OU749
目录号 : GC12981
Inhibitor of γ-glutamyl transferase
Cas No.:519170-13-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 519170-13-9 | SDF | |
| 化学名 | 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 | ||
| 分子式 | C16H15N3O3S2 | 分子量 | 361.4 |
| 溶解度 | ≤5mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.767 mL | 13.8351 mL | 27.6702 mL |
| 5 mM | 0.5534 mL | 2.767 mL | 5.534 mL |
| 10 mM | 0.2767 mL | 1.3835 mL | 2.767 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。