2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC6-IN-80

HDAC6-IN-80 是一种口服有效的、选择性的 HDAC6 抑制剂，IC50 为 8.5 nM。HDAC6-IN-80 可抑制脂多糖诱导的小胶质细胞活化，降低 iNOS、COX-2、TNF−α 和 IL-6 的水平，并缓解感觉超敏行为。HDAC6-IN-80 可用于炎性疼痛和化疗诱导的周围神经病变的研究。

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HDAC6-IN-80

HDAC6-IN-80 Chemical Structure

CAS No. : 3118852-74-4

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HDAC6-IN-80 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy[1].

IC50 & Target[1]

HDAC6

 

体外研究
(In Vitro)

HDAC6-IN-80 (Compound 36) (1-10 μg/mL; 6.5-24.5 h) 通过降低亚硝酸盐水平及促炎介质 (iNOS、COX-2、TNF-α、IL-6) 的 mRNA 和蛋白表达，抑制 BV2 小胶质细胞中 LPS 诱导的炎症反应，且在浓度高达 10 μg/mL 时不影响细胞活力[1]。

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

HDAC6-IN-80 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax T1/2 Tmax AUC0-t AUC0-∞ Bioavailability CL
Mice[1] 3 mg/kg i.v. / 0.15 h / 106 ng·h/mL 106 ng·h/mL / 478 mL/min/kg
Mice[1] 10 mg/kg p.o. 111 ng/mL 0.50 h 0.25 h 78.6 ng·h/mL 80.9 ng·h/mL 22.85 % /
体内研究
(In Vivo)

HDAC6-IN-80 (Compound 36) (15-60 mg/kg；口服；单次给药) 可剂量依赖性地缓解 Carrageenan (HY-125474) 诱导的小鼠炎症性疼痛，其 ED50 为 35.66 mg/kg[1]。
HDAC6-IN-80 (15-60 mg/kg；口服；单次给药) 可剂量依赖性地缓解 Paclitaxel (HY-B0015) 诱导的小鼠神经性疼痛，其 ED50 为 37.89 mg/kg[1]。
HDAC6-IN-80 (15-60 mg/kg；口服；单次给药) 在剂量高达 30 mg/kg 时对小鼠的运动协调性仅产生极微弱影响，仅在 60 mg/kg 剂量下才会造成显著损伤[1]。

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

Animal Model: ICR (male, 20-32 g)[1]
Dosage: 15 mg/kg; 30 mg/kg; 60 mg/kg
Administration: p.o.; single dose
Result: Produced a maximum possible effect (MPE) of 45.84% at 30 mg/kg.
Dose-dependently increased mechanical paw withdrawal thresholds (MWTs) across all tested doses.
Significantly elevated the area under the curve (AUC) of MWTs in a dose-related manner.
Achieved an ED50 value of 35.66 mg/kg for alleviating carrageenan-induced allodynia.
Animal Model: ICR (male, 20-32 g)[1]
Dosage: 15 mg/kg; 30 mg/kg; 60 mg/kg
Administration: p.o.; single dose
Result: Dose-dependently increased mechanical withdrawal thresholds (MWTs) in paclitaxel-treated mice.
Achieved an ED50 value of 37.89 mg/kg for alleviating paclitaxel-induced mechanical allodynia.
Significantly elevated the area under the curve (AUC) of MWTs in a dose-related manner.
Animal Model: ICR (male, 20-32 g)[1]
Dosage: 15 mg/kg; 30 mg/kg; 60 mg/kg
Administration: p.o.; single dose
Result: Did not induce statistically significant motor impairment at 15 and 30 mg/kg.
Significantly reduced rotarod latency at 30, 60, and 90 minutes post-administration at 60 mg/kg (p < 0.01 vs vehicle).
分子量

381.43

Formula

C21H23N3O4
CAS 号
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HDAC6-IN-80 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC6-IN-803118852-74-4HDACHistone deacetylasesIL-6BV2 microglial cellsCOX-2iNOSchemotherapy-induced peripheral neuropathyinflammatory painHDAC6microgliamiceTNF-αInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-182777
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