货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T97351-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T97351-1ml ￥648.00 现货	5 5	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T97351-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

PARP抑制剂;PARP Inhibitors;;InformationRBN012759 RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.Targetshuman PARP14 (Cell-free assay); mouse PARP14 (Cell-free assay) <3 nM; 5 nMIn vitroRBN012759 is a sufficiently soluble, highly permeable, low efflux and potent inhibitor of human and mouse PARP14 with high PARP family selectivity. RBN012759 treatment of human primary macrophages decreases the MAR/PAR signal corresponding to PARP14 self-MARylation and stabilizes PARP14 protein in a dose-dependent manner. Treatment of primary human macrophages with RBN012759 leads to decreased IL-4 driven M2-like gene expression, suggesting that PARP14 inhibition results in a less immunosuppressive phenotype.In vivoRBN012759 has moderate clearance and oral bioavailability in mice. RBN012759 is well-tolerated in mice with repeat dosing up to 500 mg/kg BID (75-fold coverage of the PARP14 mouse).

体内研究：

RBN012759 (500 mg/kg BID；口服) 在小鼠中具有良好的耐受性，重复给药。
RBN012759 (100 mg/kg；口服) 表现出适度的口服生物利用度 (30%) 和由于中等清除率 (54 mL/min/kg) 和低稳态分布容积 (1.4 L/kg) 在小鼠体内的短血浆半衰期 (0.4 小时)。

参考文献：

1. Schenkel L, et, al. A potent and selective PARP14 inhibitor decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants. AACR Annual Meeting 2020.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.642 ml	13.211 ml	26.423 ml
5 mM	0.528 ml	2.642 ml	5.285 ml
10 mM	0.264 ml	1.321 ml	2.642 ml
50 mM	0.053 ml	0.264 ml	0.528 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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