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219671

Sigma-Aldrich

CFTR Inhibitor II, GlyH-101

CFTR Inhibitor II, GlyH-101, CAS 328541-79-3, is a cell-permeable potent, selective and reversible open-channel blocker of CFTR (Ki = 4.3 µM in CFTR-expressing FRT cells).

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Synonym(s):
CFTR Inhibitor II, GlyH-101, N-(2-Naphthalenyl)-((3,5-dibromo-2,4-dihydroxyphenyl)methylene)glycine hydrazide
Empirical Formula (Hill Notation):
C19H15Br2N3O3
CAS Number:
Molecular Weight:
493.15

Quality Level

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

yellow

solubility

DMSO: 200 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C19H15Br2N3O3/c20-15-8-13(18(26)17(21)19(15)27)9-23-24-16(25)10-22-14-6-5-11-3-1-2-4-12(11)7-14/h1-9,22,26-27H,10H2,(H,24,25)/b23-9+

InChI key

RMBDLOATEPYBSI-NUGSKGIGSA-N

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This Item
219675219670219677
CFTR Inhibitor II, GlyH-101 CFTR Inhibitor II, GlyH-101, CAS 328541-79-3, is a cell-permeable potent, selective and reversible open-channel blocker of CFTR (Ki = 4.3 µM in CFTR-expressing FRT cells).

219671

CFTR Inhibitor II, GlyH-101

Sigma-Aldrich

219675

CFTR Inhibitor II, GlyH-101

CFTR Inhibitor-172 CFTR Inhibitor-172, CAS 307510-92-5, is a cell-permeable, potent, reversible, rapid, and voltage-independent inhibitor of CFTR-mediated Cl- transport in human airway cells (Ki ~ 300 nM).

219670

CFTR Inhibitor-172

CFTR Inhibitor IV, PPQ-102 The CFTR Inhibitor IV, PPQ-102, also referenced under CAS 931706-15-9, controls the biological activity of CFTR. This small molecule/inhibitor is primarily used for Neuroscience applications.

219677

CFTR Inhibitor IV, PPQ-102

assay

≥97% (HPLC)

assay

≥97% (HPLC)

assay

≥95% (HPLC)

assay

≥95% (HPLC)

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

−70°C

storage temp.

2-8°C

storage temp.

−20°C

solubility

DMSO: 200 mg/mL

solubility

-

solubility

DMSO: 5 mg/mL

solubility

DMSO: 5 mg/mL

General description

A cell-permeable glycinyl hydrazone compound that acts as a potent, selective and reversible open-channel blocker of CFTR with intermediate speed (<1 min; 95% inhibition at 50 µM; Ki = 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl- currents, and is effective in nasal and intestinal epithelia in vivo.
A cell-permeable glycinyl hydrazone compound that acts as a potent, selective and reversible open-channel blocker of CFTR with intermediate speed (<1 min; 95% inhibition at 50 µM; Ki = 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl- currents, and is effective in nasal and intestinal epithelia in vivo. Also available as a 25 mM solution in DMSO (Cat. No. 219675).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
CFTR
Product does not compete with ATP.
Reversible: yes
Target IC50: 95% inhibition at 50 µM
Target Ki: 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl- current

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Sonawane, N.D., et al. 2006. FASEB J.20, 130.
Muanprasat, C., et al. 2004. J. Gen. Physiol.124, 125.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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