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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
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Keywords: HC 067047, HC 067047 supplier, HC067047, trpv4, transient, receptor, potential, channels, potent, selective, antagonists, TRPV, 4100, Tocris Bioscience
13 Citations for HC 067047
Citations are publications that use Tocris products. Selected citations for HC 067047 include:
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
Trevisan et al (2013) Novel therapeutic strategy to prevent chemotherapy-induced persistent sensory neuropathy by TRPA1 blockade. Cancer Res 73 3120 PMID: 23477783
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
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
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
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
Klinger et al (2011) Mechanotransductional basis of endothelial cell response to intravascular bubbles. Integr Biol (Camb) 3 1033 PMID: 21931900
Vizin TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats. Acta Physiol 214 275 PMID: 25739906
Mundt et al (2018) TRPV4 is the temperature-sensitive ion channel of human sperm. Elife 7 PMID: 29963982
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
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Reviews for HC 067047
Average Rating: 5 (Based on 2 Reviews.)
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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.
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