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Merck
CN

219675

CFTR Inhibitor II, GlyH-101

InSolution, ≥97%, potent, selective and reversible open-channel blocker of CFTR

Synonym(s):

InSolution CFTR Inhibitor II, GlyH-101, N-(2-Naphthalenyl)-((3,5-dibromo-2,4-dihydroxyphenyl)methylene)glycine hydrazide

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About This Item

Empirical Formula (Hill Notation):
C19H15Br2N3O3
CAS Number:
Molecular Weight:
493.15
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.28
Assay:
≥97% (HPLC)
Form:
liquid
Storage condition:
OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
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Quality Segment

assay

≥97% (HPLC)

form

liquid

potency

4.3 μM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

shipped in

dry ice

storage temp.

−70°C

SMILES string

Brc1c(c(cc(c1O)\C=N\NC(=O)CNc2cc3c(cc2)cccc3)Br)O

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

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.

Biochem/physiol Actions

Cell permeable: yes
Reversible: yes

Packaging

Packaged under inert gas

Physical form

A 25 mM (5 mg/406 µL) solution of CFTR Inhibitor II, GlyH-101 (Cat. No. 219671) in DMSO.

Preparation Note

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 3 months at -70°C.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)


Storage Class

10 - Combustible liquids

wgk

WGK 1

flash_point_f

188.6 °F - closed cup - (refers to pure substance)

flash_point_c

87 °C - closed cup - (refers to pure substance)



Certificates of Analysis (COA)

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