产品
编 号：F756072
分子式：C21H21BrN10O3
分子量：541.36
分子式：C21H21BrN10O3
分子量：541.36
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2803768-09-2
产品详情
生物活性：
IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research.
体内研究：
The Adjuvant arthritis (AA) model and Collagen-induced arthritis (CIA) model have similar pathogenesis and pathological characteristics to human rheumatoid arthritis (RA).IDO2-IN-1 (compound 22) (100 mg/kg; p.o.; once dose) exhibits excellent anti-inflammatory activity, higher than naproxen, a prescription drug reducing pain, swelling, and joint stiffness from arthritis. IDO2-IN-1 (25, 50, 100 mg/kg; i.p.; once daily, for 19 d) exhibits excellent inhibitory effect on mice paw swelling, shows efficacy in a collagen-induced arthritis model in mice.IDO2-IN-1 (30, 60, 120 mg/kg; i.p.; once daily, for 15 d) inhibits joint inflammation and displays potential effect in autoimmune arthritis improvement.Pharmacokinetic Profile in RatRouteDose (mg/kg)T1/2/sub> (h)Tmax (h)Cmax (ng/mL)AUC(0-∞) (h?ng/mL)CL (mL/h/kg)Vz (mL/kg)MRT(0-∞) (h)F (%)
i.v.10.69//375.1267326750.55/
p.o.102.020.75153.8670.5//7.4817.87
Animal Model:Xylene-induced ear swelling mouse model (ICR mice, male, 6 weeks old)
Dosage:100 mg/kg
Administration:Oral gavage; once dose; evenly coated right ear with 25 μL of xylene after 1 h treatment
Result:Significantly relieved mouse ear swelling with a high swelling inhibition rate of 65.32%.
Animal Model:Collagen-induced arthritis (CIA) mice model (DBA/1J mice, male, 6 weeks old)
Dosage:25, 50, 100 mg/kg
Administration:Intraperitoneal injection; once daily; 19 days, began on day 56 after collagen induced
Result:Decreased the expression of inflammatory cytokines IL-18 and IL-33.Reduced inflammation and cartilage and bone erosions symptoms.
Animal Model:Adjuvant arthritis (AA) rat model (Sprague-Dawley rats, male, 180 ± 20 g)
Dosage:30, 60, 120 mg/kg
Administration:Intraperitoneal injection; once daily; 15 days, began on day 21 after chondrex induced
Result:Significantly reduced IL-6 and TNF-α levels.Decreased synovial hyperplasia accompanied by inflammatory cell infiltration, pannus formation, and bone erosion of cartilage in a dose-dependent manner.
体外研究：
IDO2-IN-1 (compound 22) shows stronger inhibition on IDO2 (IC50 =112 nM) over IDO1 (IC50 =411 nM).IDO2-IN-1 inhibits hIDO1 expression (EC50=633 nM) in HeLa cell-based IDO1/kynurenine assay, co-incubated with hIFN-γ (100 ng/mL final concentration), which is used for producing N-formylkynurenine.
IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research.
体内研究：
The Adjuvant arthritis (AA) model and Collagen-induced arthritis (CIA) model have similar pathogenesis and pathological characteristics to human rheumatoid arthritis (RA).IDO2-IN-1 (compound 22) (100 mg/kg; p.o.; once dose) exhibits excellent anti-inflammatory activity, higher than naproxen, a prescription drug reducing pain, swelling, and joint stiffness from arthritis. IDO2-IN-1 (25, 50, 100 mg/kg; i.p.; once daily, for 19 d) exhibits excellent inhibitory effect on mice paw swelling, shows efficacy in a collagen-induced arthritis model in mice.IDO2-IN-1 (30, 60, 120 mg/kg; i.p.; once daily, for 15 d) inhibits joint inflammation and displays potential effect in autoimmune arthritis improvement.Pharmacokinetic Profile in RatRouteDose (mg/kg)T1/2/sub> (h)Tmax (h)Cmax (ng/mL)AUC(0-∞) (h?ng/mL)CL (mL/h/kg)Vz (mL/kg)MRT(0-∞) (h)F (%)
i.v.10.69//375.1267326750.55/
p.o.102.020.75153.8670.5//7.4817.87
Animal Model:Xylene-induced ear swelling mouse model (ICR mice, male, 6 weeks old)
Dosage:100 mg/kg
Administration:Oral gavage; once dose; evenly coated right ear with 25 μL of xylene after 1 h treatment
Result:Significantly relieved mouse ear swelling with a high swelling inhibition rate of 65.32%.
Animal Model:Collagen-induced arthritis (CIA) mice model (DBA/1J mice, male, 6 weeks old)
Dosage:25, 50, 100 mg/kg
Administration:Intraperitoneal injection; once daily; 19 days, began on day 56 after collagen induced
Result:Decreased the expression of inflammatory cytokines IL-18 and IL-33.Reduced inflammation and cartilage and bone erosions symptoms.
Animal Model:Adjuvant arthritis (AA) rat model (Sprague-Dawley rats, male, 180 ± 20 g)
Dosage:30, 60, 120 mg/kg
Administration:Intraperitoneal injection; once daily; 15 days, began on day 21 after chondrex induced
Result:Significantly reduced IL-6 and TNF-α levels.Decreased synovial hyperplasia accompanied by inflammatory cell infiltration, pannus formation, and bone erosion of cartilage in a dose-dependent manner.
体外研究：
IDO2-IN-1 (compound 22) shows stronger inhibition on IDO2 (IC50 =112 nM) over IDO1 (IC50 =411 nM).IDO2-IN-1 inhibits hIDO1 expression (EC50=633 nM) in HeLa cell-based IDO1/kynurenine assay, co-incubated with hIFN-γ (100 ng/mL final concentration), which is used for producing N-formylkynurenine.
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