Art. -Nr.: HY-101188

INCB38579

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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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Reinheit: 99.33%
CAS. Nr.: 1246207-65-7
Formel: C₂₅H₃₄N₆O
Molecular Weight:434.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

INCB38579 Chemical Structure

CAS. Nr.: 1246207-65-7

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Human H₄ Receptor

4.8 nM (IC₅₀)

Mouse H₄ Receptor

42 nM (IC₅₀)

Rat H₄ receptor

21 nM (IC₅₀)

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 1246207-65-7
Appearance Solid
Molecular Weight 434.58
Formel C₂₅H₃₄N₆O
Color Off-white to light yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Niu Shin, et al. INCB38579, a novel and potent histamine H₄ receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions. Eur J Pharmacol. 2012 Jan 30;675(1-3):47-56. [Content Brief]

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.

Complete Stock Solution Preparation Table

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

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

INCB38579

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

INCB38579 Related Classifications

HY-101188 Related Classifications