Avasimibe(Synonyms: CI-1011; PD-148515)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Avasimibe (Synonyms: CI-1011; PD-148515) 纯度: 99.58%

Avasimibe (CI-1011; PD-148515) 是一种有效的,具有口服活性的酰基辅酶 A: 胆固醇酰基转移酶 (ACAT) 抑制剂,对 ACAT1ACAT2IC50 分别为 24 和 9.2 µM。Avasimibe 可用于前列腺癌的研究。

Avasimibe(Synonyms: CI-1011;  PD-148515)

Avasimibe Chemical Structure

CAS No. : 166518-60-1

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10 mM * 1 mL in DMSO ¥550 In-stock
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100 mg ¥3200 In-stock
200 mg ¥5200 In-stock
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Avasimibe 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Lipid Metabolism Compound Library
  • Targeted Diversity Library

生物活性

Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively[1]. Avasimibe can be used for the research of prostate cancer[2].

IC50 & Target[1]

ACAT1

24 μM (IC50)

ACAT2

9.2 μM (IC50)

体外研究
(In Vitro)

Avasimibe (0, 0.25, 5, 10, 20, 40 and 80 µM; for 1, 2, and 3 days) reduces proliferation in the prostate cancer (PCa) cells[2].
Avasimibe (10 and 20 µM; 48 h) reduces the expression of β-catenin, Vimentin, N-cadherin, Snail and MMP9, which are tightly associated with epithelial-mesenchymal transition (EMT)[2].
Avasimibe (10 and 20 µM) trigger cell cycle arrest via the E2F-1 signalling pathway in prostate cancer. Avasimibe induces G1 phase cell cycle arrest of PCa cells[2].
Avasimibe (10 and 20 µM) inhibits the metastasis of PCa cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: PCa cells (PC-3 and DU 145)
Concentration: 0, 0.25, 5, 10, 20, 40 and 80 µM
Incubation Time: 1, 2, and 3 days
Result: Dose dependently inhibited PC-3 and DU 145 cell viability.

Western Blot Analysis[2]

Cell Line: PCa cells (PC-3 and DU 145)
Concentration: 10 and 20 µM
Incubation Time: 48 hours
Result: Reduced protein levels of EMT-related proteins (β-catenin, Vimentin, N-cadherin, Snail, MMP9 and E-cadherin).

Cell Cycle Analysis[2]

Cell Line: PCa cells (PC-3 and DU 145)
Concentration: 10 and 20 µM
Incubation Time: 48 hours
Result: Induced G1 phase cycle arrest and altered the G1 phase-related protein levels in PCa cells.

体内研究
(In Vivo)

Avasimibe (30 mg/kg, intraperitoneally injected on alternate days for 7 weeks) suppresses PCa cell growth and metastasis in vivo. Avasimibe has good biocompatibility and low toxicity[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SPF male mice (BALB/c-nude, 4 weeks old) bearing PCa cells[2]
Dosage: 30 mg/kg
Administration: Intraperitoneally injected for 7 weeks
Result: Reduced tumour volume compared with that of the control group. Inhibited PCa growth and migration in vivo.

分子量

501.72

Formula

C29H43NO4S

CAS 号

166518-60-1

中文名称

阿伐麦布

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (498.29 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9931 mL 9.9657 mL 19.9314 mL
5 mM 0.3986 mL 1.9931 mL 3.9863 mL
10 mM 0.1993 mL 0.9966 mL 1.9931 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.25 mg/mL (4.48 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.25 mg/mL (4.48 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.15 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.15 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Taichi Ohshiro,et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15.

    [2]. Kangping Xiong, et al. The cholesterol esterification inhibitor avasimibe suppresses tumour proliferation and metastasis via the E2F-1 signalling pathway in prostate cancer.Cancer Cell Int. 2021 Aug 30;21(1):461.

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