ML-314 is a brain penetrant nonpeptidic β-arrestin biased ggonist of the neurotensin NTR1 receptor, which exhibits full agonist behavior against NTR1 (EC50 = 2.0 μM) in the primary assay and selectivity against NTR2. The effect of ML314 is blocked by the NTR1 antagonist SR142948A in a dose-dependent manner. Unlike peptide-based NTR1 agonists, ML314 has no significant response in a Ca2+ mobilization assay and is thus a biased agonist that activates the β-arrestin pathway rather than the traditional Gq coupled pathway. This bias has distinct biochemical and functional consequences that may lead to physiological advantages. ML314 displays good brain penetration in rodents, and studies examining its in vivo properties are underway.

Product information

CAS Number: 1448895-09-7

Molecular Weight: 420.50

Formula: C24H28N4O3

Chemical Name: 2-cyclopropyl-6,7-dimethoxy-4-[4-(2-methoxyphenyl)piperazin-1-yl]quinazoline

Smiles: COC1=CC=CC=C1N1CCN(CC1)C1=NC(=NC2=CC(OC)=C(C=C21)OC)C1CC1

InChiKey: SWEOAXMICIJCQC-UHFFFAOYSA-N

InChi: InChI=1S/C24H28N4O3/c1-29-20-7-5-4-6-19(20)27-10-12-28(13-11-27)24-17-14-21(30-2)22(31-3)15-18(17)25-23(26-24)16-8-9-16/h4-7,14-16H,8-13H2,1-3H3

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: ≥360 days 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.