For research use only. Not for therapeutic Use.
SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM[1][2].
SBI-553 (0.03-30 μM) induces β-blocking protein recruitment and NTSR1 internalization, but does not stimulate Gq protein activation, 1,4, 5-triphosphate (IP3) production or calcium mobilization[2].
SBI-553 (12 mg/kg intraperitoneally administered) alleviates cocaine-or methamphetamine-induced hyperactivity in wild-type mice[2].
| Catalog Number | I018108 |
| CAS Number | 1849603-72-0 |
| Synonyms | 2-[[2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl]-methylamino]ethanol |
| Molecular Formula | C26H31FN4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H31FN4O2/c1-30(15-16-32)19-7-8-22-21(17-19)24(29-25(28-22)26(27)11-12-26)31-13-9-18(10-14-31)20-5-3-4-6-23(20)33-2/h3-8,17-18,32H,9-16H2,1-2H3 |
| InChIKey | BLWXTJQMEBQCIZ-UHFFFAOYSA-N |
| SMILES | CN(CCO)C1=CC2=C(C=C1)N=C(N=C2N3CCC(CC3)C4=CC=CC=C4OC)C5(CC5)F |
| Reference | [1]. Pinkerton AB, et al. Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators. J Med Chem. 2019 Aug 20. [2]. Slosky LM, et al. β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors. Cell. 2020 Jun 11;181(6):1364-1379.e14. |
