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 (3)
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.

Compound Libraries

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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.

Select a batch to recalculate based on the batch molecular weight:
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 products' biological activity.

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 PMID:


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Keywords: HC067047 trpv4 transient receptor potential channels potent selective antagonists TRPV

3 Citations for HC 067047

Citations are publications that use Tocris products. Selected citations for HC 067047 include:

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

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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Pathways for HC 067047

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