VU6028418 is a potent, highly selective and orally bioavailable M 4 mAChR antagonist with an IC 50 of 4.1 nM against hM 4
In Vivo
VU6028418 is orally bioavailable . In Vivo PK Parameters for VU6028418 parameter rat (SD) a mouse (CD-1) a dog (beagle) a dose (mg/kg) iv/po 1/10 1/3 1/3 CL p (mL/min/kg) 6.1 17 43 V ss (L/kg) 6.7 10.6 8.5 elimination t 1/2 (h) 13 NC 15 C max (ng/mL) po 17 000 181 70 T max (h) po 1.5 6.67 17 AUC 0-inf (ng/mL•h) po 30 000 NC 1100 F (%) po ≥100 ≥100 86 total brain/total plasma (K p ) 6.4 ND ND unbound brain/unbound plasma (K p,uu ) 0.61 ND ND CSF/plasma unbound (K p,u ) 0.24 ND ND 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., C max was one of the last three time points). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
Form:Solid
IC50& Target:mAChR4
사양
사양 및 순도
≥99%
생화학 및 생리적 메커니즘
VU6028418 is a potent, highly selective and orally bioavailable M 4 mAChR antagonist with an IC 50 of 4.1 nM against hM 4.
Products are supplied to verified businesses, institutions, and qualified professionals for research and development use only. Not for use in humans, animals, diagnosis, or therapy.