SBI-553

SBI-553 is a β-arrestin-biased positive allosteric modulator (PAM) of neurotensin receptor 1 (NTSR1).1 It binds to NSTR1 and increases neurotensin-1 affinity for NSTR1 in HEK293 cells expressing the human receptor when used at concentrations ranging from 0.01 to 10 µM. SBI-553 (0.03-30 µM) induces β-arrestin recruitment and NTSR1 internalization without stimulating Gq protein activation, 1,4,5-triphosphate (IP3) generation, or calcium mobilization in cell-based assays. In vivo, SBI-553 (12 mg/kg, i.p.) attenuates cocaine- or methamphetamine-induced hyperlocomotion in wild-type but not β-arrestin-2 knockout mice. It also reduces cocaine self-administration in mice.WARNING This product is not for human or veterinary use.

A β-arrestin-biased positive allosteric modulator of NTSR1

450.6

≥98%

Biochemicals/Receptor Pharmacology/Allosteric Modulators

Formal_Name:2-[[2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)-1-piperidinyl]-6-quinazolinyl]methylamino]-ethanol

FC1(CC1)C2=NC3=C(C(N4CCC(CC4)C5=C(OC)C=CC=C5)=N2)C=C(N(CCO)C)C=C3

C26H31FN4O2

1849603-72-0

≥ 4 years

DMF: 3 mg/ml DMSO: Slightly soluble Ethanol: Slightly soluble