| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Z-Asp-CH2-DCB is a novel potent and irreversible caspase inhibitor with anti-inflammatory activity. Also inhibits the caspase-like activity of proteases. Z-Asp-CH2-DCB suppresses the production of IL-1β, TNF-α, IL-6, and IFN-γ in a dose-dependent manner.
| ln Vitro |
In a dose-dependent way, Z-Asp-CH2-DCB (10-100 μM) inhibits the production of IL-1β, TNF-α, IL-6, and IFN-γ in SEB-stimulated (200 ng; 16 h) PBMC. Additionally, there was an inhibition of MCP-1, MIP-1α, and MIP-1β chemokine production. On TSST-1-activated PBMC, Z-Asp-CH2-DCB had a comparable inhibitory impact, decreasing MCP-1, MIP-1α, TNF-α, IFN-γ, IL-1β, IL-6, and MIP-1β, in that order. 10%, 36%, 25%, 10%, 11%, 25%, and 30% of cell levels in the untreated state [1]. In PBMC treated with 200 ng SEB/ml, Z-Asp-CH2-DCB (10-100 μM; 48 hours) suppresses T cell proliferation [1].
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| ln Vivo |
Z-Asp-CH2-DCB (1 mg; i.p.; every day for 3 weeks) inhibits the apoptosis of septal cells induced by SU5416 [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: human peripheral blood mononuclear cells Tested Concentrations: 10, 50, 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: T cell proliferation was inhibited in SEB-stimulated PBMC. |
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (SU5416+ Z-Asp-CH2-DCB group) [1]
Doses: 1 mg Route of Administration: intraperitoneal (ip) injection; one time/day for 3 weeks Experimental Results: caspase in the lungs of SU5416-treated rats 3-like activity was Dramatically increased, while there was no increase in apoptotic activity in the lungs of rats treated with SU5416+Z-Asp-CH2-DCB. |
| References |
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| Molecular Formula |
C20H17NO7CL2
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|---|---|
| Molecular Weight |
454.25748
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| Exact Mass |
453.038
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| Elemental Analysis |
C, 52.88; H, 3.77; Cl, 15.61; N, 3.08; O, 24.65
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| CAS # |
153088-73-4
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| PubChem CID |
9911778
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
674.2±55.0 °C at 760 mmHg
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| Flash Point |
361.6±31.5 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.594
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| LogP |
5.29
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
30
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| Complexity |
614
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC=C(C=C1)COC(=O)N[C@@H](CC(=O)O)C(=O)COC(=O)C2=C(C=CC=C2Cl)Cl
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| InChi Key |
FKJMFCOMZYPWCO-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C20H17Cl2NO7/c21-13-7-4-8-14(22)18(13)19(27)29-11-16(24)15(9-17(25)26)23-20(28)30-10-12-5-2-1-3-6-12/h1-8,15H,9-11H2,(H,23,28)(H,25,26)/t15-/m0/s1
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| Chemical Name |
(3S)-5-(2,6-dichlorobenzoyl)oxy-4-oxo-3-(phenylmethoxycarbonylamino)pentanoic acid
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| Synonyms |
Z-Asp-CH2-DCB; PASE-1 INHIBITOR V; FHN88734; FHN-88734; FHN 88734;
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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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~220.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.58 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 20.8 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: ≥ 2.08 mg/mL (4.58 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 20.8 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: ≥ 2.08 mg/mL (4.58 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 | 2.2014 mL | 11.0069 mL | 22.0138 mL | |
| 5 mM | 0.4403 mL | 2.2014 mL | 4.4028 mL | |
| 10 mM | 0.2201 mL | 1.1007 mL | 2.2014 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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