RN-1734 是一种选择性TRPV4通道拮抗剂，完全拮抗 4αPDD 介导的 TRPV4 活化，作用于 hTRPV4, mTRPV4, 和 rTRPV4，IC50分别为 2.3 μM、5.9 μM、3.2 μM。RN-1734 能明显降低肿瘤坏死因子 α (TNF-α) 和白细胞介素 1β (IL-1β) 的产生，而不改变 olig2- 阳性细胞的数量。
| 生物活性 | RN-1734 is selective antagonist of theTRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolarIC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM)[1]. 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[2]. |
| IC50& Target | IC50: 2.3 μM (hTRPV4), 5.9 μM (mTRPV4), 3.2 μM (rTRPV4)[1] |
体外研究
(In Vitro) | RN-1734 (27 hours; 10μM) reverses the increase in the apoptotic rate of oligodendrocytes induced by CM (LPS-activated microglia group) apoptosis[2].
RN-1734 (27 hours; 10μM) alleviates CM-induced decreases in CNP[2].
Apoptosis Analysis[2] | Cell Line: | Microglial cells | | Concentration: | 27 hours | | Incubation Time: | 10μM | | Result: | Significantly decreased the percentage of cleaved-caspase 3 positive cells. |
Western Blot Analysis[2] | Cell Line: | Microglial cells | | Concentration: | 27 hours | | Incubation Time: | 10 μM | | Result: | Alleviated CM (with LPS only)-induced decreases in CNP. |
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体内研究
(In Vivo) | 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[2].
| Animal Model: | CPZ-induced demyelination mouse model (C57BL/6 male mice)[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(70.76 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.8304 mL | 14.1519 mL | 28.3038 mL | | 5 mM | 0.5661 mL | 2.8304 mL | 5.6608 mL | | 10 mM | 0.2830 mL | 1.4152 mL | 2.8304 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 3.25 mg/mL (9.20 mM); Clear solution
此方案可获得 ≥ 3.25 mg/mL (9.20 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 3.25 mg/mL (9.20 mM); Clear solution
此方案可获得 ≥ 3.25 mg/mL (9.20 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 3.25 mg/mL (9.20 mM); Clear solution
此方案可获得 ≥ 3.25 mg/mL (9.20 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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