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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-RSV-TMC353121
TMC353121

Chemical Structure : TMC353121

CAS No.: 857066-90-1

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TMC353121 (TMC 353121;TMC-353121)

货号: PC-42807Not For Human Use, Lab Use Only.

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9, shows activity against groups A and B RSV and against a panel of clinical isolates with equal potency (EC50<0.1 ng/mL).

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5 mg ￥1250 In stock
25 mg ￥3850 In stock
100 mg ￥8250 In stock
500 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9, shows activity against groups A and B RSV and against a panel of clinical isolates with equal potency (EC50<0.1 ng/mL); binds at a hydrophobic pocket of the 6HB formed by amino acid residues from both HR1 and HR2 heptad-repeats, stabilizes the interaction of HR1 and HR2 in an alternate conformation of the 6HB; demonstrates in vivo activity in the cotton rat models, significantly reduces viral load, bronchoalveolar lavage cell accumulation and the severity of lung histopathological change at dose of 0.25-10 mg/Kg.

物理化学性质&存储条件

分子量 558.7143
分子式 C32H42N6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-Pyridinol, 2-[[6-[[[2-(3-hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(4-morpholinyl)propyl]amino]-1H-benzimidazol-1-yl]methyl]-6-methyl-

参考文献

1. Bonfanti JF, et al. J Med Chem. 2008 Feb 28;51(4):875-96.

2. Roymans D, et al. Proc Natl Acad Sci U S A. 2010 Jan 5;107(1):308-13.

3. Rouan MC, et al. Antimicrob Agents Chemother. 2010 Nov;54(11):4534-9.

4. Ispas G, et al. PLoS One. 2015 May 26;10(5):e0126959.

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