货号	规格	价格	上海	北京	珠海	重庆	武汉
S83042-5mg买3赠1	99.20%	￥800.00 S83042-5mg ￥800.00 现货（买3赠1）	6 6	-	-	-	-
S83042-10mg促销	99.20%	￥1050.00 ￥840.00 S83042-10mg ￥840.00 现货	5 5	-	-	-	-
S83042-25mg促销	99.20%	￥2000.00 ￥1600.00 S83042-25mg ￥1600.00 现货	5 5	-	-	-	-
S83042-50mg促销	≥99%	￥3200.00 ￥2560.00 S83042-50mg ￥2560.00 2-3天	0 货期：2-3天	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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