| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
Ac-YVAD-AOM targets caspase-1 (interleukin-1β converting enzyme, ICE) and related caspases. Caspases are a family of cysteine proteases that play essential roles in apoptosis and inflammation. Caspase-1 is involved in the processing of pro-inflammatory cytokines such as IL-1β and IL-18. By inhibiting caspase-1, Ac-YVAD-AOM modulates inflammatory responses and apoptosis.
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|---|---|
| ln Vitro |
In cell-free biochemical systems, Ac-YVAD-AOM inhibits caspase-1 activity. The compound's inhibition of caspase-1 can be assessed using fluorogenic substrates that are cleaved by caspase-1, releasing a fluorescent signal. The IC50 is determined from dose-response curves. The compound's selectivity for different caspases can be assessed by testing against a panel of purified caspase enzymes.
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| ln Vivo |
In cell-based assays, Ac-YVAD-AOM inhibits caspase-1 activity, leading to reduced processing of pro-inflammatory cytokines and modulation of apoptosis. The compound's effects are evaluated in immune cells by measuring IL-1β and IL-18 processing. The compound can be used to study the role of caspase-1 in inflammation and cell death.
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| Enzyme Assay |
The cell-free assay for caspase-1 inhibition involves measuring the enzymatic activity of purified caspase-1 in the presence of the compound. The assay uses a fluorogenic substrate (e.g., Ac-YVAD-AMC) that is cleaved by caspase-1, releasing a fluorescent signal. The compound is incubated with the enzyme and substrate, and the fluorescence is measured over time. The IC50 is determined from dose-response curves.
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| Cell Assay |
Cell-based assays for Ac-YVAD-AOM involve culturing immune cells such as macrophages and treating them with the compound at concentrations ranging from 0.01 to 100 μM. Cells are stimulated with LPS or other inflammasome activators to induce caspase-1 activation. Caspase-1 activity is assessed by measuring the processing of pro-IL-1β to mature IL-1β by Western blotting or ELISA. Apoptosis is assessed by measuring caspase-3 activity or by Annexin V staining.
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| Animal Protocol |
In animal models, Ac-YVAD-AOM has been evaluated for its ability to inhibit caspase-1 and modulate inflammatory responses. Typical studies involve administration of the compound to mice via intraperitoneal or intravenous routes. Inflammatory disease models are used to assess the compound's ability to reduce inflammation. Tissues are collected for analysis of caspase-1 activity, cytokine levels, and inflammatory markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Ac-YVAD-AOM have not been extensively reported. As a peptide-based compound with a molecular weight of approximately 612.6 g/mol, the compound would be expected to have limited oral bioavailability and may require parenteral administration. The compound is typically metabolized by peptidases and other enzymes. Further pharmacokinetic studies would be required for therapeutic development.
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| Toxicity/Toxicokinetics |
Ac-YVAD-AOM is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this chemical reagent. As a caspase-1 inhibitor, the compound may have effects on immune function and inflammatory responses. Standard toxicity studies would be required for therapeutic development.
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| References | |
| Additional Infomation |
Ac-YVAD-AOM is a research-grade compound supplied for caspase and apoptosis research. It is not an approved pharmaceutical and has no clinical trial history. The compound is a peptide-based caspase-1 inhibitor with a fluorophore for detection. This product is intended for research use only.
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| Molecular Formula |
C33H42N4O10
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|---|---|
| Molecular Weight |
654.71
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| Exact Mass |
654.29
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| CAS # |
154674-81-4
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| PubChem CID |
9852588
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1029.6±65.0 °C at 760 mmHg
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| Flash Point |
576.5±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.566
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| LogP |
4.77
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
47
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| Complexity |
1130
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC([C@H](NC([C@@H](NC(C)=O)CC1=CC=C(O)C=C1)=O)C(N[C@H](C(N[C@H](C(COC(C2=C(C=CC=C2C)C)=O)=O)CC(O)=O)=O)C)=O)C
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| InChi Key |
LOACDHZQOPEFKK-NFJAKAEBSA-N
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| InChi Code |
InChI=1S/C33H42N4O10/c1-17(2)29(37-31(44)25(35-21(6)38)14-22-10-12-23(39)13-11-22)32(45)34-20(5)30(43)36-24(15-27(41)42)26(40)16-47-33(46)28-18(3)8-7-9-19(28)4/h7-13,17,20,24-25,29,39H,14-16H2,1-6H3,(H,34,45)(H,35,38)(H,36,43)(H,37,44)(H,41,42)/t20-,24-,25-,29-/m0/s1
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| Chemical Name |
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-5-(2,6-dimethylbenzoyl)oxy-4-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) |
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 | 1.5274 mL | 7.6370 mL | 15.2739 mL | |
| 5 mM | 0.3055 mL | 1.5274 mL | 3.0548 mL | |
| 10 mM | 0.1527 mL | 0.7637 mL | 1.5274 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.
Products are for research use only; We do not sell to patients
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