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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)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg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 (hH4RIC50=4.8 nM, mH4RIC50=42 nM, rH4RIC50=32 nM)。INCB38579 具有抗炎和抗瘙痒的活性。
生物活性

INCB38579 is an orally active, highly brain penetrable, and selective histamineH4receptor(HH4R) antagonist (hH4RIC50=4.8 nM, mH4RIC50=42 nM, rH4RIC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities[1].

IC50& Target[1]

Human H4Receptor

4.8 nM (IC50)

Mouse H4Receptor

42 nM (IC50)

Rat H4receptor

21 nM (IC50)

体外研究
(In Vitro)

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.
体内研究
(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.
分子量

434.58

性状

Solid

Formula

C25H34N6O

CAS 号

1246207-65-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 230 mg/mL(529.25 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3011 mL11.5054 mL23.0107 mL
5 mM0.4602 mL2.3011 mL4.6021 mL
10 mM0.2301 mL1.1505 mL2.3011 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。