货
25 mg
¥ 3,730
现货
50 mg
¥ 5,320
现货
100 mg
¥ 7,280
现货
500 mg
¥ 14,500
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产品介绍


AC265347 AI Summary
AC265347 exhibits a wide range of bioactivities across various biological systems. It demonstrates high intrinsic clearance in human liver microsomes with a clearance rate of 396.0 mL.min^-1.g^-1. Functionally, it acts as a positive allosteric modulator of the calcium sensing receptor, showing an efficacy of 91.0% and an EC50 value of 25.12 nM in a cell-based assay. It also inhibits Plasmodium falciparum proliferation, displaying potencies that vary between 0.9 nM and 18821.2 nM across different strains of the parasite. In terms of cell viability, AC265347 has variable impacts depending on the cell type. It enhances growth rates in HEK293T cells from 0.84 to 0.99, whereas it exhibits a broader range of effects in U2OS cells, with growth rates spanning from -0.06 to 0.99. In human fibroblast cells, the compound consistently promotes cell growth, with rates ranging from 0.44 to 0.92, highlighting its potential cell-type specific bioactivities. Thermal Shift Assay results indicate that AC265347 affects the thermal stability of various protein domains differently. It decreases thermal stability in domains N44-E168 and M626-G740 (Delta TM = -2.23°C and -2.16°C respectively), suggesting protein destabilization. Conversely, it increases stability in domains E122-S403, P449-E759, and M1-S360 (Delta TM = 0.51°C, 0.21°C, and 0.76°C respectively), signifying a stabilizing effect. Furthermore, AC265347 exhibits inhibitory effects in GPCR beta-arrestin recruitment assays targeting multiple receptors including CX3CR1, AGTR1, ADGRF1, C5AR1, GLP1R, FFAR4, GPR119, ADRA2A, FPR2, GPR35, S1PR1, ADRB2, APLNR, and ADGRF1. Some assays also suggest a positive maximal effect on receptors such as GLP1R, ADRA2A, FPR2, GPR35, AGTR1, S1PR1, APLNR, and FFAR4. Overall, AC265347 demonstrates a complex interplay of stabilizing and destabilizing effects on protein structures and varied impacts on cell viability and GPCR activity..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
AC265347 is a potent calcium-sensitive receptor (CaSR) agonist and ago-PAM orthosteric modulator with antitumour activity that inhibits neuroblastoma tumour growth by inducing differentiation.AC265347 can be used to study neuroblastoma.
别名AC-265347
化学信息
分子量283.39
分子式C17H17NOS
CAS No.1253901-26-6
SmilesOC(C1=NC=2C=CC=CC2S1)(C3=CC=C(C=C3C)C)C
密度no data available
储存&溶解度
存储store at low temperature | 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: 80 mg/mL (282.3 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (11.64 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 mM3.5287 mL17.6435 mL35.2871 mL176.4353 mL
5 mM0.7057 mL3.5287 mL7.0574 mL35.2871 mL
10 mM0.3529 mL1.7644 mL3.5287 mL17.6435 mL
20 mM0.1764 mL0.8822 mL1.7644 mL8.8218 mL
50 mM0.0706 mL0.3529 mL0.7057 mL3.5287 mL
100 mM0.0353 mL0.1764 mL0.3529 mL1.7644 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

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