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Merck

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:
328541-79-3
分子量:
493.15
MDL number:
MFCD01532954
UNSPSC Code:
12352200
NACRES:
NA.28

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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).

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

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

Quality Level

100

関連するカテゴリー

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

Disclaimer

Toxicity: Standard Handling (A)

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).

Other Notes

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

Preparation Note

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

Legal Information

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

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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以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

Amnah Yamani et al.
Mucosal immunology, 14(1), 135-143 (2020-06-25)
Food-triggered anaphylaxis can encompass a variety of systemic and intestinal symptoms. Murine-based and clinical studies have revealed a role for histamine and H1R and H2R-pathway in the systemic response; however, the molecular processes that regulate the gastrointestinal (GI) response are
Juliette L Simonin et al.
Cells, 11(9) (2022-05-15)
Defective hydration of airway surface mucosa is associated with recurrent lung infection in cystic fibrosis (CF), a disease caused by CF transmembrane conductance regulator (CFTR) gene mutations. Whether the composition and/or presence of an airway surface liquid (ASL) is sufficient
R K Dutta et al.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 142, 112090-112090 (2021-09-01)
MicroRNAs play an important role in health and disease. TGF-β signaling, upregulated by HIV Tat, and in chronic airway diseases and smokers upregulates miR-145-5p to suppress cystic fibrosis transmembrane conductance regulator (CFTR). CFTR suppression in chronic airway diseases like Cystic
Barbara Calabrese et al.
Nature communications, 13(1), 6037-6037 (2022-10-14)
During early ischemic brain injury, glutamate receptor hyperactivation mediates neuronal death via osmotic cell swelling. Here we show that ischemia and excess NMDA receptor activation cause actin to rapidly and extensively reorganize within the somatodendritic compartment. Normally, F-actin is concentrated

グローバルトレードアイテム番号

カタログ番号GTIN
219671-5MGCN07790788048747

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