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

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.

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INCB38579 Chemical Structure

INCB38579 Chemical Structure

CAS No. : 1246207-65-7

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Based on 1 publication(s) in Google Scholar

INCB38579 Related Antibodies

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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].

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

INCB38579 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

Off-white to light yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 230 mg/mL (529.25 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3011 mL 11.5054 mL 23.0107 mL 57.5268 mL
5 mM 0.4602 mL 2.3011 mL 4.6021 mL 11.5054 mL
10 mM 0.2301 mL 1.1505 mL 2.3011 mL 5.7527 mL
15 mM 0.1534 mL 0.7670 mL 1.5340 mL 3.8351 mL
20 mM 0.1151 mL 0.5753 mL 1.1505 mL 2.8763 mL
25 mM 0.0920 mL 0.4602 mL 0.9204 mL 2.3011 mL
30 mM 0.0767 mL 0.3835 mL 0.7670 mL 1.9176 mL
40 mM 0.0575 mL 0.2876 mL 0.5753 mL 1.4382 mL
50 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1505 mL
60 mM 0.0384 mL 0.1918 mL 0.3835 mL 0.9588 mL
80 mM 0.0288 mL 0.1438 mL 0.2876 mL 0.7191 mL
100 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
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INCB38579 Related Classifications

Help & FAQs
  • 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.

Keywords:

INCB385791246207-65-7INCB 38579INCB-38579Histamine Receptororal activityhighly brain penetrableanti-inflammatory painanti-pruritic activityHEK293human monocytesmouse bone marrow celland human eosinophilsInhibitorinhibitorinhibit

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