MW 471.5 Da, Purity >99%. Potent and selective reversible TRPV4 antagonist (IC50 values are 17, 48 and 133 nM for mouse, human and rat orthologs, respectively.) Potently inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM). Shows antivasoconstrictive effects in vivo.
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Key facts
- CAS number
- 883031-03-6
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 471.5 Da
- Molecular formula
- C26H28F3N3O2
- PubChem identifier
- 2742550
- Nature
- Synthetic
Target data
Alternative names
BCYM3, CMT2C, HMSN2C, OSM9 like transient receptor potential channel 4, OTRPC 4, Osm-9-like TRP channel 4, Osmosensitive transient receptor potential channel 4, SMAL, SPSMA, SSQTL1, TRP 12, TRPV4_HUMAN, Transient receptor potential cation channel subfamily V member 4, Transient receptor potential protein 12, VR 4, VR-OAC, VRL-2, Vanilloid receptor-like channel 2, Vanilloid receptor-like protein 2, Vanilloid receptor-related osmotically-activated channel
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MW 471.5 Da, Purity >99%. Potent and selective reversible TRPV4 antagonist (IC50 values are 17, 48 and 133 nM for mouse, human and rat orthologs, respectively.) Potently inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM). Shows antivasoconstrictive effects in vivo.
Key facts
- CAS number
- 883031-03-6
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 471.5 Da
- Molecular formula
- C26H28F3N3O2
- PubChem identifier
- 2742550
- Nature
- Synthetic
- Solubility
Soluble in ethanol to 50 mM and in DMSO to 100 mM.
- Biochemical name
- 2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
- Biological description
Potent and selective reversible TRPV4 antagonist (IC50 values are 17, 48 and 133 nM for mouse, human and rat orthologs, respectively.) Potently inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM). Shows antivasoconstrictive effects in vivo.
- Canonical SMILES
- CC1=C(C=C(N1CCCN2CCOCC2)C3=CC=CC=C3)C(=O)NC4=CC=CC(=C4)C(F)(F)F
- InChI
- 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)
- InChIKey
- NCZYSQOTAYFTNM-UHFFFAOYSA-N
- IUPAC name
- 2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
TRPV4 also known as transient receptor potential vanilloid 4 is an ion channel protein that plays a mechanical role in the human body. This protein with a mass of approximately 98 kDa is sensitive to osmotic pressure mechanical forces and temperature changes. It acts as a calcium-permeable non-selective cation channel. TRPV4 is widely expressed in various tissues including the choroid plexus as well as in the epithelial cells endothelium and certain neurons. The expression pattern suggests its involvement in various physiological processes.
- Biological function summary
TRPV4 serves functions essential for osmoregulation mechanosensation and thermosensation. It often forms a complex with other proteins to modulate calcium influx which influences cellular responses. TRPV4 impacts various biological processes such as maintaining cell volume and adapting to temperature changes. Its role in regulating fluid movement across barriers like those in the choroid plexus demonstrates its involvement in maintaining homeostasis. These interactions highlight the protein's widespread influence on various cellular functions.
- Pathways
TRPV4 integrates into critical signal transduction pathways that include the mechanotransduction and osmoregulation pathways. It is closely related to other TRP family members such as TRPV1 and TRPC1 within these pathways. The mechanotransduction pathway allows it to convey mechanical stimuli into electrochemical activity impacting various systems throughout the body. The osmoregulation pathway highlights its ability to sense and respond to osmotic shifts maintaining cellular and systemic equilibrium.
- Associated diseases and disorders
TRPV4 has significant links to a range of pathologies such as skeletal dysplasias and neuropathies. Mutations in TRPV4 can lead to altered channel function contributing to conditions like Charcot-Marie-Tooth disease and congenital distal spinal muscular atrophy. These associations often involve the misregulation of calcium homeostasis where TRPV4's interaction with proteins like TRPV1 leads to a disruption of normal cellular processes highlighting the importance of maintaining TRPV4's proper function to prevent those diseases.
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1 product image
Chemical Structure - HC 067047, TRPV4 antagonist (ab145868)
2D chemical structure image of ab145868, HC 067047, TRPV4 antagonist
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