1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. INCB38579

INCB38579 

Cat. No.: HY-101188
Handling Instructions

INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities.

For research use only. We do not sell to patients.

INCB38579 Chemical Structure

INCB38579 Chemical Structure

CAS No. : 1246207-65-7

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Description

INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities[1].

IC50 & Target[1]

Human H4 Receptor

4.8 nM (IC50)

Mouse H4 Receptor

42 nM (IC50)

Rat H4 receptor

21 nM (IC50)

In Vitro

INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H4 receptors[1].
INCB38579 (0.1 nM-10 μM; 20 min) blocks histamine-induced migration of dendritic cells differentiated from human monocytes and mouse bone marrow cells[1].
NCB38579 (0-30 nM; 1.5 h) inhibits histamine-induced cell shape change and migration of purified human eosinophils dose-dependently[1].

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

Cell Viability Assay[1]

Cell Line: HEK293 cells
Concentration: 0.1 nM-10 μM
Incubation Time: 1.5 hours
Result: Showed the IC50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H4 receptors, respectively.

Cell Viability Assay[1]

Cell Line: Human monocytes, mouse bone marrow cells, and human eosinophils
Concentration: 0.1 nM-10 μM
Incubation Time: 20 min
Result: Showed IC50s of 13.2 and 77 nM for human monocytes and mouse bone marrow cells,respectively.
Showed IC50 values of approximately 20-30 nM for purified human eosinophils.

Cell Viability Assay[1]

Cell Line: HEK293 cells
Concentration: 0-30 nM
Incubation Time: 1.5 hours
Result: Showed the IC50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H4 receptors, respectively.
In Vivo

INCB38579 (oral gavage; 100 mg/kg; once) inhibits histamine-mediated pruritus in mice[1].
INCB38579 (oral gavage; 100 mg/kg; once) shows antinociceptive functions in this acute model of inflammatory pain[1].
INCB38579 (oral gavage; 3, 10, 30, and 100 mg/kg; once) inhibits formalin-induced pain in rats and mice[1].

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

Animal Model: Female CD-1 mice histamine-induced pruritus[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 100 mg/kg; once
Result: Reduced the number of scratching bouts significantly (P<0.05).
Animal Model: Sprague-Dawley rats injected with carrageenan[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 100 mg/kg; once
Result: Increased the paw withdrawal threshold from a baseline of 61 g to approximately 100 g, achieving approximately 60% in maximal possible effect.
Animal Model: Male Sprague–Dawley rats and male ICR mice injected with formalin into the hind paws[1]
Dosage: 3, 10, 30, and 100 mg/kg
Administration: Oral gavage; 3, 10, 30, and 100 mg/kg; once
Result: Showed a significant dose-dependent analgesic effect from 10 to 100 mg/kg in the phase 1 response and 30 to 100 mg/kg in the phase 2 response in the mouse formalin test.
Observed a dose-dependent and statistically significant effect in the phase 1 response, ranging from10 to 100 mg/kg, in the rat formalin test.
Molecular Weight

434.58

Formula

C25H34N6O

CAS No.
SMILES

O=C(CC1CCCC1)N2CCC3=CC=C(C4=NC(N)=NC(N5CCN(C)CC5)=C4)C=C3C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 230 mg/mL (529.25 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3011 mL 11.5054 mL 23.0107 mL
5 mM 0.4602 mL 2.3011 mL 4.6021 mL
10 mM 0.2301 mL 1.1505 mL 2.3011 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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INCB38579
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HY-101188
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