INCB38579|cas:1246207-65-7|西域试剂

INCB38579,99.97%

产品编号：Bellancom-101188| CAS NO：1246207-65-7| 分子式：C₂₅H₃₄N₆O| 分子量：434.58

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-101188	￥3500.00	杭州北京（现货）
Bellancom-101188	￥6000.00	杭州北京（现货）
Bellancom-101188	￥12500.00	杭州北京（现货）

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INCB38579

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。

生物活性

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.

体外研究

INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H₄ 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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

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.

体内研究
(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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式