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
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VU6028418
CAS number：2649803-05-2 molecular formula：C23H27F3N4O
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2649803-05-2 | molecular formula | C23H27F3N4O |
| molecular weight | 432.48 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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