219671
GlyH-101
≥97% (HPLC), solid, CFTR inhibitor, Calbiochem®
別名:
CFTR Inhibitor II, GlyH-101, N-(2-Naphthalenyl)-((3,5-dibromo-2,4-dihydroxyphenyl)methylene)glycine hydrazide
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この商品について
実験式（ヒル表記法）:
C19H15Br2N3O3
CAS番号:
分子量:
493.15
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.28
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze
製品名
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).
Quality Segment
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
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. Also available as a 25 mM solution in DMSO (Cat. No. 219675).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CFTR
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
Preparation Note
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.
Muanprasat, C., et al. 2004. J. Gen. Physiol.124, 125.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書（COA）
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