2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. INCB38579

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。

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INCB38579 Chemical Structure

INCB38579 Chemical Structure

CAS No. : 1246207-65-7

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥3300
In-stock
1 mg ￥1363
In-stock
5 mg ￥3000
In-stock
10 mg ￥4500
In-stock
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

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Customer Review

INCB38579 相关抗体

Top Publications Citing Use of Products

查看 Histamine Receptor 亚型特异性产品:

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target[1]

Human H4 Receptor

4.8 nM (IC50)

Mouse H4 Receptor

42 nM (IC50)

Rat H4 receptor

21 nM (IC50)

体外研究
(In Vitro)

INCB38579 (0.1 nM-10 μM；1.5 小时) 抑制组胺与重组人和啮齿动物组胺 H4 受体的结合[1]。
INCB38579 (0.1 nM-10 μM；20 分钟) 阻断组胺诱导的人单核细胞和小鼠骨髓细胞分化的树突状细胞迁移[1]。
NCB38579 (0-30 nM；1.5 小时) 剂量依赖性地抑制组胺诱导的细胞形状变化和纯化人嗜酸性粒细胞的迁移[1]。

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

INCB38579 相关抗体:

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.
体内研究
(In Vivo)

INCB38579 (口服灌胃；100 mg/kg；一次) 抑制小鼠组胺介导的瘙痒症[1]。
INCB38579 (口服强饲法；100 mg/kg；一次) 在这种炎症性疼痛的急性模型中表现出镇痛功能[1]。
INCB38579 (口服灌胃；3、10、30 和 100 mg/kg；一次) 抑制大鼠和小鼠福尔马林诱导的疼痛[1]。

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

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

Formula

C25H34N6O
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 230 mg/mL (529.25 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

INCB38579 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3011 mL 11.5054 mL 23.0107 mL 57.5268 mL
5 mM 0.4602 mL 2.3011 mL 4.6021 mL 11.5054 mL
10 mM 0.2301 mL 1.1505 mL 2.3011 mL 5.7527 mL
15 mM 0.1534 mL 0.7670 mL 1.5340 mL 3.8351 mL
20 mM 0.1151 mL 0.5753 mL 1.1505 mL 2.8763 mL
25 mM 0.0920 mL 0.4602 mL 0.9204 mL 2.3011 mL
30 mM 0.0767 mL 0.3835 mL 0.7670 mL 1.9176 mL
40 mM 0.0575 mL 0.2876 mL 0.5753 mL 1.4382 mL
50 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1505 mL
60 mM 0.0384 mL 0.1918 mL 0.3835 mL 0.9588 mL
80 mM 0.0288 mL 0.1438 mL 0.2876 mL 0.7191 mL
100 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

INCB385791246207-65-7INCB 38579INCB-38579Histamine Receptororal activityhighly brain penetrableanti-inflammatory painanti-pruritic activityHEK293human monocytesmouse bone marrow celland human eosinophilsInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-101188
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