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) |
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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. |
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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. |
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| 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 |
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| 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 | 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℃, 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。 |
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