| 产品介绍 |
IDO2-IN-1 是一种具有口服活性的强效吲哚胺 2,3- 双加氧酶 (IDO2) 抑制剂，IC50 为 112 nM。IDO2-IN-1 能够用于对炎症性自身免疫的研究。
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| 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.
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| 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.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
| Cell Line: |
HeLa cells line expressing hIDO1 induced by IFN-γ |
| Concentration: |
1 nM-0.1 mM |
| Incubation Time: |
48 hours |
| Result: |
Showed additional potency against IDO1 with an EC50 value of 633 nM.
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体内研究
(In Vivo) |
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 Rat
| Route |
Dose (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. |
1 |
0.69 |
/ |
/ |
375.1 |
2673 |
2675 |
0.55 |
/ |
| p.o. |
10 |
2.02 |
0.75 |
153.8 |
670.5 |
/ |
/ |
7.48 |
17.87 |
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| 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%.
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| 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.
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| 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 Rat
| Route |
Dose (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. |
1 |
0.69 |
/ |
/ |
375.1 |
2673 |
2675 |
0.55 |
/ |
| p.o. |
10 |
2.02 |
0.75 |
153.8 |
670.5 |
/ |
/ |
7.48 |
17.87 |
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 Rat
| Route |
Dose (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. |
1 |
0.69 |
/ |
/ |
375.1 |
2673 |
2675 |
0.55 |
/ |
| p.o. |
10 |
2.02 |
0.75 |
153.8 |
670.5 |
/ |
/ |
7.48 |
17.87 |
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| 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.
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| 性状 | Solid |
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| 溶解性数据 |
In Vitro:
DMSO : 140 mg/mL (258.61 mM; Need ultrasonic)
配制储备液
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浓度
溶剂体积
质量
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1 mg |
5 mg |
10 mg |
| 1 mM |
1.8472 mL |
9.2360 mL |
18.4720 mL |
| 5 mM |
0.3694 mL |
1.8472 mL |
3.6944 mL |
| 10 mM |
0.1847 mL |
0.9236 mL |
1.8472 mL |
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moisture and light
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| 参考文献 | |
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