Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2
Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 is a MOR-selective antagonist with a pA2 value of 9.9. Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 blocks G protein- and β-arrestin2-mediated downstream signaling pathways of MOR. Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 significantly delays the development of μ-opioid agonist-induced analgesic tolerance by blocking peripheral MOR. Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 is applicable to studies related to opioid receptor function and analgesic tolerance.
For research use only. We do not sell to patients.
- CAS No.: 3081054-30-7
- Formula: C42H51BrN8O8
- Molecular Weight:875.81
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
![Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 Chemical Structure](https://file.medchemexpress.com/product_pic/hy-p11896.gif "Click to View Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 Chemical Structure")
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 (Compound 11) exhibits no agonist activity against human MOR, KOR, and DOR in CHO-K1/Gα15 cells[1].
Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 (0.1-10 μM) is a potent and selective MOR antagonist in CHO-K1/Gα15 cells, with no significant KOR or DOR antagonistic activity at the tested concentrations[1].
Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 (0.01-1 μM) acts as a MOR antagonist in HEK293T cells and blocks the G protein-mediated cAMP inhibition downstream of MOR activation[1].
Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 (0.01-1 μM) blocks the β-arrestin2-mediated downstream signaling pathway activated by MOR in HEK293T cells[1].
Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 (72 h) exhibits greater enzymatic stability in mouse plasma, with a half-life exceeding 72 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3081054-30-7
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Molecular Weight 875.81
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Formula C42H51BrN8O8
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Sequence
Tyr-Cyclo({d-Lys}-{Phe(p-Br)}-Phe-Asp)-{d-Pro}-NH2
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Sequence Shortening
Y-Cyclo({d-Lys}-{Phe(p-Br)}-FD)-{d-Pro}-NH2
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 Related Classifications
HY-P11896 Related Classifications
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