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Submit ReviewHC 067047
Description: Potent and selective TRPV4 antagonist
Chemical Name: 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Purity: ≥99% (HPLC)
Biological Activity 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.
Technical Data for HC 067047
| M. Wt | 471.51 |
| Formula | C26H28F3N3O2 |
| Storage | Store at +4°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for HC 067047
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.15 | 100 | |
| ethanol | 11.79 | 25 |
Preparing Stock Solutions for HC 067047
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for HC 067047
References for HC 067047
References are publications that support the biological activity of the product.
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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Keywords: HC 067047, HC 067047 supplier, HC067047, trpv4, transient, receptor, potential, channels, potent, selective, antagonists, TRPV, 4100, Tocris Bioscience
26 Citations for HC 067047
Citations are publications that use Tocris products. Selected citations for HC 067047 include:
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
Do you know of a great paper that uses HC 067047 from Tocris? Please let us know.
Reviews for HC 067047
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HC067047 inhibit TRPV4 channels in pig pregromerular arteries.
By
Jennifer Neves on 01/23/2018
Assay Type: In Vitro
Species: Other
Cell Line/Tissue: 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
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: 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.
