HC-067047 是一种有效的选择性TRPV4拮抗剂，可逆地抑制流经人，大鼠和小鼠TRPV4直系同源物的电流，IC50值分别为 48 nM，133 nM 和 17 nM。
| 生物活性 | HC-067047 is a potent and selectiveTRPV4antagonist and reversibly inhibits currents through the human, rat, and mouseTRPV4orthologs withIC50values of 48 nM, 133 nM, and 17 nM, respectively[1]. |
| IC50& Target | IC50: 48 nM (human TRPV4), 133 nM (rat TRPV4), 17 nM (mouse TRPV4)[1] |
体外研究
(In Vitro) | HC-067047 (1 μM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells[2].
HC-067047 (1 μM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein[2].
HC-067047 (1 μM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation[2].
HC-067047 (1 μM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis[2].
RT-PCR[2] | Cell Line: | HEI-OC1 cells | | Concentration: | 1 μM | | Incubation Time: | 24 hours | | Result: | The mRNA expression was significantly decreased. |
Western Blot Analysis[2] | Cell Line: | HEI-OC1 cells | | Concentration: | 1 μM | | Incubation Time: | 24 hours | | Result: | The expression of TRPV4 protein was significantly decreased. |
Cell Proliferation Assay[2] | Cell Line: | HEI-OC1 cells | | Concentration: | 1 μM | | Incubation Time: | 48 hours | | Result: | Inhibited cell proliferation. |
Apoptosis Analysis[2] | Cell Line: | HEI-OC1 cells | | Concentration: | 1 μM | | Incubation Time: | 48 hours | | Result: | Promoted cell apoptosis. |
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体内研究
(In Vivo) | HC-067047 (0-50 mg/kg; intraperitoneal injection; for 30 minutes; cyclophosphamide-treated WT and Trpv4–/–mice, and naive WT mice) treatment increases functional bladder capacity and reduces micturition frequency in WT mice with cystitis. HC-067047 do not affect bladder function in Trpv4–/–mice[1].
| Animal Model: | Cyclophosphamide-treated WT and Trpv4–/–mice, and naive WT mice[1] | | Dosage: | 0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg | | Administration: | Intraperitoneal injection; for 30 minutes | | Result: | Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4–/–mice. |
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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 : 50 mg/mL(106.04 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1208 mL | 10.6042 mL | 21.2085 mL | | 5 mM | 0.4242 mL | 2.1208 mL | 4.2417 mL | | 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 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: ≥ 2.5 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.30 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 25.0 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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