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INCB38579
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
INCB38579图片
CAS NO:1246207-65-7
包装与价格:
包装价格(元)
10mg电议
25mg电议

产品介绍
INCB38579 是一种具有口服活性、高度脑穿透和选择性的组胺 H4 受体 (HH4R) 拮抗剂 (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM)。INCB38579 具有抗炎和抗瘙痒的活性。
Cas No.1246207-65-7
分子式C25H34N6O
分子量434.58
溶解度DMSO : 230 mg/mL (529.25 mM; ultrasonic and warming and heat to 60°C)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

INCB38579 is an orally active, highly brain penetrable, and selective histamine H4receptor (HH4R) antagonist (hH4RIC50=4.8 nM, mH4RIC50=42 nM, rH4RIC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities[1].

INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H4receptors[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 IC50values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H4receptors, 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 IC50values 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 IC50values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H4receptors, respectively.

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.