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Merck

SML0143

HC-067047

≥98% (HPLC), TRPV4 antagonist, powder

Synonym(s):

2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide

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About This Item

Empirical Formula (Hill Notation):
C26H28F3N3O2
CAS Number:
Molecular Weight:
471.51
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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Product Name

HC-067047, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to tan

solubility

DMSO: ≥15 mg/mL

storage temp.

2-8°C

SMILES string

CC1=C(C(NC2=CC(C(F)(F)F)=CC=C2)=O)C=C(C3=CC=CC=C3)N1CCCN4CCOCC4

InChI

1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33)

InChI key

NCZYSQOTAYFTNM-UHFFFAOYSA-N

Application

HC-067047 has been used as a transient receptor potential cation channel subfamily V member 4 (TRPV4) inhibitor:
  • to study its effects on organoid formation and proliferation in human endometrial tissues
  • to determine its effects on neuronal survival after intracerebral hemorrhage (ICH)
  • to study its effects on TRPV4 regulation of angiotensin II receptor type 1 (AT1R) task, phosphorylation and β-arrestin recruitment in choroid plexus

Biochem/physiol Actions

HC-067047 is a TRPV4 antagonist
HC-067047 is a potent, selective inhibitor of hTRPV4. The compound inhibits human, rat and mouse TRPV4 with IC50 values of 48, 133 and 17 nM, respectively. HC-067047 does not inhibit other TRPV isoforms at concentrations up to 5 μM. HC-067047 inhibits hERG channel and the menthol receptor TRPM8 with IC50 values of 370 and 780 nM, respectively.


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Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Lihua Ying et al.
Science translational medicine, 7(319), 319ra204-319ra204 (2015-12-25)
The importance of gaining insight into the mechanisms underlying uterine quiescence and contractility is highlighted by the absence of an effective strategy to prevent or treat preterm labor, the greatest cause of perinatal mortality and morbidity worldwide. Although current evidence
J Liu et al.
International endodontic journal, 52(11), 1617-1628 (2019-06-18)
To investigate the influence of tumour necrosis factor (TNF)-α on transient receptor potential channel vanilloid subfamily type 2 (TRPV2) and TRPV4 channels in human dental pulp cells (HDPCs), and explore the potential downstream signalling pathway mediating this process. Immunofluorescence staining
Runchen Zhao et al.
Science advances, 5(7), eaaw7243-eaaw7243 (2019-07-30)
How cells sense hydraulic pressure and make directional choices in confinement remains elusive. Using trifurcating Ψ-like microchannels of different hydraulic resistances and cross-sectional areas, we discovered that the TRPM7 ion channel is the critical mechanosensor, which directs decision-making of blebbing