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Art. -Nr.: HY-189235

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IHCH-8110

IHCH-8110 is a peripherally restricted, non-brain-penetrant 5-HT_2AR and 5-HT_2CR agonist (K_i=47.86 nM) that antagonizes 5-HT_2BR. IHCH-8110 induces CXCL10 and IL-18 expression by activating 5-HT_2AR on enteric glial cells, thereby promoting CD8⁺ T cell recruitment and effector polarization, and avoids the risk of cardiac valvulopathy associated with 5-HT_2BR 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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3078735-55-1
Formel: C₂₁H₃₅N₃O₂
Molecular Weight:361.52

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

IHCH-8110 Chemical Structure

CAS. Nr.: 3078735-55-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

5-HT_2A Receptor

47.86 nM (Ki)

5-HT_2B Receptor

5-HT_2C Receptor

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

IHCH-8110 exhibits high binding affinity for the 5-HT_2AR with a K_i of 47.86 nM^[1].
IHCH-8110 (2-8 μM; 24 h) does not directly enhance CD8⁺ T cell migration or cytotoxicity in vitro^[1].

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

In Vivo

IHCH-8110 (1-10 mg/kg; i.p.; daily; 10 days) suppresses MC38 colorectal cancer progression by enhancing CD8⁺ T cell recruitment and cytotoxicity, and synergistically enhances the efficacy of anti-PD-1 therapy^[1].
IHCH-8110 (10 mg/kg; i.p.; daily; 10 days) suppresses colorectal cancer progression via activating 5-HT_2AR 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.

Animal Model:

C57BL/6J (mixed-sex, 6-10 weeks)^[1]
Dosage:

1 mg/kg; 10 mg/kg
Administration:

i.p.; daily; 10 days
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.

Animal Model:

C57BL/6J (mixed-sex, 6-10 weeks; Htr2a^flox/flox and Htr2a^ΔEGC)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; daily; 10 days
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.

Animal Model:

C57BL/6J (mixed-sex, 6-10 weeks; Htr2a^flox/flox and Htr2a^ΔEGC)^[1]
Dosage:

1 mg/kg; 10 mg/kg
Administration:

i.p.; daily; 10 days
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.

Chemical Information

CAS. Nr. 3078735-55-1
Molecular Weight 361.52
Formel C₂₁H₃₅N₃O₂
SMILES

CCCCCCOC1=CC=C(C=C1)CNC(N([C@@H]2CC[C@H](CC2)N)C)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wen Y, et al. Targeting peripheral 5-HTR enhances antitumor immunity in colorectal cancer. Cell. 2026 Sep 03;189(18):5688-5705.e13.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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