2. Immunology/Inflammation
  3. Toll-like Receptor (TLR) Interleukin Related
  4. TLR7 antagonist-1

TLR7 antagonist-1 (Compound 44#) 是一种具有口服活性的、选择性的 TLR7 拮抗剂，对 TLR7 的 IC50 值为 0.3 nM。TLR7 antagonist-1 可选择性结合 TLR7，抑制其活化，并下调 c-Rel 信号通路。\nTLR7 antagonist-1 可下调促炎细胞因子 IL-1β、IL-6、TNF-α 的 mRNA 水平。TLR7 antagonist-1 可减轻 Imiquimod (HY-B0180) 诱导的银屑病样皮损。TLR7 antagonist-1 可用于银屑病的相关研究。

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TLR7 antagonist-1

TLR7 antagonist-1 Chemical Structure

CAS No. : 3104353-70-7

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TLR7 antagonist-1 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TLR7 antagonist-1 (Compound 44#) is an orally active, selective TLR7 antagonist with an IC50 value of 0.3 nM against TLR7. TLR7 antagonist-1 selectively binds to TLR7, inhibits its activation, and downregulates the c-Rel signaling pathway. TLR7 antagonist-1 downregulates the mRNA levels of proinflammatory cytokines IL-1β, IL-6, and TNF-α. TLR7 antagonist-1 alleviates Imiquimod (HY-B0180)-induced psoriasis-like skin lesions. TLR7 antagonist-1 is applicable to research related to psoriasis[1].

IC50 & Target[1]

IL-1β

 

IL-6

 

TLR7

0.3 nM (IC50)

体外研究
(In Vitro)

TLR7 antagonist-1 可在 HEK-Blue-HTLR7 细胞中强效且选择性地抑制 TLR7，其 IC50 为 0.3 nM，对 TLR8 和 TLR9 的活性则弱得多[1]。
TLR7 antagonist-1 (0.005-5 μM; 12 h) 可浓度依赖性地抑制 RAW264.7 和 HEK-Blue-HTLR7 细胞中 TLR7 介导的炎性细胞因子[1]。

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

TLR7 antagonist-1 相关抗体:

Real Time qPCR[1]

Cell Line: RAW264.7 cells, HEK-Blue-HTLR7 cells
Concentration: 0.005-5 μM (RAW264.7 cells); 0.005-5 μM (HEK-Blue-HTLR7 cells)
Incubation Time: 12 h
Result: Concentration-dependently downregulated R848-induced mRNA levels of IL-1β, IL-6, TNF-α in RAW264.7 cells.
Concentration-dependently reduced IFN-α mRNA levels in HEK-Blue-HTLR7 cells, with 0.5 μM showing better efficacy than 5 μM Enpatoran (HY-134581).
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-t AUC0-∞ MRT0-∞ T1/2 Tmax Bioavailability
Rat[1] 1 mg/kg i.v. 144.67 ng/mL 492.47 ng·h/mL 687.31 ng·h/mL 17.84 h 13.34 h / /
Rat[1] 10 mg/kg p.o. 153.25 ng/mL 2300.94 ng·h/mL 3329.35 ng·h/mL 20.76 h 13.63 h 6 h 46.66 %
体内研究
(In Vivo)

TLR7 antagonist-1 (15-45 mg/kg；口服) 可有效缓解雌性 BALB/C 小鼠中 Imiquimod (HY-B0180) 诱导的银屑病样皮肤炎症、全身免疫应答及相关肝肾功能损伤，且炎症标志物水平和组织损伤程度呈剂量依赖性降低[1]。

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

Animal Model: BALB/C (female, 6 weeks old, 15-16 g, imiquimod-induced psoriasis-like dermatitis)[1]
Dosage: 15 mg/kg; 45 mg/kg
Administration: p.o.
Result: Reduced PASI scores significantly compared to the model group, with only slight skin thickening appearing from day 18.
Reduced epidermis/stratum corneum thickening, Munro microabscesses, and subdermal lymphocyte infiltration compared to the model group, with dermis and cuticle thickness near control levels.
Reversed spleen enlargement, with spleen weights near control levels.
Reduced mRNA levels of NF-κB p65 and c-Rel in skin tissue in a dose-dependent manner, with high-dose group c-Rel levels comparable to control group.
Reduced serum and skin tissue levels of inflammatory cytokines IL-17A and IL-1β in a dose-dependent manner.
Normalized elevated white blood cell counts, lymphocyte counts, and lymphocyte percentages in the model group to control levels.
Reduced model group increases in ALT, AST, BUN, and Scr in a dose-dependent manner, with high-dose group showing the most significant liver and renal function protection.
Showed no significant differences in body weight, liver/kidney weight, or histopathological damage to liver, kidney, or spleen across groups.
分子量

455.90

Formula

C21H25ClF3N5O
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

TLR7 antagonist-1 相关分类

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Help & FAQs
  • 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.

Keywords:

TLR7 antagonist-13104353-70-7Toll-like Receptor (TLR)Interleukin RelatedILTLR8IL-1βTLR7c-RelToll-like receptor 7MX1IL-6TNF-αNF-κB signaling pathwaysTLR9Inhibitorinhibitorinhibit

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