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616521

Sigma-Aldrich

TRPV4 Antagonist II, HC-067047

The TRPV4 Antagonist II, HC-067047 controls the biological activity of TRPV4.

Synonym(s):

TRPV4 Antagonist II, HC-067047, 2-Methyl-1-(3-morpholinopropyl)-5-phenyl-N-(3-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide, Transient Receptor Potential Vanilloid-4 Antagonist II, HC067047, HC067047, 2-Methyl-1-(3-morpholinopropyl)-5-phenyl-N-(3-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide, Transient Receptor Potential Vanilloid-4 Antagonist II

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About This Item

Empirical Formula (Hill Notation):
C26H28F3N3O2
CAS Number:
883031-03-6
Molecular Weight:
471.51
MDL number:
MFCD01571257
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 50 mg/mL, clear, colorless

shipped in

ambient

storage temp.

2-8°C

General description

A pyrrolocarboxamide compound that potently antagonizes TRP (transient receptor potential) family cation channel TRPV4 activity (IC50 = 17, 48, and 133 nM, respectively, against mouse, human, or rat TRPV4 in whole cell voltage-gated current measurement) in a reversible manner, displaying much reduced potency against human ERG and TRPM8 (IC50 = 368 and 780 nM, respectively) and little or no activity toward hKv1.3, hTRPA1, hTRPC5, hTRPV1/2/3/6, mTRPM7, mTRPV2, or rKv1.2. HC-067047 is efficacious (10 mg/kg via i.p.) in reducing micturition (urination) frequency and increasing voided urine volume of mice and rats suffering from CPA- (Cat. No. 239785) induced cystitis in vivo.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Everaerts, W., et al. 2010. Proc. Natl. Acad. Sci. USA107, 19084.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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