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ChemicalBook--->CAS DataBase List--->1246207-65-7

1246207-65-7

1246207-65-7 Structure

1246207-65-7 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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
1246207-65-7 suppliers list
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