ML314 free base · Synonyms: ML-314 · ML 314

ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1.

For research use only. Not for human or veterinary use.

Target GPR35 Neurotensin Receptor

Research area Neurological Disease Endocrinology

Purity >98% Stock Inquire

Data Sheet SDS COA

ML314 structure

CAS No.: 1448895-09-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 460.00	BP-02452-25mg	In stock	Get quote
50 mg	USD 740.00	BP-02452-50mg	In stock	Get quote
100 mg	USD 1,180.00	BP-02452-100mg	In stock	Get quote
250 mg	USD 2,360.00	BP-02452-250mg	In stock	Get quote
500 mg	USD 3,770.00	BP-02452-500mg	In stock	Get quote
1 g	Inquire	BP-02452-1g	In stock	Inquire

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Description

ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .

Biological activity

In Vitro ML314 (10 μM) induces aggregation of β-arrestin in NTR1β-arrestin2/GFP containing U2OS cells. ML314 (10 μM, 10 min) antagonizes G protein signaling in HEK293 cells expressing NTR1. ML314 (2 μM) increases the number of NTR1 binding in U2OS cells. In Vivo ML314 (20 mg/kg, i.p., single dose) reduces locomotion in Dopamine Transporter knock-out mice. ML314 (10-30 mg/kg, i.p., single dose) reduces hyperlocomotion and conditioned place preference in C57BL/6J mice exposed to Methamphetamine.

Identifiers

SMILES: COC1=CC=CC=C1N2CCN(C3=C4C=C(OC)C(OC)=CC4=NC(C5CC5)=N3)CC2
InChIKey: SWEOAXMICIJCQC-UHFFFAOYSA-N

Specifications

MW (average): 420.5041
Formula: C₂₄H₂₈N₄O₃
CAS No.: 1448895-09-7
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[1].Hershberger P, et al. Small Molecule Agonists for the Neurotensin 1 Receptor (NTR1 Agonists). Probe Reports from the NIH Molecular Libraries Program

[2]. Barak, L. S., et al., (2016). ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse. ACS chemical biology, 11(7), 1880–1890.

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