INCB38579
目录号 : GC65937
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
Sample solution is provided at 25 µL, 10mM.
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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].
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. |
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. |
| Cas No. | 1246207-65-7 | SDF | Download SDF |
| 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 tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet