946387-07-1
中文名稱
2,4-二氯-N-(異丙基)-N-[2-[(異丙基)氨基]乙基]苯磺酰胺
英文名稱
2,4-dichloro-N-isopropyl-N-[2-(isopropylamino)ethyl]benzenesulfonamide
CAS
946387-07-1
分子式
C14H22Cl2N2O2S
分子量
353.31
MOL 文件
946387-07-1.mol
更新日期
2024/10/21 09:50:54
946387-07-1 結(jié)構(gòu)式
基本信息
中文別名
2,4-二氯-N-(異丙基)-N-[2-[(異丙基)氨基]乙基]苯磺酰胺 英文別名
RN 1734TRPV4 Antagonist I, RN-1734
TRPV4 Antagonist I, RN-1734 - CAS 946387-07-1 - Calbiochem
2,4-dichloro-N-isopropyl-N-[2-(isopropylamino)ethyl]benzenesulfonamide
2,4-dichloro-N-propan-2-yl-N-[2-(propan-2-ylamino)ethyl]benzenesulfonamide
2,4-Dichloro-N-isopropyl-N-(2-isopropylaminoethyl)benzenesulphonamide (RN-1734)
2,4-Dichloro-N-(1-methylethyl)-N-[2-[(1-methylethyl)amino]ethyl]benzenesulfonamide
Benzenesulfonamide, 2,4-dichloro-N-(1-methylethyl)-N-[2-[(1-methylethyl)amino]ethyl]-
所屬類別
生物化工：激動(dòng)劑抑制劑常見問題列表
生物活性
RN-1734 (TRPV4 Antagonist I)是一種選擇性的 transient receptor potential vanilloid 4 (TRPV4) 拮抗劑，對(duì)于hTRPV4、mTRPV4和rTRPV4的IC50值分別為2.3 μM、5.9 μM和3.2 μM。RN-1734 在不改變olig2陽性細(xì)胞數(shù)量的情況下，可減輕脫髓鞘作用并抑制神經(jīng)膠質(zhì)活化以及抑制 tumor necrosis factor α (TNF-α) 和 interleukin 1β (IL-1β) 的產(chǎn)生。靶點(diǎn)
| 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 |
體外研究
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. |
體內(nèi)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. |