RN-1734 - TRP Channel Antagonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERN-1734Cat. No.: HY-19975CAS No.: 946387-07-1分式: CHClNOS分量: 353.31作靶點(diǎn): TRP Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50

2、 mg/mL (141.52 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.8304 mL 14.1519 mL 28.3038 mL5 mM 0.5661 mL 2.8304 mL 5.6608 mL10 mM 0.2830 mL 1.4152 mL 2.8304 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，

3、建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3.25 mg/mL (9.20 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3.25 mg/mL (9.20 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubi

4、lity: 3.25 mg/mL (9.20 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 RN-1734種選擇性 TRPV4 通道拮抗劑，完全拮抗 4PDD 介導(dǎo)的 TRPV4 活化，作于 hTRPV4, mTRPV4,和 rTRPV4，IC50 分別為 2.3 M、5.9 M、3.2 M 1。RN-1734 能明顯降低腫瘤壞死因 (TNF-) 和細(xì)胞介素 1 (IL-1) 的產(chǎn)，不改變 olig2- 陽(yáng)性細(xì)胞的數(shù)量 2。IC50 & Target IC50

5、: 2.3 M (hTRPV4), 5.9 M (mTRPV4), 3.2 M (rTRPV4) 1體外研究 RN-1734 (27 hours; 10M) reverses the increase in the apoptotic rate of oligodendrocytes induced by CM(LPS-activated microglia group) apoptosis 2.RN-1734 (27 hours; 10M) alleviates CM-induced decreases in CNP 2.Apoptosis Analysis 2Cell Line: Micr

6、oglial cellsConcentration: 27 hoursIncubation Time: 10MResult: Significantly decreased the percentage of cleaved-caspase 3 positive cells.Western Blot Analysis 2Cell Line: Microglial cellsConcentration: 27 hoursIncubation Time: 10 MResult: Alleviated CM (with LPS only)-induced decreases in CNP.體內(nèi)研究

7、RN-1734 (0.5 l; microinjector pump; daily for 5 weeks) significantly reverses the decrease in CNP proteinand improves myelination in CPZ-induced demyelination mouse 2.Animal Model: CPZ-induced demyelination mouse model (C57BL/6 male mice) 2Dosage: 0.5 l (10 M in 5% DMSO and 0.9% NaCl)Administration:

8、 Microinjector pump for 5 weeksResult: Significantly reversed the decrease in CNP protein and improved myelination in CPZ-induced demyelination mouse.戶使本產(chǎn)品發(fā)表的科研獻(xiàn)2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE PLoS One. 2019 Jun 10;14(6):e0217511.See more customer validations on HYPERLINK / www.Med

9、ChemEREFERENCES1. Kato K, et al. Acidosis environment promotes osteoclast formation by acting on the last phase of preosteoclast differentiation: a study toelucidate the action points of acidosis and search for putative target molecules. Eur J Pharmacol. 2011 Aug 1;663(1-3):27-39.2. Vincent F, et al

10、. Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov20;389(3):490-4.3. Liu M, et al. TRPV4 Inhibition Improved Myelination and Reduced Glia Reactivity and Inflammation in a Cuprizone-Induced MouseModel of Demyelination. Front Cell Neurosci. 2018 Nov 5;12:392.McePdfHeightCaution: Product has not been fully val