Motolimod

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Chemical Structure| 926927-61-9 同义名 : VTX-2337;VTX-378
CAS号 : 926927-61-9
货号 : A388121
分子式 : C28H34N4O2
纯度 : 99%+
分子量 : 458.595
MDL号 : MFCD28044318
存储条件：

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

In solvent -20°C:3-6个月-80°C:12个月
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

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].
实验方案
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
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.