Identification | Back Directory | [Name]
Ethanone, 1-[7-[2-amino-6-(4-methyl-1-piperazinyl)-4-pyrimidinyl]-3,4-dihydro-2(1H)-isoquinolinyl]-2-cyclopentyl- | [CAS]
1246207-65-7 | [Synonyms]
INCB38579 Ethanone, 1-[7-[2-amino-6-(4-methyl-1-piperazinyl)-4-pyrimidinyl]-3,4-dihydro-2(1H)-isoquinolinyl]-2-cyclopentyl- | [Molecular Formula]
C25H34N6O | [MOL File]
1246207-65-7.mol | [Molecular Weight]
434.58 |
Chemical Properties | Back Directory | [Boiling point ]
715.8±70.0 °C(Predicted) | [density ]
1.204±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 230 mg/mL (529.25 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
7.98±0.10(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Uses]
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]. | [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. |
| [IC 50]
Human H4 Receptor: 4.8 nM (IC50); Mouse H4 Receptor: 42 nM (IC50); Rat H4 receptor: 21 nM (IC50) | [References]
[1] Niu Shin, et al. INCB38579, a novel and potent histamine H? receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions. Eur J Pharmacol. 2012 Jan 30;675(1-3):47-56. DOI:10.1016/j.ejphar.2011.11.027 |
|
|