Size | Price | Stock | Qty |
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5mg |
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10mg |
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Other Sizes |
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Targets |
Ki: 0.4 μM[1], 0.56 μM (glyoxalase I)[2]
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ln Vitro |
With a binding affinity greater than GSH and a selectivity for GSTP that is over 50 times greater than that of the GSTM and GSTA classes (Ki=0.4 μM), TLK117 is the most specific GSTP inhibitor found to date[1]. TER 117 is a GST P1-1 isoenzyme inhibitor designed to avoid the known role of GST P1-1 in tumor cells' resistance to drugs. TER 117 is administered as a diethyl ester (TER 117 DEE, also known as TER 199) to aid in its cellular uptake. It has been discovered that TER 117 is a competitive inhibitor of glyoxalase I and GST P1-1[2].
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ln Vivo |
When the GSTP inhibitor TLK117 is administered orally during the pharyngeal stage of fibrosis, it reduces the amount of remodeling caused by bleomycin and AdTGFβ, α-SMA, caspase activation, FAS S-glutathionylation, and total protein S-glutathionylation. GSTP activity is significantly reduced four hours after the administration of 50 mg/kg TLK117, and it stays reduced by roughly 60% for at least twenty-four hours[2].
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References |
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Additional Infomation |
See also: ... View More ...
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Molecular Formula |
C23H27N3O6S
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Molecular Weight |
473.541984796524
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Exact Mass |
473.162
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CAS # |
152684-53-2
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Related CAS # |
Ezatiostat;168682-53-9
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PubChem CID |
444051
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Appearance |
White to off-white solid powder
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LogP |
-0.9
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Hydrogen Bond Donor Count |
5
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Hydrogen Bond Acceptor Count |
8
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Rotatable Bond Count |
13
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Heavy Atom Count |
33
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Complexity |
665
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Defined Atom Stereocenter Count |
3
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SMILES |
[C@@H](C1C=CC=CC=1)(C(=O)O)NC(=O)[C@H](CSCC1C=CC=CC=1)NC(=O)CC[C@H](N)C(=O)O
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InChi Key |
ZPSKWMFLCHMEOY-CMKODMSKSA-N
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InChi Code |
InChI=1S/C23H27N3O6S/c24-17(22(29)30)11-12-19(27)25-18(14-33-13-15-7-3-1-4-8-15)21(28)26-20(23(31)32)16-9-5-2-6-10-16/h1-10,17-18,20H,11-14,24H2,(H,25,27)(H,26,28)(H,29,30)(H,31,32)/t17-,18-,20+/m0/s1
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Chemical Name |
(2S)-2-amino-5-[[(2R)-3-benzylsulfanyl-1-[[(R)-carboxy(phenyl)methyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 150 mg/mL (316.76 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1118 mL | 10.5588 mL | 21.1175 mL | |
5 mM | 0.4224 mL | 2.1118 mL | 4.2235 mL | |
10 mM | 0.2112 mL | 1.0559 mL | 2.1118 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.