VU0467485

Product Name: VU0467485
CAS No.: 1451994-10-7
Chemical Name: VU0467485
Synonyms: VU0467485;AZ13713945;VU0467485,VU-0467485;5-Amino-N-(3-fluoro-4-methoxybenzyl)-3,4-dimethylthieno[2,3-c]pyridazine-6-carboxamide;Thieno[2,3-c]pyridazine-6-carboxamide, 5-amino-N-[(3-fluoro-4-methoxyphenyl)methyl]-3,4-dimethyl-
CBNumber: CB05821343
Molecular Formula: C17H17FN4O2S
Formula Weight: 360.41
MOL File: 1451994-10-7.mol

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VU0467485 Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris

Product number: 6932
Product name: VU0467485
Purity: ≥98%(HPLC)
Packaging: 10
Price: $199
Updated: 2021/12/16

Tocris

Product number: 6932
Product name: VU0467485
Purity: ≥98%(HPLC)
Packaging: 50
Price: $839
Updated: 2021/12/16

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VU0467485 Chemical Properties,Usage,Production

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 C_max, AUC_o-inf and elimination t_1/2 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 C_max, AUC_o-inf and elimination t_1/2 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

VU0467485 Preparation Products And Raw materials

Raw materials

Preparation Products

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VU0467485 Suppliers

China 12 United States 3 Global 15

Tianjin Kailiqi Biotechnology Co., Ltd.

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TargetMol Chemicals Inc.

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Bide Pharmatech Ltd.

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Beijing Biocreative Technology Co., Ltd.

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TargetMol Chemicals Inc.

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Nantong QuanYi Biotechnology Co., Ltd

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Shanghai Yifei Biotechnology Co. , Ltd.

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Shanghai Fine Biotech Co.，Ltd

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VU0467485

Thieno[2,3-c]pyridazine-6-carboxamide, 5-amino-N-[(3-fluoro-4-methoxyphenyl)methyl]-3,4-dimethyl-

AZ13713945

VU0467485,VU-0467485

5-Amino-N-(3-fluoro-4-methoxybenzyl)-3,4-dimethylthieno[2,3-c]pyridazine-6-carboxamide

1451994-10-7