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。
| 生物活性 | IDO2-IN-1 is an orally active and potentIndoleamine 2,3-dioxygenase2(IDO2) inhibitor with anIC50value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research[1]. |
| IC50& Target | IDO1 411 nM (IC50) | IDO2 112 (IC50) |
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体外研究
(In Vitro) | IDO2-IN-1 (compound 22) shows stronger inhibition on IDO2 (IC50=112 nM) over IDO1 (IC50=411 nM)[1].
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[1].
Cell Viability Assay[1] | 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 EC50value 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[1].
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[1].
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[1].
Pharmacokinetic Profile in Rat[1]
| Route | Dose (mg/kg) | T1/2/sub>(h) | Tmax(h) | Cmax(ng/mL) | AUC(0-∞)(hong/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 |
| Animal Model: | Xylene-induced ear swelling mouse model (ICR mice, male, 6 weeks old)[1] | | 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)[1] | | 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)[1] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 140 mg/mL(258.61 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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