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HDAC6-IN-13

产品编号 T61474

HDAC6-IN-13 (Compound 35m) is a potent and highly selective orally active inhibitor of HDAC6, with an IC50 of 0.019 μM. It also demonstrates inhibitory activity against HDAC1, HDAC2, and HDAC3, with IC50 values of 1.53 μM, 2.06 μM, and 1.03 μM, respectively. HDAC6-IN-13 exhibits substantial blood-brain barrier permeability and displays anti-inflammatory properties [1].

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HDAC6-IN-13

HDAC6-IN-13, CAS N/A

规格	价格/CNY	货期
25 mg	￥ 10,600	10-14周
50 mg	￥ 13,800	10-14周
100 mg	￥ 17,500	10-14周

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生物活性

化学信息

存储 & 溶解度

产品描述	HDAC6-IN-13 (Compound 35m) is a potent and highly selective orally active inhibitor of HDAC6, with an IC50 of 0.019 μM. It also demonstrates inhibitory activity against HDAC1, HDAC2, and HDAC3, with IC50 values of 1.53 μM, 2.06 μM, and 1.03 μM, respectively. HDAC6-IN-13 exhibits substantial blood-brain barrier permeability and displays anti-inflammatory properties [1].
体外活性	HDAC6-IN-13 (Compound 35m) (0.1-1 μM; 24 h) is highly selective toward HDAC6 versus class I HDACs [1]. HDAC6-IN-13 is a slow-on and slow-off tight-binding HDAC6 inhibitor, while exhibits fast-on properties for HDAC1, 2, and 3 [1]. HDAC6-IN-13 (5-20 μM; 8 h) shows anti-inflammatory activity in vitro [1]. Western Blot Analysis [1] Cell Line: MV4 11 and J774A.1 Concentration: 0.1, 0.2, 0.5 and 1 μM Incubation Time: 24 h Result: Concentration-related accumulation of acetylated tubulin (Ac-Tubulin) was observed, while upregulation of acetylated histone H3 (AcHH3) and acetylated histone H4 (AcHH4) was not apparent even at the concentration of 1 μM. Western Blot Analysis [1] Cell Line: J774A.1 cells Concentration: 5, 10 and 20 μM Incubation Time: 8 h Result: Inhibited the cleavage of pro-caspase 1 to p20 in a dose-dependent manner, inhibited the interaction between HDAC6 and dynein.
体内活性	HDAC6-IN-13 (Compound 35m) (20 mg/kg; p.o. and i.p.; once) displays a remarkable inhibition in LPS-induced inflammation in mice [1]. HDAC6-IN-13 (20 mg/kg; p.o.; once) shows very high oral bioavailability (F% = 93.4%) and significant BBB permeability in mice [1]. Animal Model: Male C57BL/6 WT mice, LPS-induced endotoxic shock model [1] Dosage: 20 mg/kg Administration: PO and IP, immediately after the LPS injection Result: Significantly decreased the serum IL-1β levels in LPS-induced mice via both ip and po administration. Animal Model: Male CD-1 mice [1] Dosage: 5 mg/kg or 20 mg/kg Administration: IV (5 mg/kg) or PO (20 mg/kg) (Pharmacokinetic Study) Result: Pharmacokinetics Characterization of HDAC6-IN-13 (Compound 35m) with iv and Oral Administration a [1] PK parameters HDAC6-IN-13 HDAC6-IN-13 administered dose (mg/kg) iv at 5 mg/kg oral at 20 mg/kg C max (ng/mL) 4604 ± 551 5570 ± 551 t 1/2 (h) 7.95 ± 0.370 6.80 ± 0.145 AUC 0 inf (ng h/mL) 2755 ± 395 10292 ± 1385 F% n/a 93.4 ± 12.6 a HDAC6-IN-13 was administrated via iv and po (n = 3). The blood sample was collected at different time points after dosing, and the plasma concentration of HDAC6-IN-13 was determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) was calculated using the linear trapezoidal method. The pharmacokinetic parameters were obtained using the noncompartmental method. Data are shown as mean ± SD.

分子量	370.45
分子式	C23H22N4O

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：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。

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