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SML0143

HC-067047

Name: HC-067047
Brand: SIGMA

≥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:

883031-03-6

Molecular Weight:

471.51

UNSPSC Code:

12352200

PubChem Substance ID:

329825191

NACRES:

NA.77

MDL number:

MFCD01571257

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

desiccated

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Product Name

HC-067047, ≥98% (HPLC)

Quality Level

100

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

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Bioactive Small Molecules

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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The transient receptor potential vanilloid 4 channel modulates uterine tone during pregnancy.

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

Functional Cooperation between KCa3.1 and TRPV4 Channels in Bronchial Smooth Muscle Cell Proliferation Associated with Chronic Asthma.

Zhihua Yu et al.

Frontiers in pharmacology, 8, 559-559 (2017-10-04)

Airway smooth muscle cells (SMC) proliferation contributes to the airways remodeling and irreversible airway obstruction during severe asthma, but the mechanisms of airway SMC proliferation are poorly understood. Intracellular Ca

TRPV4 channels contribute to renal myogenic autoregulation in neonatal pigs.

Hitesh Soni et al.

American journal of physiology. Renal physiology, 313(5), F1136-F1148 (2017-08-05)

Myogenic response, a phenomenon in which resistance size arteries and arterioles swiftly constrict or dilate in response to an acute elevation or reduction, respectively, in intravascular pressure is a key component of renal autoregulation mechanisms. Although it is well established

Cell sensing and decision-making in confinement: The role of TRPM7 in a tug of war between hydraulic pressure and cross-sectional area.

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

Optogenetic stimulation of phosphoinositides reveals a critical role of primary cilia in eye pressure regulation.

Philipp P Prosseda et al.

Science advances, 6(18), eaay8699-eaay8699 (2020-06-05)

Glaucoma is a group of progressive optic neuropathies that cause irreversible vision loss. Although elevated intraocular pressure (IOP) is associated with the development and progression of glaucoma, the mechanisms for its regulation are not well understood. Here, we have designed

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Global Trade Item Number

SKU	GTIN
SML0143-25MG	04061833027257
SML0143-5MG	04061837076978

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