IHCH-8110
IHCH-8110 is a peripherally restricted, non-brain-penetrant 5-HT2AR and 5-HT2CR agonist (Ki=47.86 nM) that antagonizes 5-HT2BR. IHCH-8110 induces CXCL10 and IL-18 expression by activating 5-HT2AR on enteric glial cells, thereby promoting CD8+ T cell recruitment and effector polarization, and avoids the risk of cardiac valvulopathy associated with 5-HT2BR activation. IHCH-8110 exhibits a low risk of hERG channel inhibition (IC50=5.96 μM) and is well tolerated, sensitizing immunologically cold colorectal cancer to PD-1 blockade therapy, making it suitable for research related to colorectal cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3078735-55-1
- 分子式: C21H35N3O2
- 分子量:361.52
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
5-HT2A Receptor 47.86 nM (Ki) |
5-HT2B Receptor |
5-HT2C Receptor |
体外実験
体内実験
IHCH-8110 (10 mg/kg; i.p.; daily; 10 days) suppresses colorectal cancer progression via activating 5-HT2AR on enteric glial cells to enhance CD8+ T cell recruitment and cytotoxicity[1].
IHCH-8110 (10 mg/kg; i.p.; daily) in combination with anti-PD-1 suppresses primary tumor growth and liver metastasis in the aggressive AKPS CRC model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (mixed-sex, 6-10 weeks)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Inhibited MC38 tumor growth, reducing tumor volume and tumor weight at 10 mg/kg.
Increased the ratio and number of tumor-infiltrating T cells, specifically CD8+ T cells.
Enhanced tumor infiltration of cytotoxic CD8+ T cell subsets (IFN-γ+, TNF-α+, GZMB+, PD-1+).
Inhibited tumor growth in the MC38-OVA model with an increased ratio of OVA-specific CD8+ T cells.
Completely abolished antitumor effects upon CD8+ T cell depletion.
In combination with anti-PD-1, led to complete tumor rejection in most mice by day 10.
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Animal Model:C57BL/6J (mixed-sex, 6-10 weeks; Htr2a^flox/flox and Htr2a^ΔEGC)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Reduced tumor volume and tumor weight in Htr2a^flox/flox mice.
Increased tumor-infiltrating CD8+ T cells (IFN-γ+, TNF-α+, GZMB+, PD-1+) in Htr2a^flox/flox mice.
Failed to suppress tumor progression and did not increase CD8+ T cells in Htr2a^ΔEGC mice.
Antitumor effects were largely abrogated in Cxcl10^ΔEGC mice.
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Animal Model:C57BL/6J (mixed-sex, 6-10 weeks; Htr2a^flox/flox and Htr2a^ΔEGC)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Markedly reduced tumor volume and tumor weight in AKP tumors.
Substantially increased the proportion and number of tumor-infiltrating CD8+ T cells.
Reduced tumor volume and weight and increased CD8+ T cells in Htr2a^flox/flox mice.
Failed to suppress tumor progression and did not increase CD8+ T cells in Htr2a^ΔEGC mice.
In combination with anti-PD-1, synergistically enhanced the antitumor effect, leading to maximal inhibition of AKP tumor growth.
化学情報
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CAS 番号 3078735-55-1
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分子量 361.52
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分子式 C21H35N3O2
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SMILES
CCCCCCOC1=CC=C(C=C1)CNC(N([C@@H]2CC[C@H](CC2)N)C)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
IHCH-8110 関連分類
HY-189235 関連分類
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