Molecular Formula | C14H22Cl2N2O2S |
Molar Mass | 353.31 |
Solubility | DMSO: >20mg/mL |
Appearance | Yellow solid |
Color | white to off-white |
Storage Condition | 2-8°C |
In vitro study | 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. |
In vivo study | 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. |
WGK Germany | nwg |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.833 ml | 14.164 ml | 28.329 ml |
5 mM | 0.567 ml | 2.833 ml | 5.666 ml |
10 mM | 0.283 ml | 1.416 ml | 2.833 ml |
5 mM | 0.057 ml | 0.283 ml | 0.567 ml |
biological activity | RN-1734 (TRPV4 Antagonist I) is a selective transient receptor potential vanilloid 4 (TRPV4) antagonist, and the IC50 values for hTRPV4, mTRPV4 and rTRPV4 are 2.3 μM, 5.9 μM and 3.2 μM respectively. RN-1734, without changing the number of olig2-positive cells, attenuated demyelination and inhibited glial activation as well as inhibition of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) production. |
target | TargetValue TNF-α () IL-1β () hTRPV4 (Cell-free assay) 2.3 μM rTRPV4 (Cell-free assay) 3.2 μM TRPV4 (Cell-free assay) 5.9 μM |
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 |
in vitro study | RN-1734 (27 hours; 10 μM) reverses the increase in the apoptotic rate of oligodendrocytes induced by CM (LPS-activated microglia group) apoptosis. RN-1734 (27 hours; 10 μM) alleviates CM-induced decreases in CNP. Apoptosis Analysis Cell Line: Microglial cells Concentration: 27 hours Incubation Time: 10 μM 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. |
Cell Line: | Microglial cells Microglial cells |
Concentration: | 27 hours 27 hours |
Incubation Time: | 10μM 10 μM |
Result: | Significantly decreased the percentage of cleaved-caspase 3 positive cells. Alleviated CM (with LPS only)-induced decreases in CNP. Significantly reversed the decrease in CNP protein and improved myelination in CPZ-induced demyelination mouse. |
in vivo research | 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. |
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 |