1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide

Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide is a μ/δ opioid receptor ligand with high μ opioid receptor selectivity and agonist activity. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide has an IC50 of 237 nM for μ receptors and 1050 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide shows Ki values of 17 nM for μ receptors and 480 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide inhibits electrically evoked contractions of guinea pig ileum and mouse vas deferens. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide serves as a starting compound for structure-activity relationship investigations of μ receptor recognition.

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Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide

Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide Chemical Structure

CAS No. : 72732-17-3

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Description

Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide is a μ/δ opioid receptor ligand with high μ opioid receptor selectivity and agonist activity. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide has an IC50 of 237 nM for μ receptors and 1050 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide shows Ki values of 17 nM for μ receptors and 480 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide inhibits electrically evoked contractions of guinea pig ileum and mouse vas deferens. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide serves as a starting compound for structure-activity relationship investigations of μ receptor recognition[1].

IC50 & Target[1]

μ Opioid Receptor/MOR

237 nM (IC50)

δ Opioid Receptor/DOR

1050 nM (IC50)

μ Opioid Receptor/MOR

17 nM (Ki)

δ Opioid Receptor/DOR

480 nM (Ki)

In Vitro

Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide (TRIMU 4) inhibits electrically evoked contractions of guinea pig ileum with an IC50 of 237 nM, indicating activity at μ opioid receptors[1].
Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide inhibits electrically evoked contractions of mouse vas deferens with an IC50 of 1050 nM, with a 4.35-fold preference for μ over δ opioid receptors[1].
Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide (40 min) inhibits binding of the μ-selective ligand [3H]DAGO to rat brain membrane μ opioid receptors with a Ki of 17.0 nM[1].
Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide (40 min) inhibits binding of the δ-selective ligand [3H]DSLET to rat brain membrane δ opioid receptors with a Ki of 480 nM, with a 28-fold preference for μ over δ opioid receptors[1].

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

Molecular Weight

392.49

Formula

C20H32N4O4

CAS No.
SMILES

CC(C)CC(C)NC(CNC([C@@H](C)NC([C@@H](N)CC1=CC=C(C=C1)O)=O)=O)=O

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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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Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide Related Classifications

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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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Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide
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