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Motolimod {[allProObj[0].p_purity_real_show]}

货号:A388121 同义名: VTX-2337;VTX-378

Motolimod is a Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM with immunostimulatory and antineoplastic activities.

Motolimod 化学结构 CAS号:926927-61-9
Motolimod 化学结构
CAS号:926927-61-9
Motolimod 3D分子结构
CAS号:926927-61-9
Motolimod 化学结构 CAS号:926927-61-9
Motolimod 3D分子结构 CAS号:926927-61-9
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Motolimod 纯度/质量文件 产品仅供科研

货号:A388121 标准纯度: {[allProObj[0].p_purity_real_show]}
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Motolimod 生物活性

描述 The toll-like receptors (TLR) are a family of protein that are responsible for pathogen recognition. TLR8 is expressed within the endolysosomal compartmental pathway and it is able to recognize the intracellular pathogens[3]. Motolimod is a novel small molecule TLR8 agonist with EC50 of about 100 nmol/L[4]. The THP-1 cells were treated with motolimod from 3 nM to 10 μM overnight. The IL-1β and IL-18 mRNA level measured by RT-PCR were significantly increased after the treatment of motolimod. The IL-β, caspase-1 and pro-IL-1 protein level were also increased significantly as detected by western blotting assay[5]. The hind paw of C57BL/6 mice was intradermally injected with 50 µg of motolimod and spontaneous pain behaviors were counted every 5 min for 30 min. It was found that the treatment of motolimod could induced lifting, flinching and licking in the first 15 min[6].
作用机制 Motolimod is an ultra-potent TLR8 selective agonist by binding with the TLR-8[7].

Motolimod 动物研究

Dose Monkey: 1 mg/kg, 10 mg/kg[1] (s.c.)
Administration s.c.

Motolimod 参考文献

[1]Dietsch GN, Lu H, et al. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity. PLoS One. 2016 Feb 29;11(2):e0148764.

[2]Lu H, Dietsch GN, 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.

[3]Kawai T, Akira S. The role of pattern-recognition receptors in innate immunity: update on Toll-like receptors. Nat Immunol. 2010 May;11(5):373-84.

[4]Lu H, Dietsch GN, Matthews MA, Yang Y, Ghanekar S, Inokuma M, Suni M, Maino VC, Henderson KE, Howbert JJ, Disis ML, Hershberg RM. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509.

[5]Dietsch GN, Lu H, Yang Y, Morishima C, Chow LQ, Disis ML, Hershberg RM. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity. PLoS One. 2016 Feb 29;11(2):e0148764.

[6]Zhang ZJ, Guo JS, Li SS, Wu XB, Cao DL, Jiang BC, Jing PB, Bai XQ, Li CH, Wu ZH, Lu Y, Gao YJ. TLR8 and its endogenous ligand miR-21 contribute to neuropathic pain in murine DRG. J Exp Med. 2018 Dec 3;215(12):3019-3037.

[7]Dowling DJ, Tan Z, Prokopowicz ZM, Palmer CD, Matthews MA, Dietsch GN, Hershberg RM, Levy O. The ultra-potent and selective TLR8 agonist VTX-294 activates human newborn and adult leukocytes. PLoS One. 2013;8(3):e58164.

Motolimod 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.90mL

2.18mL

1.09mL

21.81mL

4.36mL

2.18mL

Motolimod 技术信息

CAS号926927-61-9
分子式C28H34N4O2
分子量 458.595
别名 VTX-2337;VTX-378
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 50 mg/mL(109.03 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

PO 0.5% CMC-Na 65 mg/mL suspension

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