HC 067047

Pricing Availability Delivery Time Qty
Cat.No. 4100 - HC 067047 | C26H28F3N3O2 | CAS No. 883031-03-6
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)
Datasheet
Citations (9)
Reviews (2)
Literature

Biological Activity

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.15 100
ethanol 11.79 25

Preparing Stock Solutions

The following data is based on the product molecular weight 471.51. Batch specific molecular weights may vary from batch to batch due to solvent 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

Safety Datasheet

References

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

9 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

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

Trevisan et al (2013) Novel therapeutic strategy to prevent chemotherapy-induced persistent sensory neuropathy by TRPA1 blockade. Cancer Res 73 3120 PMID: 23477783

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

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

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

Kim et al (2015) Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction. Nat Chem Biol 35 8245 PMID: 26019339

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

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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.

PMID: 28768667 Reference
review image

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.

PMID: 25832173 Reference
review image

Literature in this Area

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