| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Ac5GalNTGc epimer targets the biosynthesis of mucin‑type O‑linked glycosylation. Mucin‑type O‑glycosylation is a post‑translational modification in which N‑acetylgalactosamine (GalNAc) is attached to serine or threonine residues of proteins by UDP‑GalNAc:polypeptide N‑acetylgalactosaminyltransferases (ppGalNAc‑Ts). This modification is critical for the structure and function of mucins and many other proteins. Ac5GalNTGc is a per‑acetylated, C‑2 thioacetyl‑substituted analogue of GalNAc that inhibits O‑glycosylation by interfering with the transfer of GalNAc to the protein backbone. The epimer mixture contains both diastereomers, which may have different inhibitory properties.
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| ln Vitro |
Ac5GalNTGc epimer is an analogue of hexosamine and the racemate of Ac5GalNTGc. Ac5GalNTGc is a per‑acetylated, C‑2 thioacetyl‑substituted potent GalNAc analogue that effectively inhibits the biosynthesis of mucin‑type O‑linked glycosylation. The compound can reduce the expression level of sialyl‑Lewis‑X on the surface of leukocytes, inhibit L‑selectin‑ and P‑selectin‑mediated cell rolling, and inhibit P‑selectin‑dependent leukocyte‑platelet adhesion. In a thioglycolate‑induced acute peritonitis model, Ac5GalNTGc exhibits anti‑inflammatory activity. No specific IC₅0 values are reported.
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| ln Vivo |
Ac5GalNTGc epimer has been studied in vivo in a mouse model of acute peritonitis. The compound exhibits anti‑inflammatory activity. Ac5GalNTGc can be used in research on O‑glycosylation/mucin biology, inflammation, and its associated translational medicine applications. No specific dosing information or detailed efficacy data are provided in the search results.
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| Enzyme Assay |
Ac5GalNTGc epimer is not evaluated in traditional enzyme/receptor binding assays. Its ability to inhibit O‑glycosylation is measured by cellular metabolic labeling assays. Cells are treated with a per‑acetylated, azido‑ or alkyne‑modified sugar analogue that is incorporated into glycoproteins, followed by click chemistry detection. Alternatively, the expression of specific glycan epitopes (e.g., sialyl‑Lewis‑X, Tn antigen) on cell surfaces is measured by flow cytometry using specific lectins or antibodies. No specific IC₅0 values are reported.
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| Cell Assay |
For cellular assays, human leukocytes (e.g., HL‑60 cells, THP‑1 cells) or other cell lines expressing mucin‑type O‑glycosylation are seeded in 6‑ or 96‑well plates. Cells are treated with Ac5GalNTGc epimer at concentrations of 1‑100 uM for 24‑72 h. O‑glycosylation is assessed by: (1) metabolic labeling with an azido‑ or alkyne‑modified sugar analogue (e.g., Ac4GalNAz) followed by click chemistry with a fluorescent dye and analysis by flow cytometry or fluorescence microscopy; (2) flow cytometry with lectins (e.g., Vicia villosa agglutinin (VVA) for Tn antigen, or wheat germ agglutinin (WGA) for sialic acid) to measure cell surface glycans; or (3) Western blot of isolated cell lysates with anti‑mucin antibodies (e.g., anti‑MUC1). The expression of sialyl‑Lewis‑X (sLex) is measured by flow cytometry using the HECA‑452 antibody. Cell viability is assessed by MTT or LDH assays.
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| Animal Protocol |
For in vivo evaluation of anti‑inflammatory activity, the thioglycolate‑induced acute peritonitis model in mice is used. 6‑8‑week‑old male C57BL/6 mice are injected intraperitoneally (IP) with 1 mL of 4% thioglycolate to induce peritoneal inflammation. Ac5GalNTGc epimer is administered IP at doses of 10‑100 mg/kg, either 1‑2 h before or immediately after thioglycolate injection. After 4‑6 h, the mice are euthanized, and peritoneal lavage fluid is collected. The total number of inflammatory cells (neutrophils, macrophages) in the lavage fluid is counted. The expression of sialyl‑Lewis‑X on the surface of leukocytes is measured by flow cytometry. The levels of pro‑inflammatory cytokines (IL‑1beta, IL‑6, TNF‑alpha) in the lavage fluid are measured by ELISA. Ac5GalNTGc epimer (C1₈H2₅NO11S, MW = 463.46, purity ≥98%, CAS 1334320-77-2) is a solid powder. For storage, the powder should be kept at -20 degC for up to 3 years, sealed and protected from light (‑25 to -15 degC). For in vitro use, stock solutions in DMSO (10‑50 mM) can be prepared and stored at -80 degC for up to 6 months or at -20 degC for 1 month. The compound is soluble in DMSO. No detailed PK parameters are reported.
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| ADME/Pharmacokinetics |
No specific toxicity data for Ac5GalNTGc epimer are reported. As a research‑grade compound, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling chemicals should be followed. Inhibition of O‑glycosylation may have broad effects on cell surface glycoproteins, which could lead to off‑target effects at high concentrations. No LD₅0 or formal toxicology studies are available.
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| Toxicity/Toxicokinetics |
Ac5GalNTGc epimer is a research‑grade hexosamine analogue that inhibits mucin‑type O‑linked glycosylation. Mucin‑type O‑glycosylation is a post‑translational modification that plays critical roles in cell‑cell and cell‑matrix interactions, immune recognition, cancer metastasis, and inflammation. The compound is a per‑acetylated analogue, which enhances cell permeability; the acetyl groups are removed by intracellular esterases to release the active compound. The C‑2 thioacetyl substitution is thought to interfere with the action of ppGalNAc‑Ts, the enzymes that initiate O‑glycosylation. Ac5GalNTGc epimer is the racemate of Ac5GalNTGc, meaning it contains both enantiomers. This compound is for research use only and has no clinical applications.
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| References |
| Molecular Formula |
C18H25NO11S
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| Molecular Weight |
463.46
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| Exact Mass |
463.114
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| CAS # |
1334320-77-2
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| PubChem CID |
154724792
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| Appearance |
Solid powder
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| LogP |
0.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
31
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| Complexity |
725
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(=O)OC[C@@H]1[C@@H]([C@@H]([C@H](C(O1)OC(=O)C)NC(=O)CSC(=O)C)OC(=O)C)OC(=O)C
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| InChi Key |
QIAVTYOXBOYXHI-SRKZOOFXSA-N
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| InChi Code |
InChI=1S/C18H25NO11S/c1-8(20)26-6-13-16(27-9(2)21)17(28-10(3)22)15(18(30-13)29-11(4)23)19-14(25)7-31-12(5)24/h13,15-18H,6-7H2,1-5H3,(H,19,25)/t13-,15-,16+,17-,18?/m1/s1
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| Chemical Name |
[(2R,3R,4R,5R)-3,4,6-triacetyloxy-5-[(2-acetylsulfanylacetyl)amino]oxan-2-yl]methyl acetate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1577 mL | 10.7884 mL | 21.5768 mL | |
| 5 mM | 0.4315 mL | 2.1577 mL | 4.3154 mL | |
| 10 mM | 0.2158 mL | 1.0788 mL | 2.1577 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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