1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. Aryl Hydrocarbon Receptor Cytochrome P450
  3. AHR agonist 10

AHR agonist 10 (B19) is a potent AHR agonist (EC50 = 2.01 nM). AHR agonist 10 can elevate the transcript levels of key AHR downstream pathway target genes, including CYP1A1 and CYP1B1. AHR agonist 10 can downregulate the expression levels of CD36, IL-18 and shows low cytotoxicity (>40 μM) to normal cells. AHR agonist 10 can suppress the expression of CCL5, CCL20, IL-6, IL-8, S100A9, TLR4, TNF-α, and TNFR1, demonstrating that AHR agonist 10 effectively modulate inflammatory responses through AHR dependent signaling pathways. AHR agonist 10 can be used for psoriasis research.

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AHR agonist 10

AHR agonist 10 Chemical Structure

CAS No. : 1191937-43-5

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Description

AHR agonist 10 (B19) is a potent AHR agonist (EC50 = 2.01 nM). AHR agonist 10 can elevate the transcript levels of key AHR downstream pathway target genes, including CYP1A1 and CYP1B1. AHR agonist 10 can downregulate the expression levels of CD36, IL-18 and shows low cytotoxicity (>40 μM) to normal cells. AHR agonist 10 can suppress the expression of CCL5, CCL20, IL-6, IL-8, S100A9, TLR4, TNF-α, and TNFR1, demonstrating that AHR agonist 10 effectively modulate inflammatory responses through AHR dependent signaling pathways. AHR agonist 10 can be used for psoriasis research[1].

In Vitro

AHR agonist 10 (10 μM, 20 μM, 24 h) can effectively enhance the expression levels of CYP1A1 and CYP1B1 in the AHR knockdown HaCaT cells[1].
AHR agonist 10 (5 μM) can suppress the expression on the mRNA level of CYP1A1, CYP1B1, CCL5, CCL20, IL-6, IL-8, S100A9, TLR4, TNF-α, and TNFR1 on the Lipopolysaccharides (HY-D1056) (LPS)-induced HaCaT cell[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: AHR knockdown HaCaT cell
Concentration: 10 μM , 20 μM
Incubation Time: 24 h
Result: Enhanced the expression levels of CYP1A1 and CYP1B1 on the HaCaT cells.
In Vivo

AHR agonist 10 (1%, topical application, once daily, 7 days) inhibits the onset and progression of Imiquimod (HY-B0180)-induced psoriasis symptoms on the mice’s backs, marked by reduced erythema and scaling[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Babl/C mice (7-8 weeks old) were administered topically with Imiquimod (62.5 mg/mouse) on the hair-free back[1].
Dosage: 1%
Administration: Topical application, once daily, 7 days.
Result: Exhibited the ability to decrease the thickness of the stratum corneum and stratum spinosum of the skin , ameliorating epidermal hyperplasia.
Downregulated the expression of Ki67 and PCNA.
Mitigated psoriasis-associated epidermal hyperplasia by curbing excessive epidermal cell proliferation.
Enhanced the expression levels of ZO-1 and occludin.
Downregulated the expression levels of IL-17, IL-23, and IL-17F, effectively halting the progression of psoriasis by disrupting the responsible cytokine cascade and subsequent inflammatory response.
Effectively activated the AHR pathway, leading to enhanced expression levels of CYP1A1, CYP1B1, and HSP90.
Molecular Weight

284.35

Formula

C18H20O3

CAS No.
SMILES

CC(C1=C(C=C(C=C1O)/C=C/C2=CC=C(C=C2)OC)O)C

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Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AHR agonist 10
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HY-178053
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