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Motolimod (VTX-378) 是一种有效且特异性的 Toll 样受体 8 (TLR8) 激动剂,EC50约为 100 nM。
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Motolimod (VTX-378) 是一种有效且特异性的 Toll 样受体 8 (TLR8) 激动剂,EC50约为 100 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 311 | 现货 | |
5 mg | ¥ 738 | 现货 | |
10 mg | ¥ 1,180 | 现货 | |
25 mg | ¥ 2,200 | 现货 | |
50 mg | ¥ 3,170 | 现货 | |
100 mg | ¥ 4,360 | 现货 | |
200 mg | ¥ 5,870 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 750 | 现货 |
产品描述 | Motolimod (VTX-378) (VTX-2337) is an effective and specific Toll-like receptor (TLR) 8 agonist (EC50: 100 nM), > 50-fold selectivity over TLR7. |
靶点活性 | TLR8:100 nM(EC50) |
体外活性 | Motolimod在PBMCs中诱导TNFα(EC50:140 nM)和IL-12(EC50:120 nM)的产生。在mDCs和单核细胞中,Motolimod通过NF-κB激活特异性诱导IL-12和TNFα的产生。Motolimod还诱导NK细胞产生IFNγ,增强NK细胞的溶解功能,并增强ADCC。 |
体内活性 | 在卵巢癌小鼠模型中,TX-2337增强了聚乙二醇化脂质体紫杉醇(PLD)的效果。 |
激酶实验 | 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. |
细胞实验 | 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. |
别名 | VTX-378, VTX-2337 |
分子量 | 458.6 |
分子式 | C28H34N4O2 |
CAS No. | 926927-61-9 |
Smiles | CCCN(CCC)C(=O)C1=Cc2ccc(cc2N=C(N)C1)-c1ccc(cc1)C(=O)N1CCCC1 |
密度 | 1.19 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 12 mg/mL (26.2 mM) DMSO: 51 mg/mL (111.2 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
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