ACY-1083|cas:1708113-43-2|西域试剂

ACY-1083,98.0%

产品编号：Bellancom-111791| CAS NO：1708113-43-2| 分子式：C₁₇H₁₈F₂N₄O₂| 分子量：348.35

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货号	价格	库存与货期
Bellancom-111791	￥4000.00	杭州北京（现货）
Bellancom-111791	￥6750.00	杭州北京（现货）
Bellancom-111791	￥20000.00	杭州北京（现货）
Bellancom-111791	￥29000.00	杭州北京（现货）

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ACY-1083

产品介绍

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。

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.

体外研究

Treatment with ACY-1083 (30 and 300 nM) significantly improves cell viability in a dose-dependent manner.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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 (C_max) of 936 ng/mL, a half-life (T_1/2) of 3.5 hours, and a biologically active plasma exposure of 8 hours after dosing.

西域 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
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
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.

体内研究

西域 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
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
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.

体内研究

西域 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
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
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.

性状

Oil

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。