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TG100-115

Cat. No. M1886
TG100-115 Structure
Size Price Availability Quantity
10mg USD 165 In stock
50mg USD 560 In stock
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Quality Control
Biological Activity

TG100-115 is a potent small molecule PI3K γ/δ inhibitor potently inhibited edema and inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor and platelet-activating factor. TG100-115, inhibited PI3Kγ and -δ (IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and -β were relatively unaffected (IC50 values >1 μM). TG100-115 also blocked histamine-induced permeability, as predicted based on PI3K's role in GPCR signaling. Additionally, TG100-115 did not block VEGF-induced angiogenesis in vivo.

Protocol
Cell Experiment
Cell lines Human umbilical vein EC
Preparation method Cell proliferation assay.
Human umbilical vein EC plated in 96-well cluster plates (5,000 cells/well) were cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF) in the presence or absence of test compounds (10 μM), and cell numbers were quantified by XTT assay (Promega, Madison, WI) 24, 48, or 72 h later.
Concentrations 10 μM
Incubation time 24, 48, or 72 h
Animal Experiment
Animal models Rodent and porcine MI models
Formulation either PEG or sulfobutyl ether β-cyclodextrin (CyDex, Lenexa, KS) formulations
Dosages 0.5mg/kg or 1mg/kg
Administration i.v. at 0–3 h after reperfusion
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 346.34
Formula C18H14N6O2
CAS Number 677297-51-7
Purity 98.62%
Solubility DMSO
Storage at -20°C
References

Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.
Doukas J, et al. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71. PMID: 17172449.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TG100-115 supplier, PI3K, inhibitors

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