产品
编 号:F754391
分子式:C23H27F3N4O
分子量:432.48
产品类型
结构图
CAS No: 2649803-05-2
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产品详情
生物活性:
VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4.
体内研究:
VU6028418 is orally bioavailable.In Vivo PK Parameters for VU6028418parameterrat(SD)a mouse(CD-1)a dog(beagle)a
dose (mg/kg) iv/po1/101/31/3
CLp (mL/min/kg)6.11743
Vss (L/kg)6.710.68.5
elimination t1/2 (h)13NC15
Cmax (ng/mL) po17 00018170
Tmax (h) po1.56.6717
AUC0-inf (ng/mL?h) po30 000NC1100
F (%) po≥100≥10086
total brain/total plasma (Kp)6.4NDND
unbound brain/unbound plasma (Kp,uu)0.61NDND
CSF/plasma unbound (Kp,u)0.24NDND
a Values represent means from two to three animals. ND = not determined. NC = not calculated; there was insufficient data to define the elimination phase (i.e., Cmax was one of the last three time points).Animal Model:SD rat, CD-1 mouse and beagle dog
Dosage:1, 3 and 10 mg/kg
Administration:Intravenous injection or oral administration (Pharmacokinetic Analysis)
Result:Showed good pharmacokinetic results.