| CAS NO: | 519170-13-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 361.4 |
| Cas No. | 519170-13-9 |
| Formula | C16H15N3O3S2 |
| Solubility | ≤5mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | N-[5-[(4-methoxyphenyl)methyl]-1,3,4-thiadiazol-2-yl]-benzenesulfonamide |
| Canonical SMILES | COC1=CC=C(CC2=NN=C(NS(C3=CC=CC=C3)(=O)=O)S2)C=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
OU749 is a competitive inhibitor of γ-glutamyl transpeptidase (GGT) [1].
Expression of γ-glutamyl transpeptidase (GGT) in tumors contributes to the resistance to radiation and chemotherapy. GGT is inhibited by glutamine analogues which compete with the substrate for the γ-glutamyl binding site [1].
OU749 inhibited human kidney GGT with an intrinsic Ki of 17.6 M [1]. In 786-O cells, a human renal tumor cell line, OU749 showed more than 150-fold less toxic than the GGT inhibitor acivicin toward dividing cells. OU749 inhibited GGT isolated from human kidney in a dose-dependent manner [1]. OU749 was 7-fold less potent as inhibitor of GGT isolated from rat kidney and 10-fold less potent inhibiting GGT from mouse kidney [1]. OU749 did not inhibit degradation of glutathione by GGT from rat kidney. Inhibition of GGT by OU749 is species-specific [1]. OU749 showed no inhibitory effect on GGT from pig cells. OU749 inhibited human GGT expressed in mouse fibroblasts by a similar extent to the GGT from human cells, indicated that the species specificity was determined by differences in the primary structure of the protein rather than species-specific, post-translational modifications [1].
Reference:
[1] King J B, West M B, Cook P F, et al. A novel, species-specific class of uncompetitive inhibitors of γ-glutamyl transpeptidase[J]. Journal of Biological Chemistry, 2009, 284(14): 9059-9065.
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