Motolimod

製品コードS7161 バッチS716101

印刷

化学情報

Chemical Structure Synonyms VTX-2337 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H34N4O2
分子量 458.6 CAS No. 926927-61-9
Solubility (25°C)* 体外 DMSO 55 mg/mL warmed with 50ºC water bath (119.93 mM)
Ethanol 15 mg/mL (32.7 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Motolimod is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
in vitro VTX-2337 stimulates the production of both TNFα with EC50 of 140 nM and IL-12 with EC50 of 120 nM in PBMCs. In monocytes and mDCs, VTX-2337 selectively induces the production of TNFα and IL-12 via NF-κB activation. VTX-2337 also stimulates IFNγ production from NK cells, augments the lytic function of NK cells and enhances ADCC. [1]
in vivo In an ovarian cancer mouse model, TX-2337 enhances the effect of pegylated liposomal doxorubicin (PLD). [2]

プロトコル(参考用のみ)

キナーゼアッセイ Activity assay
The activity of specific TLR agonists is assessed using the secretory embryonic alkaline phosphatase (SEAP) reporter gene that is linked to NF-κB activation in response to TLR stimulation. Measurement of SEAP activity using the Quanti-blue substrate (InvivoGen) after TLR agonist treatment is carried out.
細胞アッセイ 細胞株 PBMCs or purified NK cells
濃度 ~500 nM
反応時間 48 h
実験の流れ PBMCs or purified NK cells are prepared as previously described, and the purity of NK cells was approximately 99%. NK cell–mediated cytotoxicity is assessed by Calcein AM release from labeled target cells. In brief, PBMCs or purified NK cells are cultured for 48 hours in RPMI medium in the presence of VTX-2337 (167 or 500 nmol/L) before incubation with target cells.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Preclinical Evidence for the Glucocorticoid-Sparing Potential of a Dual Toll-Like Receptor 7/8 Inhibitor in Autoimmune Diseases [ J Pharmacol Exp Ther, 2024, 388(3):751-764] PubMed: 37673681
Induction of OCT2 contributes to regulate the gene expression program in human neutrophils activated via TLR8 [ Cell Rep, 2021, 35(7):109143] PubMed: 34010659
Human Neutrophils Activated by TLR8 Agonists, With or Without IFNγ, Synthesize and Release EBI3, but Not IL-12, IL-27, IL-35, or IL-39 [ J Leukoc Biol, 2020, 1] PubMed: 32480433
Determination of motolimod concentration in rat plasma by liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study. [ J Pharm Biomed Anal, 2020, 179:112987] PubMed: 31761376
TLR7 and TLR8 Differentially Activate the IRF and NF-κB Pathways in Specific Cell Types to Promote Inflammation. [ Immunohorizons, 2020, 4(2):93-107] PubMed: 32086319
Activation of type I interferon antiviral response in human neural stem cells. [ Stem Cell Res Ther, 2019, 10(1):387] PubMed: 31843025
Human neutrophils activated via TLR8 promote Th17 polarization through IL-23. [ J Leukoc Biol, 2019, 105(6):1155-1165] PubMed: 30817049
EV71 Infection Induces IFNβ Expression in Neural Cells. [ Viruses, 2019, 11(12)] PubMed: 31817126
TLR7/8-agonist-loaded Nanoparticles Promote the Polarization of Tumour-Associated Macrophages to Enhance Cancer Immunotherapy [ Nat Biomed Eng, 2018, 2(8):578-588] PubMed: 31015631
The anticancer effect of mebendazole may be due to M1 monocyte/macrophage activation via ERK1/2 and TLR8-dependent inflammasome activation. [ Immunopharmacol Immunotoxicol, 2017, 39(4):199-210] PubMed: 28472897

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。