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Submit ReviewHC 067047
说明： Potent and selective TRPV4 antagonist
化学名： 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
纯度： ≥99% (HPLC)
生物活性 for HC 067047
HC 067047 is a potent and selective TRPV4 antagonist. Reversibly inhibits currents through mouse, human and rat TRPV4 orthologs (IC50 values are 17, 48 and 133 nM respectively). Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM). Selective for TRPV4 over TRPV1, TRPV2, TRPV3 and TRPM8 channels.
技术数据 for HC 067047
| 分子量 | 471.51 |
| 公式 | C26H28F3N3O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 883031-03-6 |
| PubChem ID | 2742550 |
| InChI Key | NCZYSQOTAYFTNM-UHFFFAOYSA-N |
| Smiles | CC1=C(C(NC4=CC(C(F)(F)F)=CC=C4)=O)C=C(C3=CC=CC=C3)N1CCCN2CCOCC2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for HC 067047
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 47.15 | 100 | |
| ethanol | 11.79 | 25 |
制备储备液 for HC 067047
以下数据基于产品分子量 471.51。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.12 mL | 10.6 mL | 21.21 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.24 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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产品说明书 for HC 067047
参考文献 for HC 067047
参考文献是支持产品生物活性的出版物。
Everaerts et al (2010) Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis. Proc.Natl.Acad.Sci. 107 19084
If you know of a relevant reference for HC 067047, please let us know.
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关键词: HC 067047, HC 067047 supplier, HC067047, trpv4, transient, receptor, potential, channels, potent, selective, antagonists, TRPV, 4100, Tocris Bioscience
26 篇 HC 067047 的引用文献
引用文献是使用了 Tocris 产品的出版物。 HC 067047 的部分引用包括：
Mundt et al (2018) TRPV4 is the temperature-sensitive ion channel of human sperm. Elife 7 PMID: 29963982
Klinger et al (2011) Mechanotransductional basis of endothelial cell response to intravascular bubbles. Integr Biol (Camb) 3 1033 PMID: 21931900
Yu (2017) Functional cooperation between KCa3.1 and TRPV4 channels in bronchial smooth muscle cell proliferation associated with chronic asthma. Front. Pharmacol 8 559 PMID: 28970794
Kim et al (2015) Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction. Nat Chem Biol 35 8245 PMID: 26019339
Merrill and Vizzard (2014) Intravesical TRPV4 blockade reduces repeated variate stress-induced bladder dysfunction by increasing bladder capacity and decreasing voiding frequency in male rats. Am J Physiol Regul Integr Comp Physiol 307 R471 PMID: 24965792
Tong et al (2021) Formalin Itch Test: Low-Dose Formalin Induces Histamine-Independent, TRPA1-Mediated Itch in Mice. Front Med (Lausanne) 8 627725 PMID: 33681255
Minh Dang et al (2021) Astrocytes regulate ultra-slow arteriole oscillations via stretch-mediated TRPV4-COX-1 feedback. Cell Rep 36 109405 PMID: 34348138
Zhao et al (2019) Cell sensing and decision-making in confinement: The role of TRPM7 in a tug of war between hydraulic pressure and cross-sectional area. Sci Adv 5 eaaw7243 PMID: 31355337
Qian et al (2015) Eugenol dilates mesenteric arteries and reduces systemic BP by activating endothelial cell TRPV4 channels. Br J Pharmacol 172 3484-94 PMID: 25832173
Son et al (2015) Hypotonic stress induces RANKL via transient receptor potential melastatin 3 (TRPM3) and vaniloid 4 (TRPV4) in human PDL cells. J Dent Res 94 473 PMID: 25595364
Shahidullah et al (2012) TRPV4 in porcine lens epithelium regulates hemichannel-mediated ATP release and Na-K-ATPase activity. Am J Physiol Cell Physiol 302 C1751 PMID: 22492652
Jin et al (2012) Hypotonicity-induced TRPV4 function in renal collecting duct cells: modulation by progressive cross-talk with Ca2+-activated K+ channels. Cell Calcium 51 131 PMID: 22204737
Trevisan et al (2013) Novel therapeutic strategy to prevent chemotherapy-induced persistent sensory neuropathy by TRPA1 blockade. Cancer Res 73 3120 PMID: 23477783
Olivan-Viguera (2018) Pharmacological activation of TRPV4 produces immediate cell damage and induction of apoptosis in human melanoma cells and HaCaT keratinocytes. PLoS One 13 e0190307 PMID: 29293584
Lisa et al (2014) TRPV4-mediated calcium influx and ciliary activity in human native airway epithelial cells. Basic Clin Pharmacol Toxicol 114 210-6 PMID: 24034343
Rebecca L et al (2022) Endothelial cells promote smooth muscle cell resilience to H2 O2 -induced cell death in mouse cerebral arteries. Acta Physiol (Oxf) 235 e13819 PMID: 35380737
Tong et al (2022) The Role of Transient Receptor Potential A1 and G Protein-Coupled Receptor 39 in Zinc-Mediated Acute and Chronic Itch in Mice. Front Mol Neurosci 14 768731 PMID: 35095413
Steven R et al (2022) Piezo1-mediated stellate cell activation causes pressure-induced pancreatic fibrosis in mice. JCI Insight 7 PMID: 35451372
Roger et al (2023) Assessing the Potency of the Novel Tocolytics 2-APB, Glycyl-H-1152, and HC-067047 in Pregnant Human Myometrium. Reprod Sci 30 203-220 PMID: 35715551
Stefanie et al (2020) The Effects of the Anti-aging Protein Klotho on Mucociliary Clearance. Front Med (Lausanne) 6 339 PMID: 32039219
Heping et al (2020) VEGF-B Is an Autocrine Gliotrophic Factor for Müller Cells under Pathologic Conditions. Invest Ophthalmol Vis Sci 61 35 PMID: 32945843
Rodger A et al (2020) Piezo1 acts upstream of TRPV4 to induce pathological changes in endothelial cells due to shear stress. J Biol Chem 296 100171 PMID: 33298523
Stephen J et al (2020) TRPV4 channel opening mediates pressure-induced pancreatitis initiated by Piezo1 activation. J Clin Invest 130 2527-2541 PMID: 31999644
Charles E et al (2020) Female sex and Western-style diet protect mouse resistance arteries during acute oxidative stress. Am J Physiol Cell Physiol 318 C627-C639 PMID: 31891519
Garcia-Elias et al (2013) Phosphatidylinositol-4,5-biphosphate-dependent rearrangement of TRPV4 cytosolic tails enables channel activation by physiological stimuli. Proc Natl Acad Sci U S A 110 9553 PMID: 23690576
Vizin TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats. Acta Physiol 214 275 PMID: 25739906
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HC067047 inhibit TRPV4 channels in pig pregromerular arteries.
By
Jennifer Neves on 01/23/2018
分析类型： In Vitro
种属： Other
细胞系/组织： preglomerular arteries
HC067047 (1µM) was used to demonstrate that TRPV4 channels contribute to pressure-induced membrane depolarization, intracellular [Ca2+] elevation, and constriction in neonatal pig renal preglomerular arteries.
HC067047 to inhibit TRPV4 currents.
By
Jennifer Neves on 01/23/2018
分析类型： In Vitro
种属： Rat
细胞系/组织： mesenteric endothelial cells
HC067047 was used as a tool to demonstrate that eugenol activates TRPV4 currents in rat mesenteric artery endothelial cells using patch clamp electrophysiology.
