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GlyH 101
Axon 2572
CAS:
328541-79-3
Purity:
98%
- Soluble in DMSO
- MF: C19H15Br2N3O3
- MW: 493.15
Description
Highly potent and selective cystic fibrosis (CF) transmembrane regulator (CFTR) inhibitor (Ki value 4.3 µM in CFTR-expressing FRT cells) targeting mitochondrial functions, independently of chloride channel inhibition. GlyH 101 induces a rapid increase in ROS levels and depolarizes mitochondria in the four cell types, suggesting that these effects are independent of CFTR inhibition. Moreover, intraluminal GlyH 101 (2.5 g) reduced by 80% cholera toxin-induced intestinal fluid secretion in a closed-loop model of cholera.
More Information
| Parent CAS No. | 328541-79-3 |
|---|---|
| Chemical Name | N'-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(naphthalen-2-ylamino)acetohydrazide |
| SMILES | C(N/N=C/C1=CC(Br)=C(O)C(Br)=C1O)(=O)CNC1=CC=C2C(=C1)C=CC=C2 |
| MFCD | MFCD01532954 |
| InChi | 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+ |
| InChiKey | RMBDLOATEPYBSI-NUGSKGIGSA-N |
| CID | 135476586 |
| Short Description | CFTR inhibitor |
References
- C. Muanprasat et al. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy. J Gen Physiol. 2004 Aug;124(2):125-37.
- M Kelly et al. Cystic fibrosis transmembrane regulator inhibitors CFTR(inh)-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition. J Pharmacol Exp Ther. 2010 Apr;333(1):60-9.
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