Home / TRPV Antagonists / HC 067047

HC 067047

Catalog #: 4100
26 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4100/10
4100/50
HC 067047 | CAS No. 883031-03-6 | TRPV Antagonists
1 Image
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%

Product Details
Citations (26)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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

M.Wt:
471.51
Formula:
C26H28F3N3O2
Solubility:
Soluble to 100 mM in DMSO and to 25 mM in ethanol
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
883031-03-6

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.

Background References

  1. Involvement of TRPV4 in Serotonin-Evoked Scratching.
    Akiyama T, Ivanov M, Nagamine M, Davoodi A, Carstens M, Ikoma A, Cevikbas F, Kempkes C, Buddenkotte J, Steinhoff M, Carstens E
    J Invest Dermatol, 2016;136(1):154-60.
  2. Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.
    Everaerts et al.
    Proc.Natl.Acad.Sci., 2010;107:19084

Product Datasheets

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Citations for HC 067047

The citations listed below are publications that use Tocris products. Selected citations for HC 067047 include:

26 Citations: Showing 1 - 10

  1. TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats.
    Authors: Vizin
    Acta Physiol  ;214:275
  2. Assessing the Potency of the Novel Tocolytics 2-APB, Glycyl-H-1152, and HC-067047 in Pregnant Human Myometrium.
    Authors: Roger Et al.
    Reprod Sci  2023;30:203-220
  3. Piezo1-mediated stellate cell activation causes pressure-induced pancreatic fibrosis in mice.
    Authors: Steven R Et al.
    JCI Insight  2022;7
  4. Endothelial cells promote smooth muscle cell resilience to H2 O2 -induced cell death in mouse cerebral arteries.
    Authors: Rebecca L Et al.
    Acta Physiol (Oxf)  2022;235:e13819
  5. The Role of Transient Receptor Potential A1 and G Protein-Coupled Receptor 39 in Zinc-Mediated Acute and Chronic Itch in Mice.
    Authors: Tong Et al.
    Front Mol Neurosci  2022;14:768731
  6. Formalin Itch Test: Low-Dose Formalin Induces Histamine-Independent, TRPA1-Mediated Itch in Mice.
    Authors: Tong Et al.
    Front Med (Lausanne)  2021;8:627725
  7. Astrocytes regulate ultra-slow arteriole oscillations via stretch-mediated TRPV4-COX-1 feedback.
    Authors: Minh Dang Et al.
    Cell Rep  2021;36:109405
  8. The Effects of the Anti-aging Protein Klotho on Mucociliary Clearance.
    Authors: Stefanie Et al.
    Front Med (Lausanne)  2020;6:339
  9. VEGF-B Is an Autocrine Gliotrophic Factor for Müller Cells under Pathologic Conditions.
    Authors: Heping Et al.
    Invest Ophthalmol Vis Sci  2020;61:35
  10. Female sex and Western-style diet protect mouse resistance arteries during acute oxidative stress.
    Authors: Charles E Et al.
    Am J Physiol Cell Physiol  2020;318:C627-C639
  11. Piezo1 acts upstream of TRPV4 to induce pathological changes in endothelial cells due to shear stress.
    Authors: Rodger A Et al.
    J Biol Chem  2020;296:100171
  12. TRPV4 channel opening mediates pressure-induced pancreatitis initiated by Piezo1 activation.
    Authors: Stephen J Et al.
    J Clin Invest  2020;130:2527-2541
  13. Cell sensing and decision-making in confinement: The role of TRPM7 in a tug of war between hydraulic pressure and cross-sectional area.
    Authors: Zhao Et al.
    Sci Adv  2019;5:eaaw7243
  14. TRPV4 is the temperature-sensitive ion channel of human sperm.
    Authors: Mundt Et al.
    Elife  2018;7
  15. Pharmacological activation of TRPV4 produces immediate cell damage and induction of apoptosis in human melanoma cells and HaCaT keratinocytes.
    Authors: Olivan-Viguera
    PLoS One  2018;13:e0190307
  16. Functional cooperation between KCa3.1 and TRPV4 channels in bronchial smooth muscle cell proliferation associated with chronic asthma.
    Authors: Yu
    Front. Pharmacol  2017;8:559
  17. Hypotonic stress induces RANKL via transient receptor potential melastatin 3 (TRPM3) and vaniloid 4 (TRPV4) in human PDL cells.
    Authors: Son Et al.
    J Dent Res  2015;94:473
  18. Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction.
    Authors: Kim Et al.
    Nat Chem Biol  2015;35:8245
  19. Eugenol dilates mesenteric arteries and reduces systemic BP by activating endothelial cell TRPV4 channels.
    Authors: Qian Et al.
    Br J Pharmacol  2015;172:3484-94
  20. Intravesical TRPV4 blockade reduces repeated variate stress-induced bladder dysfunction by increasing bladder capacity and decreasing voiding frequency in male rats.
    Authors: Merrill and Vizzard
    Am J Physiol Regul Integr Comp Physiol  2014;307:R471
  21. TRPV4-mediated calcium influx and ciliary activity in human native airway epithelial cells.
    Authors: Lisa Et al.
    Basic Clin Pharmacol Toxicol  2014;114:210-6
  22. Novel therapeutic strategy to prevent chemotherapy-induced persistent sensory neuropathy by TRPA1 blockade.
    Authors: Trevisan Et al.
    Cancer Res  2013;73:3120
  23. Phosphatidylinositol-4,5-biphosphate-dependent rearrangement of TRPV4 cytosolic tails enables channel activation by physiological stimuli.
    Authors: Garcia-Elias Et al.
    Proc Natl Acad Sci U S A  2013;110:9553
  24. Hypotonicity-induced TRPV4 function in renal collecting duct cells: modulation by progressive cross-talk with Ca2+-activated K+ channels.
    Authors: Jin Et al.
    Cell Calcium  2012;51:131
  25. TRPV4 in porcine lens epithelium regulates hemichannel-mediated ATP release and Na-K-ATPase activity.
    Authors: Shahidullah Et al.
    Am J Physiol Cell Physiol  2012;302:C1751
  26. Mechanotransductional basis of endothelial cell response to intravascular bubbles.
    Authors: Klinger Et al.
    Integr Biol (Camb)  2011;3:1033

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