RBN012759

RBN012759 is a potent, selective, and orally active PARP14 inhibitor with an IC50 of less than 3 nM. It exhibits 300-fold selectivity over monoPARPs and 1000-fold over polyPARPs. RBN012759 diminishes pro-tumor macrophage functions and triggers inflammatory responses in tumor explants¹.

RBN012759 (0.01-10 μM) reduces the MAR/PAR signal linked to self-MARylation of PARP14 and stabilizes PARP14 protein in a dose-dependent manner in human primary macrophages¹.

RBN012759 (0.1-10 μM) lowers IL-4 stimulated cytokine secretion in human primary macrophages¹.

RBN012759 (500 mg/kg BID; pO.) is well-tolerated in mice with multiple dosing sessions¹.

RBN012759 (100 mg/kg; orally) shows moderate oral bioavailability (30%) and a short plasma half-life (0.4 hours), attributed to moderate clearance (54 mL/min/kg) and a low steady-state volume of distribution (1.4 L/kg) in mice¹.

RBN012759 (500 mg/kg BID; pO.) is well-tolerated in mice with multiple dosing sessions¹.

RBN012759 (100 mg/kg; orally) shows moderate oral bioavailability (30%) and a short plasma half-life (0.4 hours), attributed to moderate clearance (54 mL/min/kg) and a low steady-state volume of distribution (1.4 L/kg) in mice¹.

溶解方案(细胞实验)

DMSO 中的溶解度 : 233.33 mg/mL (616.52 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.08 mg/mL (5.50 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.08 mg/mL (5.50 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"