HB-0043
HB-0043 is a IL-17A and IL-36R antagonist. HB-0043 blocks IL-17A- and IL-36R-mediated signaling pathways, inhibits the production of inflammatory cytokines, and reduces the secretion of pro-inflammatory cytokines IL-6 and IL-8. HB-0043 alleviates skin thickening and inflammatory responses in oxazolone-induced and Imiquimod (HY-B0180)-induced skin reaction mouse models. HB-0043 is applicable for the research of atopic dermatitis and psoriasis.
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Activité biologique
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Chemical Information
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Activité biologique
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IL-17A |
IL-6 |
IL-8 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | IC50 |
0.07 nM
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Neutralization of IL-17A-mediated IL-6 secretion in human fibrosarcoma HT1080 cells incubated for 24 hours, measured via ELISA.
Neutralization of IL-17A-mediated IL-6 secretion in human fibrosarcoma HT1080 cells incubated for 24 hours, measured via ELISA.
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39600699 |
| NCI/ADR-RES | IC50 |
0.87 nM
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Blocking of IL-36R-mediated IL-6 secretion in human ovarian cancer NCI/ADR-RES cells incubated for 4 hours, measured via ELISA.
Blocking of IL-36R-mediated IL-6 secretion in human ovarian cancer NCI/ADR-RES cells incubated for 4 hours, measured via ELISA.
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39600699 |
HB0043 possesses Kd values of 0.01 nM for human IL‑17A, 0.13 nM for cynomolgus monkey IL‑17A, 3.66 nM for rabbit IL‑17A, 4.54 nM for rat IL‑17A, 0.49 nM for mouse IL‑17A, 0.78 nM for human IL‑36R, and 12.00 nM for cynomolgus monkey IL‑36R[1].
HB0043 (24 h) neutralizes the IL-17A signaling pathway in HT1080 cells with an IC50 of 0.07 nM, and blocks the IL-36R signaling pathway in NCI/ADR-RES cells with an IC50 of 0.87 nM[1].
HB0043 (24 h) potently inhibits the secretion of IL-6 and IL-8 in NHDF co-stimulated with IL-17A and IL-36, and its efficacy is superior to that of the parental monoclonal antibodies targeting IL-17A or IL-36R alone[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkey (5 animals/sex per group)[1]
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Dosage:20 mg/kg; 100 mg/kg; 200 mg/kg
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Administration:i.v.; once per week; 4 weeks
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Result:Determined the No Observed Adverse Effect Level (NOAEL) to be 200 mg/kg.
Increased globulin (GLB) and decreased albumin/globulin (A/G) ratio after the 3rd and 5th doses in the 200 mg/kg group.
Increased total protein (TP) in males of the 200 mg/kg group.
Increased IgG in the 100 and 200 mg/kg groups.
Induced mild to moderate subcutaneous inflammation at the administration site.
Observed no significant changes in body temperature, electrocardiogram, coagulation function, lymphocyte subsets, or urinalysis.
Chemical Information
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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)
HB-0043 Related Classifications
HY-P992521 Related Classifications
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