HC-067047

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HC-067047  纯度: 99.36%

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。

HC-067047

HC-067047 Chemical Structure

CAS No. : 883031-03-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥726 In-stock
5 mg ￥660 In-stock
10 mg ￥1100 In-stock
25 mg ￥2400 In-stock
50 mg ￥4400 In-stock
100 mg ￥7700 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

HC-067047 相关产品

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生物活性

HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

471.51

Formula

C26H28F3N3O2
CAS 号

883031-03-6
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
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (106.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Everaerts W et al. Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.Proc Natl Acad Sci U S A. 2010 Nov 2;107(44):19084-9.

    [2]. Xing Y, et al. Decreased Expression of TRPV4 Channels in HEI-OC1 Cells Induced by High Glucose Is Associated with Hearing Impairment. Yonsei Med J. 2018 Nov;59(9):1131-1137.

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