A β-arrestin-biased positive allosteric modulator of NTSR1
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SBI-553

Item No. 36782

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)-1-piperidinyl]-6-quinazolinyl]methylamino]-ethanol
CAS Number
1849603-72-0
Molecular Formula
C26H31FN4O2
Formula Weight
450.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: Slightly solubleEthanol: Slightly soluble
SMILES
FC1(CC1)C2=NC3=C(C(N4CCC(CC4)C5=C(OC)C=CC=C5)=N2)C=C(N(CCO)C)C=C3
InChi Code
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
InChi Key
BLWXTJQMEBQCIZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $141

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    10 mg

    $248

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    25 mg

    $542

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    Product Description

    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.

    References & Product Citations
    Product Description References

    1. Slosky, L.M., Bai, Y., Toth, K., et al. β-Arrestin-biased allosteric modulator of NTSR1 selectively attenuates addictive behaviors. Cell 181(6), 1364-1379.e1314 (2020).