INCB38579 - ≥99% , CAS No.1246207-65-7

CAS: 1246207-65-7 Cat. No.: I649402 Fórmula: C₂₅H₃₄N₆O Peso molecular: 434.58

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Visão geral

INCB38579 is an orally active, highly brain penetrable, and selective histamine H 4 receptor (HH 4 R) antagonist (hH 4 R IC 50 =4.8 nM, mH 4 R IC 50 =42 nM, rH 4 R IC 50 =32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities

In Vitro

INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H 4 receptors. INCB38579 (0.1 nM-10 μM; 20 min) blocks histamine-induced migration of dendritic cells differentiated from human monocytes and mouse bone marrow cells. NCB38579 (0-30 nM; 1.5 h) inhibits histamine-induced cell shape change and migration of purified human eosinophils dose-dependently. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HEK293 cells Concentration: 0.1 nM-10 μM Incubation Time: 1.5 hours Result: Showed the IC 50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H 4 receptors, respectively. Cell Viability AssayCell Line: Human monocytes, mouse bone marrow cells, and human eosinophils Concentration: 0.1 nM-10 μM Incubation Time: 20 min Result: Showed IC 50 s of 13.2 and 77 nM for human monocytes and mouse bone marrow cells，respectively. Showed IC 50 values of approximately 20-30 nM for purified human eosinophils. Cell Viability AssayCell Line: HEK293 cells Concentration: 0-30 nM Incubation Time: 1.5 hours Result: Showed the IC 50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H 4 receptors, respectively.

In Vivo

INCB38579 (oral gavage; 100 mg/kg; once) inhibits histamine-mediated pruritus in mice . INCB38579 (oral gavage; 100 mg/kg; once) shows antinociceptive functions in this acute model of inflammatory pain . INCB38579 (oral gavage; 3, 10, 30, and 100 mg/kg; once) inhibits formalin-induced pain in rats and mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD-1 mice histamine-induced pruritus 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 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 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.

Form:Solid

IC50& Target:Human H 4 Receptor 4.8 nM (IC 50 ) Mouse H 4 Receptor 42 nM (IC 50 ) Rat H 4 receptor 21 nM (IC 50 )

Specifications

Especificações e pureza

≥99%

Mecanismos bioquímicos e fisiológicos

INCB38579 is an orally active, highly brain penetrable, and selective histamine H 4 receptor (HH 4 R) antagonist (hH 4 R IC 50 =4.8 nM, mH 4 R IC 50 =42 nM, rH 4 R IC 50 =32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities.

Condições de armazenamento de armazenamento

Store at -20°C

Enviado em

Ice chest + Ice pads

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

ANTAGONIST

Pureza

≥99%

Nomes e identificadores

• Peso molecular: 434.58

Propriedades químicas e físicas

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

Perguntas frequentes

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1246207-65-7, the molecular formula is C25H34N6O, and the molecular weight is 434.58 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.