HC 067047
目录号 : GC12260
HC 067047是TRPV4通道的选择性拮抗剂，对人、大鼠和小鼠TRPV4的IC50分别为48±6nM, 133±25nM和17±3nM。
Cas No.:883031-03-6
Sample solution is provided at 25 µL, 10mM.
HC 067047 is a selective antagonist of the TRPV4 channel. HC 067047 exhibits IC50 values of 48±6nM, 133±25nM and 17±3nM against human, rat, and mouse TRPV4 channels, respectively[1].
In vitro, HC 067047 (1μM; 5min) reduces mechanoactivated currents in Schwann cells[2]. HC 067047 (1μM; 30min) reversed the hypoxia/reoxygenation (H/R)-induced elevation of intracellular Ca2+ concentration ([Ca²⁺]ᵢ) and cell injury[3].
In vivo, HC 067047 (1mg/kg; 5 weeks; s.c.) prevented the development of mechanical, but not thermal cold allodynia in diabetic mice[4]. Treatment with the selective TRPV4 antagonist HC 067047 (5, 10 and 20mg/kg; i.p.) significantly attenuated myocardial ischemia/reperfusion (I/R) injury[5]. HC 067047 (10mg/kg; i.p.) exerts protective effects against RB-induced lung injury[6].
References:
[1] Everaerts W, Zhen X, Ghosh D, Vriens J, Gevaert T, Gilbert JP, Hayward NJ, McNamara CR, Xue F, Moran MM, Strassmaier T, Uykal E, Owsianik G, Vennekens R, De Ridder D, Nilius B, Fanger CM, Voets T. 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] Mulpuri Y, Tu NH, Inoue K, Harden G, Nicholson SJ, Seenauth A, Huang Y, Escobar KG, Moayedi Y, Bunnett NW, Albertson DG, Schmidt BL. TRPV4 activation in Schwann cells mediates mechanically induced pain of oral cancer. Front Pain Res (Lausanne). 2025 Mar 12;6:1532885.
[3] Wu QF, Qian C, Zhao N, Dong Q, Li J, Wang BB, Chen L, Yu L, Han B, Du YM, Liao YH. Activation of transient receptor potential vanilloid 4 involves in hypoxia/reoxygenation injury in cardiomyocytes. Cell Death Dis. 2017 May 25;8(5):e2828.
[4] Dias FC, Alves VS, Matias DO, Figueiredo CP, Miranda ALP, Passos GF, Costa R. The selective TRPV4 channel antagonist HC-067047 attenuates mechanical allodynia in diabetic mice. Eur J Pharmacol. 2019 Aug 5;856:172408.
[5] Dong Q, Li J, Wu QF, Zhao N, Qian C, Ding D, Wang BB, Chen L, Guo KF, Fu D, Han B, Liao YH, Du YM. Blockage of transient receptor potential vanilloid 4 alleviates myocardial ischemia/reperfusion injury in mice. Sci Rep. 2017 Feb 16;7:42678.
[6] Toumpanakis D, Chatzianastasiou A, Vassilakopoulou V, Mizi E, Dettoraki M, Perlikos F, Giatra G, Mikos N, Theocharis S, Vassilakopoulos T. TRPV4 Inhibition Exerts Protective Effects Against Resistive Breathing Induced Lung Injury. Int J Chron Obstruct Pulmon Dis. 2022 Feb 15;17:343-353.
HC 067047是TRPV4通道的选择性拮抗剂，对人、大鼠和小鼠TRPV4的IC50分别为48±6nM, 133±25nM和17±3nM[1]。
在体外，HC 067047 (1μM; 5min)可抑制施万细胞中的机械激活电流[2]；HC 067047 (1μM; 30min)能逆转缺氧/复氧(H/R)引起的细胞内钙离子浓度([Ca²⁺]ᵢ)升高及细胞损伤[3]。
在体内，HC 067047 (1mg/kg; 5周; 皮下注射)可预防糖尿病小鼠机械性痛觉异常的发生，但对冷痛觉异常无效[4]；选择性TRPV4拮抗剂 HC 067047 (5, 10 and 20mg/kg; 腹腔注射)显著减轻心肌缺血/再灌注(I/R)损伤[5]。HC 067047 (10mg/kg; 腹腔注射)对辐射所致肺损伤亦具有保护作用[6]。
| Cell experiment [1]: | |
Cell lines | NRVM and H9C2 cells |
Preparation Method | NRVM and H9C2 cells, pretreated with 1μM HC 067047 for 30min, were loaded with 2μM Fluo-4/AM for 30min and then washed three times with HEPES buffer. Cells in 96-well plates were excited at 488nm and fluorescence emissions at 525nm were recorded using the Enspire Multimode Plate Reader. |
Reaction Conditions | 1μM; 30min |
Applications | HC 067047 reversed the hypoxia/reoxygenation (H/R)-induced elevation of intracellular Ca2+ concentration ([Ca2+]ᵢ) and cell injury. |
| Animal experiment [2]: | |
Animal models | Male Swiss mice (5-10 weeks) |
Preparation Method | In order to assess the effect of the selective TRPV4 channel antagonist HC 067047 on the development of mechanical and cold allodynia, the drug was subcutaneously injected once a day, at the dose of 1mg/kg, between 2 and 6 weeks after diabetes induction. Control animals received vehicle (1% DMSO and 0.25% Tween 80 in saline solution). Mechanical and thermal cold allodynia were assessed in the sixth week of the experimental protocol. |
Dosage form | 1mg/kg; 5 weeks; s.c. |
Applications | HC 067047 prevented the development of mechanical, but not thermal cold allodynia in diabetic mice. |
References: | |
| Cas No. | 883031-03-6 | SDF | |
| 化学名 | 2-methyl-1-(3-morpholinopropyl)-5-phenyl-N-(3-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide | ||
| Canonical SMILES | FC(F)(C1=CC(NC(C2=C(C)N(C(C3=CC=CC=C3)=C2)CCCN4CCOCC4)=O)=CC=C1)F | ||
| 分子式 | C26H28F3N3O2 | 分子量 | 471.51 |
| 溶解度 | ≥ 47.2mg/mL in DMSO | 储存条件 | Store at -20°C |
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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 |
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