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ACY-738
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ACY-738图片
CAS NO:1375465-91-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 270.29
Formula C14H14N4O2
CAS No. 1375465-91-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 32 mg/mL
Water: <1 mg/mL
Ethanol:
SMILES Code O=C(C1=CN=C(NC2(C3=CC=CC=C3)CC2)N=C1)NO
Synonyms ACY738; ACY 738; ACY-738
实验参考方法
In Vitro

In vitro activity: 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


Kinase Assay: ACY-738 is a novel, potent, selective, brain penetrable and orally-bioavailable HDAC6 inhibitor with an IC50s of 1.7 nM; it also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.


Cell Assay: ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells.

In VivoACY-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.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
Animal model Mice
Formulation & Dosage 5, 20, 50 mg/kg; i.p. and p.o.
References Neuropsychopharmacology. 2014 Jan;39(2):389-400.Br J Haematol. 2013 Aug;162(4):559-62.Clin Immunol. 2016 Jan;162:58-73.