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Chemical Structure : SBI-553
CAS No.: 1849603-72-0
Catalog No.: PC-38142Not For Human Use, Lab Use Only.
SBI-553 (SBI553) is a potent, selective, β-arrestin-biased, brain penetrant neurotensin receptor 1 (NTR1, NTSR1) allosteric modulator with EC50 of 0.34 uM.
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| 5 mg | $278 | In stock | |
| 10 mg | $428 | In stock | |
| 25 mg | $728 | In stock | |
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SBI-553 (SBI553) is a potent, selective, β-arrestin-biased, brain penetrant neurotensin receptor 1 (NTR1, NTSR1) allosteric modulator with EC50 of 0.34 uM.
SBI-553 had no effect on the potency of NT in the NTR1 high-content (β-arrestin2-GFP) assay.
SBI-553 not only acts as a β-arrestin-biased agonist but also extends profound β-arrestin bias to the endogenous ligand by selectively antagonizing G protein signaling.
SBI-553 only showed moderate affinity against a range of related and unrelated GPCRs using the same high-content assay format (NTR2, GPR35, GPR55, K-opioid).
SBI-553 (12 mg/kg, i.p.) attenuated basal hyperlocomotion in dopamine transporter knockout (DAT−/−) mice.
SBI-553 showed efficacy in animal models of psychostimulant abuse, including cocaine self-administration, without the side effects characteristic of balanced NTSR1 agonism.
| M.Wt | 450.558 | |
| Formula | C26H31FN4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-((2-(1-Fluorocyclopropyl)-4-(4-(2-methoxyphenyl)piperidin-1-yl)quinazolin-6-yl)(methyl)amino)ethan-1-ol |
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1. Pinkerton AB, et al. J Med Chem. 2019 Sep 12;62(17):8357-8363.
2. Slosky LM, et al. Cell. 2020 Jun 11;181(6):1364-1379.e14.
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