APG-2305
APG-2305 is a selective IL-23 receptor inhibitor. APG-2305 inhibits IL-23-induced STAT3 phosphorylation, reduces the expression of pro-inflammatory cytokines (IL-1, IL-6, IL-22) without altering IL-17 levels, and alleviates inflammation in multiple in vivo models. APG-2305 is used for research on inflammatory autoimmune diseases.
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- Formule: C44H66N10O19
- Masse moléculaire:1039.05
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[2]|
STAT3 |
IL-1 |
IL-6 |
IL-22 |
IL-23 |
In Vitro
APG-2305 (30 min) potently inhibits IL-23-induced STAT3 phosphorylation in primary mouse spleen cells with an IC50 of 1.5 nM[2].
APG-2305 (1 μM; 30 min) exhibits functional selectivity in IL-23R/IL-12Rβ1-expressing HEK-293 cells, inhibiting IL-23-induced expression of IL-1β, IL-6, and IL-22 but not IL-17A, p35, or p40[2].
APG-2305 selectively inhibits IL-23-induced IL-6 and IL-22 production but not IL-17 production in primary mouse spleen cells[2].
APG-2305 (1 μM; 30 min) inhibits IL-23-induced IL-1β and IL-6 gene expression but not IL-17 expression in Jurkat T-lymphocyte cells[2].
APG-2305 (1 μM; 30 min) does not modulate IL-12-induced cytokine gene expression in IL-12Rβ1/IL-12Rβ2-expressing HEK-293 cells[2].
APG-2305 (1 μM; 30 min) exerts a minimal effect on IL-23-induced cytokine expression in Raw Blue mouse macrophage cells[2].
APG-2305 (1 μM; 30 min) selectively inhibits IL-23-induced IL-1β and IL-6 gene expression but not IL-17 expression in human rheumatoid arthritis synoviocytes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IL-23R/IL-12Rβ1-expressing HEK-293 cells
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Concentration:1 μM (preincubation)
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Incubation Time:30 min (preincubation); 4 h (IL-23 incubation)
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Result:Effectively reduced IL-1β, IL-6, and IL-22 gene expression in IL-23-stimulated HEK-293 cells expressing the IL-23 receptor.
Did not significantly reduce IL-23-induced IL-17A, p35, and p40 mRNA levels.
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Cell Line:Jurkat T-lymphocyte cells
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Concentration:1 μM (preincubation)
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Incubation Time:30 min (preincubation); 4 h (IL-23 incubation)
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Result:Significantly reduced IL-23-induced gene expression of IL-1β and IL-6 in Jurkat cells.
Did not reduce IL-17 gene expression.
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Cell Line:IL-12Rβ1/IL-12Rβ2-expressing HEK-293 cells
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Concentration:1 μM (preincubation)
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Incubation Time:30 min (preincubation); 4 h (IL-12 incubation)
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Result:Did not interfere with IL-12-induced expression of IL-22, p35, and p40 genes in IL-12R-expressing HEK-293 cells.
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Cell Line:Raw Blue mouse macrophage cells
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Concentration:1 μM (preincubation); 100 ng/mL (ionomycin, pretreatment); 20 ng/mL (phorbol 12-myristate 13-acetate, pretreatment)
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Incubation Time:30 min (preincubation); 24 h (ionomycin/phorbol 12-myristate 13-acetate pretreatment); 4 h (IL-23 incubation)
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Result:Had only a minor effect on IL-23-induced IL-1β and IL-6 gene expression in Raw Blue mouse macrophages.
In Vivo
APG-2305 (10 mg/kg; i.p.) selectively attenuates a subset of serum inflammatory cytokines in anti-CD40-induced systemic inflammation, with no effect on liver inflammation[2].
APG-2305 (5 mg/kg; i.p.; twice daily; 21 days) inhibits 80% of clinical arthritis signs and reduces joint damage in the Collagen-induced arthritis mouse model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice (male, 5 weeks old, ear inflammation induced by daily intradermal injection of mIL-23 into the external earlobe for 5 days)[2]
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Dosage:5 mg/kg (total 10 mg·kg-1·day-1)
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Administration:i.p.; twice daily; 5 days
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Result:Inhibited ~50% of IL-23-induced ear edema.
Inhibited 50-75% of IL-1β, IL-6, and IL-22 mRNA expression induced by IL-23 in ear tissue.
Did not decrease IL-17 mRNA levels significantly.
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Animal Model:C57BL/6 mice (male, 8-12 weeks old, systemic inflammation induced by a single intraperitoneal injection of anti-CD40 antibody)[2]
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Dosage:10 mg/kg
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Administration:i.p.; once daily
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Result:Significantly attenuated serum levels of IL-2, IL-6, IL-12p70, IFN-γ, and CXCL1 induced by anti-CD40.
Decreased serum levels of IL-12p40, TNF-α, and CCL2 only marginally.
Did not reduce the severity of liver inflammation induced by anti-CD40.
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Animal Model:DBA/1J mice (male, 8 weeks old, rheumatoid arthritis induced by intradermal immunization with bovine type II collagen emulsified in complete Freund's adjuvant at the base of the tail, followed by a boost with collagen in incomplete Freund's adjuvant on day 21)[2]
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Dosage:5 mg/kg
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Administration:i.p.; twice daily; 21 days
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Result:Inhibited 80% of the clinical signs of collagen-induced arthritis, as measured by daily clinical scores and area under the clinical score curve.
Showed diminished joint damage in treated animals via radiological examination.
Revealed markedly reduced inflammatory signs in arthritic paws via histologic evaluation.
Chemical Information
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Masse moléculaire 1039.05
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Formule C44H66N10O19
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SMILES
O=C(N[C@H](CCC(O)=O)C(N[C@H](CCC(O)=O)C(N[C@H](CCC(O)=O)C(N[C@H](CCC(N)=O)C(N[C@H](CCC(N)=O)C(N[C@H](CC(C)C)C(N[C@H](CC1=CC=C(C=C1)O)C(O)=O)=O)=O)=O)=O)=O)=O)[C@@H]([C@@H](O)C)N
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Sequence
D{Thr-Glu-Glu-Glu-Gln-Gln-Leu-Tyr}
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Sequence Shortening
D{TEEEQQLY}
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
APG-2305 Related Classifications
HY-P12213 Related Classifications
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