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S83042

ACY-738

源叶(MedMol) 99%
  • 英文名:
  • ACY-738
  • 别名:
  • CAS号:
  • 1375465-91-0
  • 分子式:
  • C14H14N4O2
  • 分子量:
  • 270.2866
  • 核磁/质谱:
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源叶(MedMol) S83042-5mg 99% ¥1130.00元 6 - - - EA 加入购物车
源叶(MedMol) S83042-10mg 99% ¥1330.00元 6 - - - EA 加入购物车
源叶(MedMol) S83042-25mg 99% ¥2450.00元 6 - - - EA 加入购物车
源叶(MedMol) S83042-50mg 99% ¥4100.00元 预计交期:2-3天 - - - EA 加入购物车
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参考文献

质检证书(COA)

摩尔浓度计算器

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  • 提示:详情请下载说明书。
  • 产品描述: ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
  • 靶点: HDAC6:1.7 nM (IC50);HDAC1:94 nM (IC50);HDAC2:128 nM (IC50);HDAC3:218 nM (IC50);HDAC
  • 体外研究:
    ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells. ACY-738 (10 μM) induces cell death comparable to LBH589 and FK228
  • 体内研究:
    ACY-738 (5 mg/kg) leads to significant increase in α-tubulin acetylation in whole-brain lysates. ACY-738 (50 mg/kg) fails to produce an enhancement of locomotor activity in WT mice tested in a home cage environment. ACY-738 (5 mg/kg) reaches a maximum plasma concentration of 1310 ng/mL at 0.0830 h following treatment. ACY-738 (5 mg/kg BW) alters BM B cell differentiation, but shows no significant effect on IgG and C3 deposition in NZB/W mice. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels
  • 参考文献:
    1. Jochems J, et al. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400. 2. Regna NL, et al. Specific HDAC6 inhibition by ACY-738 reduces SLE pathogenesis in NZB/W mice. Clin Immunol. 2016 Jan;162:58-73. 3. Mithraprabhu S, et al. Histone deacetylase (HDAC) inhibitors as single agents induce multiple myeloma cell death principally through the inhibition of class I HDAC. Br J Haematol. 2013 Aug;162(4):559-62.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 3.7 ml 18.499 ml 36.998 ml
    5 mM 0.74 ml 3.7 ml 7.4 ml
    10 mM 0.37 ml 1.85 ml 3.7 ml
    50 mM 0.074 ml 0.37 ml 0.74 ml
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