| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
FK706 has an IC50 value of 230 nM and efficiently inhibits the hydrolysis of bovine cervical ligament elastin (final concentration 2 mg/mL) by human neutrophil elastase (final concentration 4 μg/mL)[1]. FK706 suppresses inflammatory chemokine release, mRNA expression of MCP-1 and IL-8, and NF-κB activation. FK706 may inhibit NF-κB activation in human lung fibroblasts directly, which would stop inflammatory chemokines from being expressed when lung inflammation brought on by cigarette smoke [2].
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| ln Vivo |
In a dose-dependent manner, FK706 (10-100 mg/kg; subcutaneous injection; duration 1-6 hours; male C57BL mice) therapy effectively reduces the edema (20 μg/paw) generated in mouse paws by human neutrophil elastase [1].
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| Animal Protocol |
Animal/Disease Models: Male C57BL mice (6 weeks old) were injected with human neutrophil elastase [1]
Doses: 10 mg/kg, 32 mg/kg, 100 mg/kg Route of Administration: subcutaneous injection; 1 hour, 2 hrs (hrs (hours)), 4 hrs (hrs (hours)), and 6 hrs (hrs (hours)) Experimental Results: Dramatically inhibited human neutrophil elastase-induced mouse paw edema in a dose-dependent manner. |
| References | |
| Additional Infomation |
See also: FK 706 (annotation moved to).
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| Molecular Formula |
C26H32F3N4NAO7
|
|---|---|
| Molecular Weight |
592.539868354797
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| Exact Mass |
592.212
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| CAS # |
144055-55-0
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| PubChem CID |
23690296
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
41
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| Complexity |
985
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| Defined Atom Stereocenter Count |
2
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| SMILES |
[Na+].FC(C(C(C(C)C)NC([C@@H]1CCCN1C([C@H](C(C)C)NC(C1C=CC(C(NCC(=O)[O-])=O)=CC=1)=O)=O)=O)=O)(F)F
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| InChi Key |
DNTYCMNNMGACPR-JSAITXCESA-M
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| InChi Code |
InChI=1S/C26H33F3N4O7.Na/c1-13(2)19(21(36)26(27,28)29)31-24(39)17-6-5-11-33(17)25(40)20(14(3)4)32-23(38)16-9-7-15(8-10-16)22(37)30-12-18(34)35;/h7-10,13-14,17,19-20H,5-6,11-12H2,1-4H3,(H,30,37)(H,31,39)(H,32,38)(H,34,35);/q;+1/p-1/t17-,19?,20-;/m0./s1
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| Chemical Name |
sodium;2-[[4-[[(2S)-3-methyl-1-oxo-1-[(2S)-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)carbamoyl]pyrrolidin-1-yl]butan-2-yl]carbamoyl]benzoyl]amino]acetate
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| Synonyms |
FK706; FK-706; FK 706
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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 : ~115 mg/mL (~194.08 mM)
H2O : ≥ 100 mg/mL (~168.76 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.44 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 50.0 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: ≥ 5 mg/mL (8.44 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 50.0 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: ≥ 5 mg/mL (8.44 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 | 1.6876 mL | 8.4382 mL | 16.8765 mL | |
| 5 mM | 0.3375 mL | 1.6876 mL | 3.3753 mL | |
| 10 mM | 0.1688 mL | 0.8438 mL | 1.6876 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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