GGsTop-Nahlsgen-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGGsTopCat. No.: HY-108467CAS No.: 926281-37-0Synonyms: Nahlsgen分式: CHNOP分量: 331.26作靶点: Others作通路: Others储存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 GGsTop (Nahlsgen)种有效、毒、度选择性和

2、不可逆的 酰基转肽酶 (glutamyl transpeptidase(GGT) 抑制剂，对 GGT 的Ki 值为 170 M。GGsTop 的 pKa 值为 9.71，对 E.coli GGT 和 GGT 的 Kon 值分别为 15010 和 513 M-1 s-1 1 2。在缺再灌注损伤模型中，GGsTop 具有保护肝脏功能 3。IC50 & Target Ki: 170 M (Human GGT) 1体外研究 GGsTop (Nahlsgen; Compound 5a) is a potent, highly selective and irreversible glutamyl tra

3、nspeptidase(GGT) inhibitor, with a Ki of 170 M for Human GGT 1. GGsTop shows pKa of 9.71, also exhibits Kons of15010 and 513 M-1 s-1 against E.coli GGT and human GGT, respectively 1 2.GGsTop is non-toxic compound, completely inhibits WT human GGT in 1 min at 1 mM, but less potentagainst the K562S mu

4、tant 2.体内研究GGsTop (1 mg/kg) lowers levels of ALT, AST, -GT at 12, 24, and 48 h after ischemia-reperfusion in rats 3.GGsTop also reduces 4-HNE and TNF- production, and decreases hepatic necrosis in rats 3.Animal Model: Male rats (9 week old) 3Dosage: 1 mg/kgAdministration: Injected into the inferior

5、vena cava for 12, 24, 48 hResult: Lowered the serum levels of ALT, AST, prevented the increase of serum -GT levels in1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEIR-GGsTop group.REFERENCES1. Han L, et al. Design, synthesis, and evaluation of gamma-phosphono diester analogues of glutamate as high

6、ly potent inhibitors andactive site probes of gamma-glutamyl transpeptidase. Biochemistry. 2007 Feb 6;46(5):1432-47.2. Kamiyama A, et al. Phosphonate-based irreversible inhibitors of human -glutamyl transpeptidase (GGT). GGsTop is a non-toxic andhighly selective inhibitor with critical electrostatic

7、 interaction with an active-site residue Lys562 for enhanced inhibitory activity. Bioorg MedChem. 2016 Nov 1;24(21):5340-5352.3. Tamura K, et al. GGsTop, a novel and specific -glutamyl transpeptidase inhibitor, protects hepatic ischemia-reperfusion injury in rats.Am J Physiol Gastrointest Liver Physiol. 2016 Aug 1;311(2):G305-12.McePdfHeightCaution: Product has not been fully validated for medical applications.For research