TG100-115
TG100-115
CAS: 677297-51-7
Molecular Formula: C18H14N6O2
TG100-115 - Names and Identifiers
| Name | TG100-115 |
| Synonyms | CS-427 TG100115 TG100-115 TG100 115 TG100 115 3,3,-(2,4-diaminopteridine-6,7-diyl)diphenol 6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol TG100-115 |
| CAS | 677297-51-7 |
TG100-115 - Physico-chemical Properties
| Molecular Formula | C18H14N6O2 |
| Molar Mass | 346.34 |
| Density | 1.516±0.06 g/cm3(Predicted) |
| Boling Point | 699.6±65.0 °C(Predicted) |
| Appearance | Yellow powder solid. |
| pKa | 8.54±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | For TG100-115 inhibition of PI3Kγ and-δ, IC50 were 83 and 235 nM, respectively. The inhibitory effect of TG100-115 on PI3Kα and-β was not significant, and the IC50 was 1.2 and 1.3 mM, respectively. At 10 μm TG100-115, Human Umbilical vein endothelial cells (HUVECs) had no effect on cell proliferation and VEGF-stimulated ERK phosphorylation. However, 10 μm TG100-115 blocked other VEGF signaling pathways, such as VE-cadherin phosphorylation. 10 μm TG100-115 acts on HUVECs to inhibit VEGF-induced increase in the overall level of VE cadherin. TG100-115 inhibits VEGF-regulated mTOR and p70 S6 kinase phosphorylation, both of which are downstream of PI3K. 125 nM to 10 μm TG100-115 also inhibited FGF-stimulated Akt phosphorylation. The IC50 for TG100-115 inhibition of PI3Kγ and-δ were 83 and 235 nM, respectively. The inhibitory effect of TG100-115 on PI3Kα and-β was not significant, and the IC50 was 1.2 and 1.3 mM, respectively. At 10 μm TG100-115, Human Umbilical vein endothelial cells (HUVECs) had no effect on cell proliferation and VEGF-stimulated ERK phosphorylation. However, 10 μm TG100-115 blocked other VEGF signaling pathways, such as VE-cadherin phosphorylation. 10 μm TG100-115 acts on HUVECs to inhibit VEGF-induced increase in the overall level of VE cadherin. TG100-115 inhibits VEGF-regulated mTOR and p70 S6 kinase phosphorylation, both of which are downstream of PI3K. 125 nM to 10 μm TG100-115 also inhibited FGF-stimulated Akt phosphorylation. |
| In vivo study | TG100-115 at a dose of 1-5 mg/kg in the Miles experimental model, reduce edema and inflammation in rats. TG100-115 according to the dose of 0.5-5 mg/kg in rodent and pig models with myocardial infarction, to provide effective cardiac protection, limit the further development of infarction, preservation of cardiac function. TG100-115 at a dose of 5 mg/kg in mice, significantly reduced the vascular permeability associated with Sema3A or VEGF, indicating that these two factors may be dependent on PI3Kγ/δ to induce vascular permeability. TG100-115 in the mouse model of asthma, significantly reduced pulmonary eosinophilia, inhibition of interleukin 13 and mucin accumulation. TG100-115 at a dose of 1-5 mg/kg in the Miles experimental model, reduce edema and inflammation in rats. TG100-115 according to the dose of 0.5-5 mg/kg in rodent and pig models with myocardial infarction, to provide effective cardiac protection, limit the further development of infarction, preservation of cardiac function. TG100-115 at a dose of 5 mg/kg in mice, significantly reduced the vascular permeability associated with Sema3A or VEGF, indicating that these two factors may be dependent on PI3Kγ/δ to induce vascular permeability. TG100-115 in the mouse model of asthma, significantly reduced pulmonary eosinophilia, inhibition of interleukin 13 and mucin accumulation. |
TG100-115 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.887 ml | 14.436 ml | 28.873 ml |
| 5 mM | 0.577 ml | 2.887 ml | 5.775 ml |
| 10 mM | 0.289 ml | 1.444 ml | 2.887 ml |
| 5 mM | 0.058 ml | 0.289 ml | 0.577 ml |
Last Update：2024-01-02 23:10:35
Supplier List
Spot supply
Product Name: TG100-115 Visit Supplier Webpage Request for quotationCAS: 677297-51-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: TG100-115 Visit Supplier Webpage Request for quotationCAS: 677297-51-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History