| Identification | Back Directory | [Name]
VU0467485 | [CAS]
1451994-10-7 | [Synonyms]
VU0467485
AZ13713945
VU0467485,VU-0467485
Thieno[2,3-c]pyridazine-6-carboxamide, 5-amino-N-[(3-fluoro-4-methoxyphenyl)methyl]-3,4-dimethyl- | [Molecular Formula]
C17H17FN4O2S | [MOL File]
1451994-10-7.mol | [Molecular Weight]
360.41 |
| Chemical Properties | Back Directory | [density ]
1.367±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
12.26±0.46(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity[1]. | [in vivo]
VU0467485 (1-10 mg/kg; p.o.) has antipsychotic-like activity in an amphetamine-induced hyperlocomotion (AHL) rat model[1].
VU0467485 (3 mg/kg; p.o.) treatment displays that the Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM h and 4.2 hours, respectively[1]. | Animal Model: | Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model) [1] | | Dosage: | 1, 3, 10 mg/kg | | Administration: | Oral administration | | Result: | Dose-dependently reverses AHL. |
| Animal Model: | Male sprague Dawley rats[1] | | Dosage: | Oral administration (Pharmacokinetic Analysis) | | Administration: | 3 mg/kg | | Result: | The Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM?h and 4.2 hours, respectively. |
| [IC 50]
mAChR4 | [storage]
Store at -20°C | [References]
[1] Wood MR, et al. Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia. ACS Med Chem Lett. 2016 Dec 16;8(2):233-238. DOI:10.1021/acsmedchemlett.6b00461 |
|
|