SBI-553, ß-Arrestin-biased NTSR1 modulator

Product Details

Formal Name: 2-[[2-(1-Fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl)quinazolin-6-yl]methylamino]ethanol

Molecular Formula: C₂₆H₃₁FN₄O₂

Formula Weight: 450.6

CAS Number: 1849603-72-0

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 12 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

ß-Arrestin-biased NTSR1 modulator

Functions

SBI-553 is a potent, brain penetrant, and orally bioavailable allosteric modulator of neurotensin receptor 1 (NTSR1; EC₅₀ = 340 nM)). It acts as a ß-Arrestin-biased agonist and selectively antagonizes G protein signaling conferring profound ß-Arrestin bias towards the endogenous ligand. SBI-553 displayed efficacy in mouse models of psychostimulant abuse without the characteristic undesirable side effects of unbiased NTSR1 agonism. This functionally selective modulation of NTSR1 may be a new therapeutic approach to treating psychostimulant abuse and other chemical and behavioral addictions.

Application Procedures

First dissolved in DMSO (12 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)