SBI-553 | ß-Arrestin-biased NTSR1 modulator
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $90.00 | ||
| 25 mg | $320.00 |
SBI-553 (1849603-72-0) 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.
References/Citations:
- 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
- Slosky et al. (2020), ß-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors; Cell 181 1364
- Duan et al. (2023), GPCR activation and GRK2 assembly by a biased intracellular agonist; Nature 620 676
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
SBI-553 (1849603-72-0) 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.
References/Citations:
- 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
- Slosky et al. (2020), ß-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors; Cell 181 1364
- Duan et al. (2023), GPCR activation and GRK2 assembly by a biased intracellular agonist; Nature 620 676
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