| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:IDO2-IN-1
CAS:2803768-09-2
Package:25mg/RMB 10600;50mg/RMB 13800;100mg/RMB 17500
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| | INDEX NAME NOT YET ASSIGNED Basic information |
| Product Name: | INDEX NAME NOT YET ASSIGNED | | Synonyms: | 2-Pyridinecarboxamide, N-[[1-[2-[[4-[(Z)-[[(3-bromophenyl)methyl]amino](hydroxyimino)methyl]-1,2,5-oxadiazol-3-yl]amino]ethyl]-1H-1,2,3-triazol-4-yl]methyl]- | | CAS: | 2803768-09-2 | | MF: | C21H21BrN10O3 | | MW: | 541.36 | | EINECS: | | | Product Categories: | | | Mol File: | 2803768-09-2.mol |  |
| | INDEX NAME NOT YET ASSIGNED Chemical Properties |
| density | 1.67±0.1 g/cm3(Predicted) | | pka | 6.12±0.69(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | INDEX NAME NOT YET ASSIGNED Usage And Synthesis |
| Uses | 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[1]. | | 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-∞) (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 |
| 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%.
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| 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.
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| 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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| | IC 50 | IDO1: 411 nM (IC50); IDO2: 112 (IC50) | | References | [1] He G, et al. Discovery of the First Selective IDO2 Inhibitor As Novel Immunotherapeutic Avenues for Rheumatoid Arthritis. J Med Chem. 2022 Aug 11. DOI:10.1021/acs.jmedchem.2c00263 |
| | INDEX NAME NOT YET ASSIGNED Preparation Products And Raw materials |
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