Motolimod(VTX-2337) is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities.
Motolimod is a novel small-molecule TLR8 agonist that activates monocytes, DCs, and NK cells. Motolimod selectively activates TLR8 with an EC(50) of about 100 nmol/L and stimulates production of TNFα and interleukin (IL)-12 from monocytes and myeloid dendritic cells (mDC). Motolimod stimulates IFNγ production from NK cells and increases the cytotoxicity of NK cells against K562 and ADCC by rituximab and trastuzumab. Effects of Motolimod on NK cells were, in part, from direct activation as increased IFNγ production and cytotoxic activity were seen with purified NK cells.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Lu H, et al. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509.
[2] Brueseke TJ, et al. Toll-like receptor 8: augmentation of innate immunity in platinum resistant ovarian carcinoma. Clin Pharmacol. 2013 May 23;5:13-9.
分子式 C28H34N4O2 |
分子量 458.6 |
CAS号 926927-61-9 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO 55 mg/mL |
Water <1 mg/mL |
Ethanol 15 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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