2. Immunology/Inflammation
  3. Toll-like Receptor (TLR) Interleukin Related IFNAR
  4. KBD4466

KBD4466 是一种口服有效的强效 TLR7 和 TLR8 抑制剂，IC50 分别为 0.9 nM 和 2.8 nM。KBD4466 抑制炎性细胞因子 IL-6 和 IFN-α 的表达。KBD4466 改善了系统性红斑狼疮 (SLE) 的 BXSB/MpJ 小鼠模型的疾病进展并提高了存活率。KBD4466 可用于自身免疫性疾病研究。

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KBD4466

KBD4466 Chemical Structure

CAS No. : 3023713-87-0

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KBD4466 相关抗体

Top Publications Citing Use of Products

查看 Toll-like Receptor (TLR) 亚型特异性产品:

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KBD4466 is an orally active potent TLR7 and TLR8 inhibitor with IC50s of 0.9 nM and 2.8 nM, respectively. KBD4466 inhibits the expression of inflammatory cytokines IL-6 and IFN-α. KBD4466 improves disease progression and survival in the BXSB/MpJ mouse model of Systemic Lupus Erythematosus (SLE). KBD4466 can be used in the study of autoimmune diseases[1].

IC50 & Target[1]

TLR7

0.9 nM (IC50)

TLR8

2.8 nM (IC50)

IL-6

 

体外研究
(In Vitro)

KBD4466 (Compound 19) 抑制 TLR7 和 TLR8 活性[1]。

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

KBD4466 相关抗体:
体内研究
(In Vivo)

KBD4466 (Compound 19) (1 mg/kg，口服，一次) 可抑制 R848 攻击的小鼠模型中 IL-6 和 IFN-α 的产生[1]。

KBD4466 (10 mg/kg，口服，每日一次，14 周) 可改善 BXSB/MpJ 小鼠狼疮模型中的疾病症状[1]。

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

Animal Model: R848 (25 μg per mouse, i.p., 1 h, 4 h, 8 h, 16 h, 24 h after administration of compound 19)-challenged mouse (female C57BL/6 mice, 6-8 weeks old) model [1]
Dosage: 1 mg/kg
Administration: p.o., once
Result: Inhibited the production of IL-6, with an inhibition rate of 99.4% at 1 hour, more than 50% at 16 hours, and more than 90% at 8 hours.
Inhibited the production of IFN-α, with an inhibition rate of 98% at 16 h, 69% at 24 h.
Animal Model: SLE model using BXSB/MpJ transgenic mice (female BXSB/MpJ mice, 7 weeks).[1]
Dosage: 10 mg/kg
Administration: p.o., once a day, 14 weeks
Result: Improved survival rates ,the survival rate reached 100%.
Relieved splenomegaly and lymphadenopathy, and reduced plasma levels of autoantibodies, including anti-histone antibodies, anti-ribosomal P (anti-RiboP), and anti-double-stranded DNA (anti-dsDNA).
Reduced urine microalbumin (MALB), urine microalbumin to creatinine ratio (MALB/CREA), and urine total protein (UTP) levels.
Improved kidney swelling.
分子量

468.47

Formula

C24H23F3N6O
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

KBD4466 相关分类

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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

KBD44663023713-87-0KBD 4466KBD-4466Toll-like Receptor (TLR)Interleukin RelatedIFNARILInterferon-α/β receptorInterferon-alpha/beta receptorInhibitorR848-challenged mouse modelBXSB/MpJ mouse lupus modelAutoimmune diseasesinhibitorinhibit

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HY-176553
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