ACY-1083

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ACY-1083  纯度: 98.14%

ACY-1083 是一种可渗透脑的选择性 HDAC6 抑制剂，IC50 为 3 nM，ACY-1083 对 HDAC6 的选择性比其他类别的 HDAC 亚型高 260 倍。ACY-1083 可有效逆转化疗引起的周围神经病变。

ACY-1083

ACY-1083 Chemical Structure

CAS No. : 1708113-43-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4400 In-stock
5 mg ￥4000 In-stock
10 mg ￥6750 In-stock
50 mg ￥20000 In-stock
100 mg ￥29000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy[1].

IC50 & Target[1]

HDAC6

3 nM (IC50)

体外研究
(In Vitro)

Treatment with ACY-1083 (30 and 300 nM) significantly improves cell viability in a dose-dependent manner[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: Mouse hippocampal (HT22) cells
Concentration: 30 and 300 nM
Incubation Time:
Result: Significant improvement in cell viability.

体内研究
(In Vivo)

ACY-1083 (i.p.; 10 mg/kg; for 7 days) effectively relieves Cisplatin-induced mechanical allodynia in C57BL/6J mice
ACY-1083 (oral doses of 3 mg/kg ACY-1083 for 7 days) reverses Paclitaxel-induced mechanical allodynia in adult male SD rats.
Mice dosed with 5 mg/kg ACY-1083 by intraperitoneal (i.p.) injection have a maximum plasma concentration (Cmax) of 936 ng/mL, a half-life (T1/2) of 3.5 hours, and a biologically active plasma exposure of 8 hours after dosing.

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: Adult male C57BL/6J mice of 8-10 weeks of age[1]
Dosage: 3 or 10 mg/kg
Administration: Administered i.p. injection; daily; for 7 days
Result: The 10 mg/kg relieved Cisplatin (2.3 mg/kg)-induced mechanical allodynia, whereas the 3 mg/kg dose did not.
Animal Model: Adult male Sprague Dawley rats[1]
Dosage: 3 mg/kg
Administration: Two daily doses were given orally for 7 days.
Result: Reversed Paclitaxel (6 mg/kg or 12 mg/kg)-induced mechanical allodynia.

分子量

348.35

Formula

C17H18F2N4O2
CAS 号

1708113-43-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 200 mg/mL (574.14 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8707 mL 14.3534 mL 28.7068 mL
5 mM 0.5741 mL 2.8707 mL 5.7414 mL
10 mM 0.2871 mL 1.4353 mL 2.8707 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 (stored under nitrogen)。-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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (14.35 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (14.35 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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

  • 2.

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

    Solubility: 5 mg/mL (14.35 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (14.35 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 50.0 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
  • 3.

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

    Solubility: ≥ 5 mg/mL (14.35 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (14.35 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 50.0 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]. Krukowski K, et al. HDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy. Pain. 2017 Jun;158(6):1126-1137.

    [2]. Vahagn C Nikolian, et al. Isoform 6-selective histone deacetylase inhibition reduces lesion size and brain swelling following traumatic brain injury and hemorrhagic shock. J Trauma Acute Care Surg. 2019 Feb;86(2):232-239.

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