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RN-1734

Catalog No. T7572 CAS 946387-07-1

RN-1734 is selective TRPV4 channel antagonist(IC50 of 2.3 μM,5.9 μM,3.2 μM for hTRPV4, mTRPV4 and rTRPV4,respectively)

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RN-1734, CAS 946387-07-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 51.00
10 mg	In stock	$ 74.00
25 mg	In stock	$ 163.00
50 mg	In stock	$ 277.00
100 mg	In stock	$ 413.00
500 mg	In stock	$ 937.00
1 mL * 10 mM (in DMSO)	In stock	$ 58.00

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Purity: 98%

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Description	RN-1734 is selective TRPV4 channel antagonist(IC50 of 2.3 μM,5.9 μM,3.2 μM for hTRPV4, mTRPV4 and rTRPV4,respectively)
Targets&IC50	TRPV4 (human):2.3 μM , TRPV4 (rat):3.2 μM, TRPV4 (mouse):5.9 μM
In vitro	In vitro, RN-1734 treatment clearly inhibited the influx of calcium and decreased the levels of IL-1β and TNF-α in lipopolysaccharide (LPS)-activated microglial cells by suppressing NF-κB P65 phosphorylation.?Apoptosis of oligodendrocyte induced by LPS-activated microglia was also alleviated by RN-1734.?Activation of TRPV4 in microglia is involved in oligodendrocyte apoptosis through the activation of the NF-κB signaling pathway, thus revealing a new mechanism of CNS demyelination[1].
Cell Research	LPS-treated microglial cells were further divided into a LPS group, a vehicle (DMSO treatment) group and a RN-1734 group.?The cells were treated with 1 μg/ml LPS (Sigma) or RN-1734 (10 μM) for 3 h .?Next, the cells were triple-washed with DMEM medium to remove LPS, and then incubated in DMEM with or without RN1734 for 24 h. Finally, the cells were collected for TRPV4 immunocytostaining, and the supernatant was collected separately for enzyme-linked immunosorbent assay (ELISA) or for the oligodendrocyte apoptosis experiment.?The supernatant of the microglial cells was mixed with DMEM/F12 at a ratio of 1:1.?The mixed medium without LPS was used for the control (Ctrl) group, the medium with LPS only was used for the conditional medium (CM) group, and the media with LPS and DMSO or RN-1734 were used for the CM-vehicle group and the CM-RN1734 group, respectively.?After oligodendrocytes grew for 2 days in 6-well plates in DMEM/F12 containing 10% FBS, the differentiation medium was replaced with the described Ctrl or different CM media for 24 h. Then, the cells were harvested for apoptosis analysis and western blot analysis separately[1].

Molecular Weight	353.31
Formula	C14H22Cl2N2O2S
CAS No.	946387-07-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (141.52 mM)

References and Literature

1. Meiying, Liu, Xuan, et al. TRPV4 Inhibition Improved Myelination and Reduced Glia Reactivity and Inflammation in a Cuprizone-Induced Mouse Model of Demyelination.[J]. Frontiers in cellular neuroscience, 2018. 2. Kato K , Morita I . Acidosis environment promotes osteoclast formation by acting on the last phase of preosteoclast differentiation: A study to elucidate the action points of acidosis and search for putative target molecules[J]. European Journal of Pharmacology, 2011, 663(1-3):27-39.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Neuronal Signaling Compound Library Ion Channel Inhibitor Library NO PAINS Compound Library ReFRAME Related Library

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Keywords

RN-1734 946387-07-1 Membrane transporter/Ion channel TRP/TRPV Channel Inhibitor Transient receptor potential channels TRP Channel RN 1734 RN1734 inhibit inhibitor

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