2,4-二氯-N-(异丙基)-N-[2-[(异丙基)氨基]乙基]苯磺酰胺

生物活性靶点体外研究体内研究 2,4-二氯-N-(异丙基)-N-[2-[(异丙基)氨基]乙基]苯磺酰胺试剂级价格

CAS号:946387-07-1
英文名:2,4-dichloro-N-isopropyl-N-[2-(isopropylamino)ethyl]benzenesulfonamide
中文名:2,4-二氯-N-(异丙基)-N-[2-[(异丙基)氨基]乙基]苯磺酰胺
CBNumber:CB11529521
分子式:C14H22Cl2N2O2S
分子量:353.31
MOL File:946387-07-1.mol

2,4-二氯-N-(异丙基)-N-[2-[(异丙基)氨基]乙基]苯磺酰胺化学性质

储存条件 :2-8°C
溶解度 :DMSO: >20mg/mL
形态 :Yellow solid
颜色 :white to off-white

安全信息

WGK Germany :nwg

2,4-二氯-N-(异丙基)-N-[2-[(异丙基)氨基]乙基]苯磺酰胺性质、用途与生产工艺

生物活性 RN-1734 (TRPV4 Antagonist I)是一种选择性的 transient receptor potential vanilloid 4 (TRPV4) 拮抗剂，对于hTRPV4、mTRPV4和rTRPV4的IC50值分别为2.3 μM、5.9 μM和3.2 μM。RN-1734 在不改变olig2阳性细胞数量的情况下，可减轻脱髓鞘作用并抑制神经胶质活化以及抑制 tumor necrosis factor α (TNF-α) 和 interleukin 1β (IL-1β) 的产生。
靶点
Target Value
TNF-α
()
IL-1β
()
hTRPV4
(Cell-free assay) 2.3 μM
rTRPV4
(Cell-free assay) 3.2 μM
mTRPV4
(Cell-free assay) 5.9 μM

体外研究

RN-1734 (27 hours; 10μM) reverses the increase in the apoptotic rate of oligodendrocytes induced by CM (LPS-activated microglia group) apoptosis.
RN-1734 (27 hours; 10μM) alleviates CM-induced decreases in CNP.

Apoptosis Analysis

Cell Line:	Microglial cells
Concentration:	27 hours
Incubation Time:	10μM
Result:	Significantly decreased the percentage of cleaved-caspase 3 positive cells.

Western Blot Analysis

Cell Line:	Microglial cells
Concentration:	27 hours
Incubation Time:	10 μM
Result:	Alleviated CM (with LPS only)-induced decreases in CNP.

体内研究

RN-1734 (0.5 μl; microinjector pump; daily for 5 weeks) significantly reverses the decrease in CNP protein and improves myelination in CPZ-induced demyelination mouse.

Animal Model:	CPZ-induced demyelination mouse model (C57BL/6 male mice)
Dosage:	0.5 μl (10 μM in 5% DMSO and 0.9% NaCl)
Administration:	Microinjector pump for 5 weeks
Result:	Significantly reversed the decrease in CNP protein and improved myelination in CPZ-induced demyelination mouse.