产品
编 号：F741852
分子式：C23H31N7
分子量：405.54
分子式：C23H31N7
分子量：405.54
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CAS No: 2920729-91-3
产品详情
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.
体内研究：
TLR7/8/9 antagonist 2 (example 7) 具有较高的体内生物利用度。Animal Model:Male Wister-Han Rats
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(%)
465751415161616.814.7100
体外研究：
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 .TLR7/8/9 antagonist 2 对 hPBMC/TLR9 具有抑制活性，IC50 值为 420 nM。
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.
体内研究：
TLR7/8/9 antagonist 2 (example 7) 具有较高的体内生物利用度。Animal Model:Male Wister-Han Rats
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(%)
465751415161616.814.7100
体外研究：
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 .TLR7/8/9 antagonist 2 对 hPBMC/TLR9 具有抑制活性，IC50 值为 420 nM。
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