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HC-067047 | TRPV4 blocker

CAS:
883031-03-6
Catalog Number:
10-1480
Activity:
TRPV4 blocker
Chemical Name:
2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Molecular Weight:
471.51
Molecular Formula:
C26H28F3N3O2
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 10 mg/ml).
Physical Properties:
white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

HC-067047 (883031-03-6) is a potent reversible and selective TRPV4 blocker. Active at mouse, human and rat TRPV4, IC50 = 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.1 Increases functional bladder capacity and reduces micturition frequency in mice and rats with cystitis.1 Inhibits brain edema in middle cerebral artery occlusion mice.2 HC-067047 induces an increase in core body temperature accompanied by increased oxygen consumption in Wistar rats.3 Active in vivo.

References/Citations:

1) 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. USA, 107 19084
2) Jie et al. (2015), Blockage of transient receptor potential vanilloid 4 inhibits brain edema in middle cerebral artery occlusion mice; Front. Cell. Neurosci., 9 141
3) Vizin et al. (2015), TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats; Acta Physiol. (Oxf.), 214 275

HC-067047 | TRPV4 blocker is also available in the Cellular Metabolism Library.
CAS:
883031-03-6
Catalog Number:
10-1480
Activity:
TRPV4 blocker
Chemical Name:
2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Molecular Weight:
471.51
Molecular Formula:
C26H28F3N3O2
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 10 mg/ml).
Physical Properties:
white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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