AF 12198 |
| Catalog No.GC11039 |
Type I IL-1 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 185413-30-3
Sample solution is provided at 25 µL, 10mM.
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IC50: 25 nM for IL-1-induced IL-8 production
Interleukin-1 (IL-1) -α and -β are potent regulators of inflammatory responses. Naturally occurring interleukin-1 receptor antagonist (IL-1ra) is effective in vitro and in vivo in modulating biological responses to IL-1. AF 12198 is a novel low molecular weight antagonist of IL-1.
In vitro: AF 12198 binds the human type I IL-1 receptor selectively but not the human type II receptor or the murine type I receptor. AF12198 also inhibits IL-1-induced IL-8 formation by human dermal fibroblasts with a half-maximal inhibition concentration or IC50 of 25 nM and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression by endothelial cells with an IC50 of 9 nM [2].
In vivo: When given as an intravenous infusion to cynomolgus monkeys, AF 12198 blocks ex vivo IL-1 induction of IL-6 and down modulates in vivo induction of IL-6. This is the first small molecule to show IL-1 receptor antagonist activity in vivo [3].
Clinical trial: Up to now, AF 12198 is still in the preclinical development stage.
Reference:
[1] Akeson AL, Woods CW, Hsieh LC, Bohnke RA, Ackermann BL, Chan KY, Robinson JL, Yanofsky SD, Jacobs JW, Barrett RW, Bowlin TL. AF12198, a novel low molecular weight antagonist, selectively binds the human type I interleukin (IL)-1 receptor and blocks in vivo responses to IL-1. J Biol Chem. 1996 Nov 29;271(48):30517-23.
| Cas No. | 185413-30-3 | SDF | |
| Chemical Name | (S,Z)-5-(((S,Z)-1-(((2S,3R)-1-((S)-2-((1Z,4Z,6S,7Z,9S,10Z,12S)-6-((1H-indol-3-yl)methyl)-1,4,7,10,15-pentahydroxy-12-((S)-2-((Z)-hydroxy(((S,Z)-1-hydroxy-1-(((S,Z)-1-hydroxy-1-(((S)-1-((S)-2-((Z)-hydroxy(((S)-1-hydroxy-1-imino-4-methylpentan-2-yl)imino)me | ||
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@]1([H])CCCN1C([C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@]2([H])CCN2C([C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@]3([H])CCCN3C([C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C)([H])CC4=CC=CC=C4)([H])CCC(O)=O)([H])CC5=CNC6= | ||
| Formula | C96H123N19O22 | M.Wt | 1895.12 |
| Solubility | Soluble to 1 mg/ml in 10% ethanol/PBS | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.5277 mL | 2.6384 mL | 5.2767 mL |
| 5 mM | 0.1055 mL | 0.5277 mL | 1.0553 mL |
| 10 mM | 0.0528 mL | 0.2638 mL | 0.5277 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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