| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
γ-glutamyl transpeptidase[1]
gamma-glutamyl transpeptidase (GGT). Acivicin inhibits GGT, an enzyme involved in glutathione metabolism and glutamine homeostasis. Inhibition of GGT affects cellular redox balance and glutamine utilization. |
|---|---|
| ln Vitro |
In human HepG2 cells, acivicin hydrochloride (AT-125 hydrochloride; 0.1-50 μM; 5 days) has an IC50 of 0.7 μM [1].
Acivicin hydrochloride exhibits antitumor, antimicrobial, and antiparasitic properties. As a GGT inhibitor, it modulates glutamine metabolism and glutathione levels in cells. Detailed IC₅0 values for GGT inhibition have not been reported in available literature. |
| ln Vivo |
Acivicin hydrochloride (AT-125 hydrochloride; 5 mg/kg; intraperitoneal injection; twice weekly) decreases γ-GT in the urine by 70–78% [3].
Acivicin hydrochloride (5 mg/kg; intraperitoneal injection; twice weekly) decreases gamma-GT in the urine by 70-78%. It can cross the blood-brain barrier, suggesting potential for central nervous system applications. |
| Enzyme Assay |
GGT inhibition assays: Acivicin hydrochloride is incubated with purified GGT enzyme and its substrate (e.g., gamma-glutamyl-p-nitroanilide). Enzyme activity is measured by spectrophotometric detection of the released product. IC₅0 values are calculated from dose-response curves.
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| Cell Assay |
Cancer cell lines or other cell types are treated with Acivicin hydrochloride. Cell viability is measured using MTT or CellTiter-Glo assays. GGT activity is measured in cell lysates or culture supernatants. Glutathione levels are measured using biochemical assays. Glutamine metabolism is assessed by measuring glutamine consumption and glutamate production.
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| Animal Protocol |
Animal/Disease Models: Male pigmented Long-Evans rats weighed between 250 g and 300 g exposed to Toluene[3]
Doses: 5 mg/kg Route of Administration: IP; twice weekly (monday and wednesday) Experimental Results: diminished urinary γ-GT by 70-78%. Animal models of cancer or infection could be used to evaluate Acivicin hydrochloride in vivo. The compound can be administered intraperitoneally. Efficacy would be assessed by tumor growth inhibition, survival, or microbial load reduction. Urinary gamma-GT levels can be measured as a pharmacodynamic marker. |
| ADME/Pharmacokinetics |
Acivicin hydrochloride has a molecular weight of 215.03 and a molecular formula of C₅H₈Cl2N2O3. It is a hydrochloride salt form of acivicin that enhances solubility and stability for in vitro and in vivo applications. It can cross the blood-brain barrier.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for Acivicin hydrochloride in standard toxicology studies. As a research compound, it is not intended for human therapeutic use. Its effects on glutamine metabolism may have implications for normal cell function.
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| References |
[1]. Kreuzer J, et al. Target discovery of acivicin in cancer cells elucidates its mechanism of growth inhibition. Chem Sci. 2014 Dec 1;6(1):237-245. Epub 2014 Sep 26.
[2]. Chikhale EG, et al. Carrier-mediated transport of the antitumor agent acivicin across the blood-brain barrier. Biochem Pharmacol. 1995 Mar 30;49(7):941-5. [3]. Delphine Waniusiow, et al. Toluene-induced hearing loss in acivicin-treated rats. Neurotoxicol Teratol. May-Jun 2008;30(3):154-60. |
| Additional Infomation |
Acivicin hydrochloride (AT-125 hydrochloride) is a natural product produced by Streptomyces sviceus. It is a gamma-glutamyl transpeptidase (GGT) inhibitor. It exhibits anticancer, antimicrobial, and antiparasitic properties. The compound is for research use only and has not entered clinical trials.
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| Molecular Formula |
C5H8CL2N2O3
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|---|---|
| Molecular Weight |
215.03461933136
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| Exact Mass |
213.991
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| CAS # |
161922-40-3
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| Related CAS # |
Acivicin;42228-92-2
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| PubChem CID |
155905759
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
206
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@H](ON=C1Cl)[C@@H](C(=O)O)N.Cl
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| InChi Key |
IXBPTDHBIYEQHX-QYEIVYHBSA-N
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| InChi Code |
InChI=1S/C5H7ClN2O3.ClH/c6-3-1-2(11-8-3)4(7)5(9)10;/h2,4H,1,7H2,(H,9,10);1H/t2-,4-;/m0./s1
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| Chemical Name |
(2S)-2-amino-2-[(5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl]acetic acid;hydrochloride
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : 100 mg/mL (465.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.63 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 (11.63 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6505 mL | 23.2526 mL | 46.5051 mL | |
| 5 mM | 0.9301 mL | 4.6505 mL | 9.3010 mL | |
| 10 mM | 0.4651 mL | 2.3253 mL | 4.6505 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.
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