1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. TLR7/8/9 antagonist 2

TLR7/8/9 antagonist 2 是一种TLR7/8/9 拮抗剂,具有口服活性。TLR7/8/9 antagonist 2 对 HEK/hTLR7、HEK/hTLR8 和 HEK/hTLR9 具有抑制活性,IC50 值为 0.011 μM、0.029 μM 和 0,052 μM, TLR7/8/9 antagonist 2 在体内具有较高的生物利用度。TLR7/8/9 antagonist 2 可用于系统性红斑狼疮或狼疮性肾炎等自身炎症性疾病的研究[1]

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TLR7/8/9 antagonist 2 Chemical Structure

TLR7/8/9 antagonist 2 Chemical Structure

CAS No. : 2920729-91-3

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查看 Toll-like Receptor (TLR) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis[1].

IC50 & Target

IC50: 0.011 μM (HEK/hTLR7); 0.029 μM (HEK/hTLR8); 0.052 μM (HEK/hTLR9); 420 nM (hPBMC/TLR9)[1].

体外研究
(In Vitro)

TLR7/8/9 antagonist 2 (example 7) 对 HEK/hTLR7、HEK/hTLR8 和 HEK/hTLR9 具有抑制活性,IC50 值分别为 0.011 μM、0.029 μM 和 0,052 μM[1] .
TLR7/8/9 antagonist 2 对 hPBMC/TLR9 具有抑制活性,IC50 值为 420 nM
[1]

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

体内研究
(In Vivo)

TLR7/8/9 antagonist 2 (example 7) 具有较高的体内生物利用度[1]

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

Animal Model: Male Wister-Han Rats[1]
Dosage: 2 mg/kg, 10 mg/kg
Administration: p.o., i.v.; single dose
Result:
PO Cmax(ng/mL) PO AUC0-last(h*ng/mL) IV AUC0-last(h*ng/mL) CL (mL/min/kg) Vss (L/kg) T1/2(h) F(%)
465 7514 1516 16 16.8 14.7 100
分子量

405.54

Formula

C23H31N7

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

TLR7/8/9 antagonist 2 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.

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