TG100-115产品描述：TG100-115 是一种选择性的
PI3Kγ/
PI3Kδ 抑制剂，
IC50 分别为 83 和 235 nM。
TG100-115产品描述：TG100-115 is a selective
PI3Kγ/
PI3Kδ inhibitor with
IC50s of 83 ａnd 235 nM, respectively.IC50 & Target: IC50: 83 nM （PI3Kγ）, 235 nM （PI3Kδ）
[1]In Vitro: TG100-115 inhibits PI3Kγ ａnd PI3Kδ with IC
50s of 83 ａnd 235 nM, respectively, whereas both PI3Kα ａnd PI3Kβ are relatively unaffected （IC
50 values >1 μM）. As a gauge of general specificity, TG100-115 is also assayed against a 133 protein kinase panel, of which are inhibited at IC
50 values <1 μM. TG100-115 potently inhibits edema ａnd inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor ａnd platelet-activating factor; by contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage
[1].
In Vivo: 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
[1].
研究领域：
Membrane Transporter/Ion Channel靶点：
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MWt:346.34
Formula:C18H14N6O2
SMILES:NC1=C（C（N=C2C3=CC（O）=CC=C3）=NC（N）=N1）N=C2C4=CC（O）=CC=C4
Research_Area:Cardiovascular Disease;Cancer
公司介绍：MedChemExpress（MCE）专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、；MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足*新的科研需求；数千种产品在上海有充足备货，24-48小时内送达客户；大量产品提供免费试用装；已为全球多个知名企业、院校构建各种定制型化合物库。
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原创作者：MedChemExpress
