Tilorone  (Synonyms: 替洛隆)

Tilorone is an orally active antiviral agent and interferon inducer that also has potential antineoplastic, immunomodulatory, and metabolic modulating effects. Tilorone induces an abnormally delayed interferon response and primarily stimulates interferon production in lymphoid tissue. Thus, Tilorone exerts antiviral effects and can be used as a chemotherapeutic agent. Tilorone has the potential to inhibit type 2 diabetes by increasing glucose uptake in vivo and in skeletal muscle cells by enhancing Akt2/AS160 signaling and glucose transporter levels^{[1][2][3][4][5]}.

Tilorone (0.8-500 μg/mL; 2 d) 在腹腔巨噬细胞和淋巴细胞中诱导的干扰素生成不显著^[1].
Tilorone 具有 52% 的人血浆蛋白结合率，具有出色的血浆稳定性，小鼠肝微粒体半衰期为 48 分钟^[2].
Tilorone (20, 35 nM; 40 h) 可增加成肌细胞中骨形态发生蛋白 (BMP) 和 Smad4 的表达^[3].
Tilorone (20, 35 nM; 40 h) 还能够增加 C2C12 细胞中 GLUT 的表达和葡萄糖摄取^[3].
Tilorone (3 μM-20 μM; 72 h) 还可以选择性靶向 CDK5 活性低的 PC3 细胞^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tilorone (50-250 mg/kg; po; 单剂量) 可以诱导干扰素反应延迟但不使其延长；并呈剂量依赖性影响循环干扰素的水平^[1].
Tilorone 在小鼠中的最大耐受单剂量为 100 mg/kg；Tilorone (2, 10 mg/kg; ip) 在小鼠中的药代动力学结果表明，Tilorone 的吸收速率高，在雌性和雄性小鼠中的半衰期为 18 小时，但雄性小鼠中的暴露量更高^[2].
Tilorone (25-50 mg/kg; ip; 每天 1 次, 共 8 天) 可保护 90% 的受到埃博拉病毒感染小鼠，使其免受致命攻击^[2].
Tilorone (25 mg/kg; iv; 单剂量) 可增强在小鼠对放射性标记的葡萄糖类似物 ¹⁸F-fluoro-2-deoxyglucose 的摄取^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

410.55

C₂₅H₃₄N₂O₃

27591-97-5

固体

替洛隆

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Stringfellow D A, et al. Tilorone hydrochloride: an oral interferon-inducing agent[J]. Antimicrobial agents and chemotherapy, 1972, 2(2): 73-78.  [Content Brief]

  [2]. Ekins S, et al. Efficacy of tilorone dihydrochloride against Ebola virus infection[J]. Antimicrobial agents and chemotherapy, 2018, 62(2): 10.1128/aac. 01711-17.  [Content Brief]

  [3]. Kohler Z M, et al. Tilorone increases glucose uptake in vivo and in skeletal muscle cells by enhancing Akt2/AS160 signaling and glucose transporter levels[J]. Journal of Cellular Physiology, 2023, 238(5): 1080-1094.  [Content Brief]

  [4]. Wissing M D, et al. Small-molecule screening of PC3 prostate cancer cells identifies tilorone dihydrochloride to selectively inhibit cell growth based on cyclin-dependent kinase 5 expression[J]. Oncology reports, 2014, 32(1): 419-424.