1246207-65-7
1246207-65-7 structure
- Name: INCB38579
- Chemical Name: INCB38579
- CAS Number: 1246207-65-7
- Molecular Formula: C25H34N6O
- Molecular Weight: 434.58
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2022-10-12 05:26:27
- Modify Date: 2024-04-03 15:23:08
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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[1].
| Name | INCB38579 |
|---|
| 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]. |
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| Related Catalog | |
| Target |
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]. 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]. 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. |
| References |
| Molecular Formula | C25H34N6O |
|---|---|
| Molecular Weight | 434.58 |