OU749 |
| Catalog No.GC12981 |
γ-Glutamyl transferase (GGT) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 519170-13-9
Sample solution is provided at 25 µL, 10mM.
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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 | |
| 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 | ||
| Formula | C16H15N3O3S2 | M.Wt | 361.4 |
| Solubility | ≤5mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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