| 产品描述: | RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells |
| 靶点: |
IC50: 2.3 μM (hTRPV4), 5.9 μM (mTRPV4), 3.2 μM (rTRPV4);TRP/TRPVChannel |
| 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. |
| 参考文献: |
1. Kato K, et al. 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. Eur J Pharmacol. 2011 Aug 1;663(1- 2. Liu M, et al. TRPV4 Inhibition Improved Myelination and Reduced Glia Reactivity and Inflammation in a Cuprizone-Induced Mouse Model of Demyelination. Front Cell Neurosci. 2018 Nov 5;12:392. 3. Vincent F, et al. Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov 20;389(3):490-4. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
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 |
| 50 mM |
0.057 ml |
0.283 ml |
0.567 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |