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APY0201

Cat. No. M8898
APY0201 Structure
Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 250 In stock
50mg USD 800 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In stimulated thioglycollate-induced mouse peritoneal exudate cells (TG-PEC), APY0201 strongly inhibits IL-12p70 and IL-12p40 production, with IC50s of 8.4 and 16 nM, respectively. APY0201 also inhibits IL-12p40 at 99 nM in human PBMC. APY0201 inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 with an IC50 of 5.2 nM. APY0201 demonstrates ameliorated inflammation in an experimental model of colitis.

In vivo: Oral APY0201 at a 30 mg/kg dose shows significant reduction of IL-12p70 production (78% inhibition relative to that of the vehicle control), which implys that the inhibitory potential of APY0201 against IL-12 is confirmed in the animal experiment.

Protocol
Cell Experiment
Cell lines Mouse TG-PEC or human PBMC
Preparation method Mouse TG-PEC or human PBMC are incubated with APY0201 (1, 10, 100, 1000 and 10000 nM) in the presence of 100 ng/mL mouse or human IFN-γ and 0.05%w/v Staphylococcus aureus Cowan I strain (SAC).
Concentrations 1, 10, 100, 1000 and 10000 nM
Incubation time
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 413.48
Formula C23H23N7O
CAS Number 1232221-74-7
Purity >98%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201.
Hayakawa N, et al. Bioorg Med Chem. 2014 Jun 1;22(11):3021-9. PMID: 24767819.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: APY0201 supplier, inhibitors

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