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
-
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")
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
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
-
CAS No. 3081054-30-7
-
Molecular Weight 875.81
-
Formula C42H51BrN8O8
-
Sequence
Tyr-Cyclo({d-Lys}-{Phe(p-Br)}-Phe-Asp)-{d-Pro}-NH2
-
Sequence Shortening
Y-Cyclo({d-Lys}-{Phe(p-Br)}-FD)-{d-Pro}-NH2
-
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
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
Powered by Bioz