| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| 25mg | |||
| Other Sizes |
| Targets |
Ac-FLTD-CMK targets inflammatory caspases, including caspase-1, caspase-4, caspase-5, and caspase-11. It acts as an irreversible inhibitor, forming a covalent bond with the active site cysteine residue. By inhibiting these caspases, it prevents the cleavage of gasdermin D (GSDMD), which is a key step in pyroptosis, a form of inflammatory cell death.
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|---|---|
| ln Vitro |
Ac-FLTD-CMK inhibits pyroptosis downstream of canonical and atypical inflammasomes, decreases IL-1 following NLRP3 inflammasome activation, and prevents GSDMD from being cleaved by caspase-1, -4, -5, and -11 in vitro. 1β released by macrophages. On the other hand, Ac-FLTD-CMK did not cause cell death or inhibit caspase-3. When caspase-1 was complexed with Ac-FLTD-CMK, the crystal structure showed that hydrogen bonds and destination contacts were involved in a wide range of enzyme-to-peer responses [1].
In vitro, Ac-FLTD-CMK inhibits caspases 1, 4, 5, and 11 with IC50 values of 46.7 nM, 1.49 µM, 329 nM, and an unspecified value, respectively. It is inactive against apoptosis-related caspase-3. The compound effectively inhibits gasdermin D cleavage. |
| ln Vivo |
In vivo activity data for Ac-FLTD-CMK are not extensively detailed in the available sources. As a pyroptosis inhibitor, it has potential for studying inflammatory diseases. Specific in vivo efficacy data are not provided.
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| Enzyme Assay |
The in vitro enzyme assay for Ac-FLTD-CMK involves measuring the inhibition of caspase activity. Recombinant caspases are incubated with a fluorogenic substrate (e.g., Ac-YVAD-AMC for caspase-1) in the presence of varying compound concentrations. The IC50 is determined by quantifying the reduction in substrate cleavage.
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| Cell Assay |
Cellular assays are performed using cells that undergo pyroptosis. Cells are treated with Ac-FLTD-CMK and stimulated with inflammasome activators. Gasdermin D cleavage is assessed by Western blotting, and pyroptosis is measured by lactate dehydrogenase (LDH) release or propidium iodide staining.
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| Animal Protocol |
In vivo animal studies for Ac-FLTD-CMK are not detailed in the available sources. The compound is used as a research tool to study pyroptosis and inflammatory diseases.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Ac-FLTD-CMK are not available in the provided sources. As a peptide-based inhibitor, it may have limited oral bioavailability and a short half-life.
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| Toxicity/Toxicokinetics |
Toxicity data for Ac-FLTD-CMK are not reported in the available sources. As a research compound, it is used in laboratory settings for studying pyroptosis.
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| References | |
| Additional Infomation |
Ac-FLTD-CMK is a research tool for studying pyroptosis and inflammatory caspases. It is a specific inhibitor of inflammatory caspases and is used to investigate the role of pyroptosis in inflammation and disease. The compound is available from chemical suppliers for research use only.
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| Molecular Formula |
C26H37CLN4O8
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|---|---|
| Molecular Weight |
569.0470
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| Exact Mass |
568.23
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| Elemental Analysis |
C, 54.88; H, 6.55; Cl, 6.23; N, 9.85; O, 22.49
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| CAS # |
2376255-48-8
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| Related CAS # |
2376255-48-8;
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| PubChem CID |
155906572
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| Appearance |
White to off-white solid powder
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| LogP |
0.2
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
39
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| Complexity |
878
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)CCl)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C)O
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| InChi Key |
UCWNTWGHVCSMJP-WPUDHWPRSA-N
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| InChi Code |
InChI=1S/C26H37ClN4O8/c1-14(2)10-19(30-24(37)20(28-16(4)33)11-17-8-6-5-7-9-17)25(38)31-23(15(3)32)26(39)29-18(12-22(35)36)21(34)13-27/h5-9,14-15,18-20,23,32H,10-13H2,1-4H3,(H,28,33)(H,29,39)(H,30,37)(H,31,38)(H,35,36)/t15-,18+,19+,20+,23+/m1/s1
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| Chemical Name |
(3S)-3-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-5-chloro-4-oxopentanoic acid
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| Synonyms |
Ac-FLTD-CMK
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). 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 (~175.73 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.39 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 (4.39 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 (4.39 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 | 1.7573 mL | 8.7866 mL | 17.5731 mL | |
| 5 mM | 0.3515 mL | 1.7573 mL | 3.5146 mL | |
| 10 mM | 0.1757 mL | 0.8787 mL | 1.7573 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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