1. GPCR/G Protein Neuronal Signaling
  2. Neurotensin Receptor
  3. Fmoc-DL-Leu-OH

Fmoc-DL-Leu-OH acts as a partial agonist of the neurotensin NTS1 receptor (NTS1R) with an EC50 of 215.50 μM. Fmoc-DL-Leu-OH triggers intracellular calcium mobilization, and its activity is blocked by selective NTS1R antagonists. Fmoc-DL-Leu-OH can be used in the research of schizophrenia.

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Fmoc-DL-Leu-OH

Fmoc-DL-Leu-OH Chemical Structure

CAS No. : 126727-03-5

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Description

Fmoc-DL-Leu-OH acts as a partial agonist of the neurotensin NTS1 receptor (NTS1R) with an EC50 of 215.50 μM. Fmoc-DL-Leu-OH triggers intracellular calcium mobilization, and its activity is blocked by selective NTS1R antagonists. Fmoc-DL-Leu-OH can be used in the research of schizophrenia[1].

IC50 & Target[2]

NTR1

215.50 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO-K1 EC50
215.5 μM
Compound: 1
Agonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as increase in intracellular calcium level by FLIPR assay
Agonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as increase in intracellular calcium level by FLIPR assay
[PMID: 18849166]
CHO-K1 EC50
216 nM
Compound: 6
Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay
Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay
[PMID: 19195889]
CHO-K1 IC50
3.79 nM
Compound: 1
Antagonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium elevation pretreated 30 mins before with SR-48692 by FLIPR assay
Antagonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium elevation pretreated 30 mins before with SR-48692 by FLIPR assay
[PMID: 18849166]
In Vitro

Fmoc-DL-Leu-OH (Compound 1) acts as a partial agonist of human NTS1R expressed in CHOK1 cells, with an EC50 of 215.50 μM and a potency reaching 60% of the maximum potency of NT[1].
Fmoc-DL-Leu-OH (50 μM) exhibited agonist activity at human NTS1R expressed in CHOK1 cells, which was blocked by the selective NTS1R antagonist SR-48692 with an IC50 of 3.79 nM[1].
Fmoc-DL-Leu-OH (60 min) shows no detectable binding to human NTS1R in a [3H]neurotensin competitive binding assay performed using stably transfected CHOK1 cell membranes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

353.42

Formula

C21H23NO4

CAS No.
SMILES

O=C(OCC1C=2C=CC=CC2C=3C=CC=CC31)NC(C(=O)O)CC(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Fmoc-DL-Leu-OH
Cat. No.:
HY-W574030
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