产品
编 号：F755589
分子式：C29H41F2N5
分子量：497.67
分子式：C29H41F2N5
分子量：497.67
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CAS No: 2761009-30-5
产品详情
生物活性：
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).
体内研究：
CXCR4 antagonist 4 (3, 10, 30 mg/kg) demonstrates better oral Bioavailability in a dose dependent and reached 27% for the 30 mg/kg.Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice.RouteDose(mg/kg)T1/2(h) Cmax(ng/mL) C12h (ng/mL)AUC0-8h(h*ng/mL)% FPO (0-8 h) Cl (L/h/kg)Vd (L/kg)
iv35.8911626511.396.3
po312.81.5034.312.9
po1054.814.3190215
po3016934.871727.1
Animal Model:mice
Dosage:3, 10, 30 mg/kg
Administration:
Result:Demonstrated better oral bioavailability in a dose dependent and reached 27% for the 30 mg/kg.
体外研究：
CXCR4 antagonist 4 (Compound 30, 0.1~10 μM, 48 hours) displays the inhibition potencies against the X4 virus in TZM-bl cells (IC50=7 nM) .
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).
体内研究：
CXCR4 antagonist 4 (3, 10, 30 mg/kg) demonstrates better oral Bioavailability in a dose dependent and reached 27% for the 30 mg/kg.Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice.RouteDose(mg/kg)T1/2(h) Cmax(ng/mL) C12h (ng/mL)AUC0-8h(h*ng/mL)% FPO (0-8 h) Cl (L/h/kg)Vd (L/kg)
iv35.8911626511.396.3
po312.81.5034.312.9
po1054.814.3190215
po3016934.871727.1
Animal Model:mice
Dosage:3, 10, 30 mg/kg
Administration:
Result:Demonstrated better oral bioavailability in a dose dependent and reached 27% for the 30 mg/kg.
体外研究：
CXCR4 antagonist 4 (Compound 30, 0.1~10 μM, 48 hours) displays the inhibition potencies against the X4 virus in TZM-bl cells (IC50=7 nM) .
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