| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T408682-1ml |
1ml |
现货  |
|
| 英文别名 | 7-methyl-2-morpholino-9-(1-(phenylamino)ethyl)-4H-pyrido[1,2-a]pyrimidin-4-one |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | TGX-221 |
| 生化机理 | TGX-221 是一种 p110β 特异性抑制剂，在无细胞实验中的 IC50 为 5 nM，对 p110β 的选择性是 p110α 的 1000 倍。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 磷脂酰肌醇-4;5-二磷酸 3-激酶催化亚基 beta 抑制剂；磷脂酰肌醇-4;5-二磷酸 3-激酶催化亚基 delta 抑制剂 |
| 产品介绍 |
TGX-221 是一种p110β-特定的抑制剂，在无细胞试验中IC50为 5 nM，作用于p110β的选择性是作用于p110α的1000倍。 Information TGX-221 is ap110β-specific inhibitor withIC50of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α. The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. TGX-221 show slow potent to p110δ with IC50 of 211 nM. Furthermore, TGX-221 partially attenuates insulin-induced phosphorylation of Ser473 of PKB in J774.2 macrophage cells. TGX-221 inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. A recent study shows that after treatment with TGX-221 (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform. In vivo As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with TGX-221 doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups. cell lines：OPM-2/GFP, KMS-11, RPMI 8226, and NCI-H929 cells Concentrations：~20 μM Incubation Time：24-72 hours Powder Purity:≥95% |
| IC50 | p110β, IC50: 5 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC(NC1=CC=CC=C1)C2=CC(=CN3C(=O)C=C(N=C23)N4CCOCC4)C |
| 分子量 | 364.44 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 92 mg/mL (199.46 mM); Ethanol: 92 mg/mL (199.46 mM); Water: Insoluble; |
|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless Transparent Liquid) | Pass |
| Record the entire process by video | Conform |
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