ML352


Catalog No. Size PriceQuantity
M22839-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

The neurotransmitter acetylcholine (ACh) plays a critical role in autonomic function, motor control, attention, learning, and memory, and reward. The high-affinity choline transporter (CHT) is the ratelimiting determinant of ACh synthesis, yet the transporter remains a largely undeveloped target for the detection and manipulation of synaptic cholinergic signaling. ML352 is a novel, noncompetitive inhibitor of the presynaptic choline transporter. In vitro: At concentrations fully antagonized CHT in transfected cells and nerve terminal preparations, ML352 exhibited no inhibition of acetylcholinesterase or cholineacetyltransferase and also lacked activity at dopamine, serotonin, and norepinephrine transporters, as well as many receptors and ion channels. ML352 exhibited noncompetitive choline uptake inhibition in intact cells and reduced the apparent density of hemicholinium-3 binding sites in membrane assays, indicating allosteric transporter interactions . In vivo: DMPK studies revealed a high intravenous plasma clearance, a combination of the oral bioavailability and total brain concentrations indicate ML352 to be a suitable probe for studies of altered in vivo ACh signaling and behavioral effects in rodents . Clinical trial: Up to now, ML352 is still in the preclinical development stage.

Product information

CAS Number: 1649450-12-3

Molecular Weight: 387.47

Formula: C21H29N3O4

Chemical Name: (Z)-4-methoxy-3-[(1-methylpiperidin-4-yl)oxy]-N-{[3-(propan-2-yl)-1,2-oxazol-5-yl]methyl}benzene-1-carboximidic acid

Smiles: CC(C)C1C=C(C/N=C(\O)/C2C=CC(OC)=C(C=2)OC2CCN(C)CC2)ON=1

InChiKey: WBLVOWHFRUAMCP-UHFFFAOYSA-N

InChi: InChI=1S/C21H29N3O4/c1-14(2)18-12-17(28-23-18)13-22-21(25)15-5-6-19(26-4)20(11-15)27-16-7-9-24(3)10-8-16/h5-6,11-12,14,16H,7-10,13H2,1-4H3,(H,22,25)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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