SR-12062
SR-12062 is a Neurotensin receptor 1 (NTSR1) full agonist that modulates NTSR1 to trigger intracellular Ca2+ mobilization. SR-12062 can be used for the research of schizophrenia, parkinson’s disease, drug addiction.
For research use only. We do not sell to patients.
- CAS No.: 1623019-77-1
- Formula: C25H25N3O3
- Molecular Weight:415.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
NTR1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
2.05 μM
Compound: 8, SR-12062
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Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay
Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay
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[PMID: 24997685] |
In Vitro
SR-12062 (Compound 8) (2 μM) acts as a full agonist of NTSR1 with an EC50 of 2 μM and 99% efficacy relative to NT(8-13), and its activity is blocked by NTSR1 antagonist 5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1623019-77-1
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Molecular Weight 415.48
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Formula C25H25N3O3
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SMILES
CC(C)C[C@@H](C(O)=O)NC(CN1C2=CC=C(C3=CC4=C(C=CC=C4)N=C3)C=C2C=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
[1]. Di Fruscia P, et al. The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1). Bioorg Med Chem Lett. 2014;24(16):3974-3978. [Content Brief]
[2]. Pinkerton AB, et al. Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators. J Med Chem. 2019;62(17):8357-8363. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SR-12062 Related Classifications
HY-182551 Related Classifications
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