| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Caspase-1 24 nM (IC50)
CZL55 targets caspase-1, a cysteine protease that plays a central role in the inflammatory response by cleaving pro-inflammatory cytokines such as IL-1β and IL-18 into their active forms. By inhibiting caspase-1, CZL55 reduces the production of active IL-1β and IL-18, thereby modulating inflammation. |
|---|---|
| ln Vitro |
CZL55 demonstrates potent in vitro inhibition of caspase-1 with an IC50 of 24 nM. It has low cytotoxicity, making it suitable for cell-based studies. The compound's activity is typically assessed in enzymatic assays measuring caspase-1 cleavage of fluorogenic substrates.
|
| ln Vivo |
In vivo activity of CZL55 has been suggested by its potential use in the study of febrile seizures. Its inhibition of caspase-1 and modulation of inflammation suggest potential for in vivo efficacy in models of inflammatory diseases, pain, and neurological disorders. Further in vivo studies are needed to evaluate its efficacy and safety.
|
| Enzyme Assay |
In vitro enzyme assays for CZL55 involve measuring its inhibition of caspase-1 activity using fluorogenic substrates such as Ac-YVAD-AMC. The assay typically uses purified recombinant caspase-1, and IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for CZL55 involve treating cells with varying concentrations of the compound and measuring caspase-1 activity, IL-1β processing, or cell viability. The compound's low cytotoxicity allows for assessment of its effects on inflammatory responses in cell culture models.
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| Animal Protocol |
In vivo animal experiments for CZL55 would typically involve administering the compound to animal models of febrile seizures, inflammation, or pain and evaluating efficacy by measuring seizure activity, inflammatory markers, or pain responses.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for CZL55 are limited. The compound has a molecular weight of 386.40 and a molecular formula of C20H22N2O6. Its absorption, distribution, metabolism, and excretion properties have not been characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for CZL55 indicate that it has low cytotoxicity. As a research compound, comprehensive toxicological studies have not been reported. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
CZL55 (CAS#: 667408-87-9) has the molecular formula C20H22N2O6 and a molecular weight of 386.40. It is a potent caspase-1 inhibitor with an IC50 of 24 nM. The compound has low cytotoxicity and is used in research on febrile seizures, inflammation, and neurobiology.
|
| Molecular Formula |
C20H22N2O6
|
|---|---|
| Molecular Weight |
386.398485660553
|
| Exact Mass |
386.15
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| Elemental Analysis |
C, 62.17; H, 5.74; N, 7.25; O, 24.84
|
| CAS # |
667408-87-9
|
| PubChem CID |
1217703
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.7
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
28
|
| Complexity |
541
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(O)(=O)CCCC(NC1=CC=CC(C(NC2=CC=C(OC)C=C2OC)=O)=C1)=O
|
| InChi Key |
IXPHIUQELSUDNK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H22N2O6/c1-27-15-9-10-16(17(12-15)28-2)22-20(26)13-5-3-6-14(11-13)21-18(23)7-4-8-19(24)25/h3,5-6,9-12H,4,7-8H2,1-2H3,(H,21,23)(H,22,26)(H,24,25)
|
| Chemical Name |
5-((3-((2,4-dimethoxyphenyl)carbamoyl)phenyl)amino)-5-oxopentanoic acid
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| Synonyms |
CZL55; CZL-55; CZL 55
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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, 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)
|
| Solubility (In Vitro) |
DMSO : 166.67 mg/mL (431.34 mM)
|
|---|---|
| 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 | 2.5880 mL | 12.9400 mL | 25.8799 mL | |
| 5 mM | 0.5176 mL | 2.5880 mL | 5.1760 mL | |
| 10 mM | 0.2588 mL | 1.2940 mL | 2.5880 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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