1417616-42-2

Name	VU0448088 (ML253)
CAS	1417616-42-2
Molecular Formula	C16H15ClN4OS
Molecular Weight	346.84
MOL File	1417616-42-2.mol

Synonyms

VU0448088 (ML253) Thieno[2,3-b]pyridine-2-carboxamide, 3-amino-5-chloro-4,6-dimethyl-N-(4-pyridinylmethyl)-

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Chemical Properties

Boiling point	612.4±55.0 °C(predicted)
density	1.402±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
form	Solid
pka	11.93±0.46(predicted)
color	White to off-white

Hazard Information

Uses

VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC50 values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic[1][2].

in vivo

VU0448088 (3, 10, 30, 56.6, 100 mg/kg; i.p.) reverses amphetamine-induced hyperlocomotion in a dose-dependent manner ^[1].

Animal Model:	Rat (amphetamine-induced hyperlocomotion)^[1]
Dosage:	3, 10, 30, 56.6, 100 mg/kg
Administration:	IP
Result:	Reversed amphetamine-induced hyperlocomotion in a dose-dependent manner, showed a modest reduction of 26% at a dose of 10 mg/kg; at the three highest doses (30, 56.6 and 100 mg/kg), showed significant reductions of 47.9%, 53.7% and 57.3%, respectively.

IC 50

mAChR4: 56 nM (EC₅₀)

References

[1] Le U, et al. Discovery of a selective M? positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorg Med Chem Lett. 2013 Jan 1;23(1):346-50. DOI:10.1016/j.bmcl.2012.10.073

Supplier

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone18149758185 18149758185

Websitehttp://www.caerulumpharma.com

Shanghai SuperLan Chemcial Technique Centre

Telephone0-2022843681 15618226720

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList19886/0_EN.htm

Guangzhou Younan Technology Co., Ltd

Telephone020-82000279 18988941452

Websitehttp://www.ubiochem.cn/

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone15000803246 18149758185

Websitehttp://www.caerulumpharma.com/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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