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SBI-553

Supplier:
Catalogue number:
10-4449-02
Size:
25 mg
Product is available in:
  • USA
  • Canada
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ß-Arrestin-biased NTSR1 modulator / SBI-553 is a potent, brain penetrant, and orally bioavailable allosteric modulator of neurotensin receptor 1 (NTSR1; EC50 = 340 nM)).1 It acts as a ß-Arrestin-biased agonist and selectively antagonizes G protein signaling conferring profound ß-Arrestin bias towards the endogenous ligand.2,3 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.

Product Type:

Biochemicals & reagents

CAS Number:

1849603-72-0

Reference:

1) Pinkerton et al. (2019), Discovery of ß-Arrestin Biased, Orally Bioavailable and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators; J. Med. Chem. 62 8357 2) Slosky et al. (2020), ß-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors; Cell 181 1364 3) Duan et al. (2023), GPCR activation and GRK2 assembly by a biased intracellular agonist; Nature 620 676

Storage Temperature:

-20°C

Additional Information:

TARGET: GPCR -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Addiction