1. 疾病领域
  2. 呼吸系统疾病
  3. 肺部疾病
  4. 肺纤维化
  5. TLR9-IN-3

TLR9-IN-3 是一种 TLR9 拮抗剂,其 IC50 为 0.4 μM。TLR9-IN-3 对 TLR4TLR8 具有选择性,且可抑制人全血中 CD69 的激活,对应的 IC50 为 1.1 μM。TLR9-IN-3 可用于肺纤维化的相关研究。

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TLR9-IN-3

TLR9-IN-3 Chemical Structure

CAS No. : 2903190-66-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TLR9-IN-3 is a TLR9 antagonist with an IC50 of 0.4 μM. TLR9-IN-3 shows selectivity for TLR4 and TLR8, and inhibits CD69 activation in human whole blood with a corresponding IC50 of 1.1 μM. TLR9-IN-3 can be used in research related to pulmonary fibrosis[1].

体外研究
(In Vitro)

TLR9-IN-3 (Compound 20) 在人源和小鼠肝微粒体中具有较高的代谢稳定性 (half-life > 120 min),但在大鼠肝微粒体中稳定性较低,且在 PAMPA 和 Caco-2 实验中表现出良好的被动渗透性[1]
TLR9-IN-3 (0-25 μM) 在 A549、RAMOS 和 THP-1 细胞系中,于最高 25 μM 的浓度下无细胞毒性[1]

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

体内研究
(In Vivo)

TLR9-IN-3 (Compound 20) (1-10 mg/kg;口服;每日 1 次;连续 2 天) 在 Bleomycin (HY-108345) 诱导的小鼠肺损伤模型中对促炎和纤维化标志物表现出具有统计学意义的抑制作用[1]

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

Animal Model: C57BL/6 (male)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; QD; 2 days
Result: Confirmed statistically significant target engagement via terminal blood CD69 detection at 10 mg/kg compared to the bleomycin control group.
Reduced bronchoalveolar lavage fluid (BALF) IL-6, TIMP-1, and soluble collagen levels in a statistically significant manner at 1 mg/kg, 3 mg/kg, and 10 mg/kg compared to the bleomycin control group.
分子量

356.47

Formula

C18H28N8

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
TLR9-IN-3
目录号:
HY-181884
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