貨號	規格	價格	上海	北京	武漢	南京
S80889-1mg	98.1%	￥170.00 S80889-1mg ￥170.00 現貨	10 10	-	-	-
S80889-5mg	98.1%	￥595.00 S80889-5mg ￥595.00 現貨	6 6	-	-	-
S80889-10mg	98.1%	￥990.00 S80889-10mg ￥990.00 現貨	8 8	-	-	-
S80889-25mg	98.1%	￥1400.00 S80889-25mg ￥1400.00 現貨	6 6	-	-	-
S80889-50mg	≥98%	￥2400.00 S80889-50mg ￥2400.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.

產品描述：

TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.

靶點：

PI3Kδ:235 nM (IC50);PI3Kγ:83 nM (IC50);PI3K

體內研究：

To correlate these in vivo responses with the molecular target of interest, PI3K pathway signaling is monitored through western blot analyses of Akt phosphorylation (a PI3K-mediated event). VEGF injection i.v. in mice induces a rapid Akt phosphorylation readily detectable in lung lysates, pretreatment with TG100-115 blocks this response. Blockade is seen with TG100-115 doses as low as 0.5 mg/kg and persists over a period of several hours. In initial dose-ranging studies, generally equivalent responses are observed using TG100-115 doses of 0.5-10 mg/kg, and we therefore elected to conduct a statistically powered test at the lowest dose. Animals dosed with TG100-115 as a single 0.5 mg/kg i.v. bolus 30 min after reperfusion developed smaller infarcts vs. vehicle-treated controls. Measuring infarct area as percent of total LV ischemic area, infarct size is reduced by 35% (P=0.04). Viable tissue within the ischemic zone is increased by 37% (P=0.04), directly demonstrating the cardioprotective effect of PI3Kγ/δ inhibition

參考文獻：

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

溶解性：

DMSO : 33.33 mg/mL (96.23 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)

保存條件：

-20℃

配置溶液濃度參考：

	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
50 mM	0.058 ml	0.289 ml	0.577 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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