Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2
Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 is a multi-opioid receptor (Opioid Receptor) modulator, acting as a MOR/KOR agonist and a DOR antagonist. Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 activates the G protein-mediated cAMP inhibitory pathway and β-arrestin2 recruitment pathway downstream of MOR, with an EC50 of 159 nM for β-arrestin2 recruitment, an EC50 of 1.1 nM for MOR-mediated calcium mobilization, and an EC50 of 397 nM for KOR. Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 exhibits potent analgesic activity in vivo. It can be used in studies related to opioid receptor function and analgesia.
For research use only. We do not sell to patients.
- CAS No.: 3081054-21-6
- Formula: C42H51FN8O8
- Molecular Weight:814.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
![Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 Chemical Structure](https://file.medchemexpress.com/product_pic/hy-p11895.gif "Click to View Tyr-c[D-Lys-p-F-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
IC50 & Target
[1]|
μ Opioid Receptor/MOR 1.1 nM (EC50) |
κ Opioid Receptor/KOR 397 nM (EC50) |
Arrestin-3/β-Arrestin 2 159 nM (EC50) |
In Vitro
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 (Analog 9) acts as a full agonist of human MOR in CHO-K1/MOR/Gα15 cells, with an EC50 of 1.1 nM[1].
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 acts as a partial agonist of human KOR in CHO-K1/KOR/Gα15 cells, with an EC50 of 397 nM[1].
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 (0.1-10 μM) acts as an antagonist of human DOR in CHO-K1/DOR/Gα15 cells[1].
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 (10 μM) acts as an agonist of human μ-opioid receptor (MOR) in HEK293T cells, and inhibits cAMP accumulation to a level comparable to that of 10 μM DAMGO[1].
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 induces β-arrestin2 recruitment of human μ-opioid receptor (MOR) in HEK293T cells with an EC50 of 159 nM, which is comparable to the potency of DAMGO (HY-P0210)[1].
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 exhibits greater enzymatic stability in mouse plasma, with a half-life of over 72 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | AUC0-∞ (Plasma) | AUC0-∞ (Brain) | Tmax |
|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 2021 ng/mL | 22312 min·ng/mL | 166.73 h·ng/g | 3 min |
In Vivo
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 (administered subcutaneously at 0.35 nmol/kg) exerts potent analgesic effects in a mouse model of acetic acid-induced visceral pain, with an ED50 of 0.35 nmol/kg[1].
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 (0.42 nmol/kg; p.o.) exerts potent oral analgesic effects in the mouse tail-flick acute pain model, with an ED50 of 0.42 nmol/kg[1].
Tyr-c[D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 (intracranial injection) exhibits supraspinal in vivo δ-opioid receptor antagonistic activity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tail-flick test in male Kunming mice (8-10 weeks old, 20-24 g); radiant heat stimulus applied 2-3 cm from the tail tip; baseline latency 3-5 s; cutoff time 10 s; 2-day habituation period[1]
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Dosage:0.18 and 0.42 nmol/kg (ED50)
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Administration:s.c. (0.18 nmol/kg); p.o. (0.42 nmol/kg)
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Result:Produced dose-dependent antinociception with an ED50 of 0.18 nmol/kg.
Lasted for 90 minutes at the highest tested dose.
Produced dose-dependent antinociception with an ED50 of 0.42 nmol/kg.
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Animal Model:Acetic acid-induced writhing test in male Kunming mice (8-10 weeks old, 20-24 g); 0.6% acetic acid (10 mL/kg) administered i.p.; writhing responses recorded from 5 to 15 min post-injection; 2-day habituation period[1]
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Dosage:0.35 nmol/kg (ED50)
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Administration:s.c.
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Result:Produced dose-dependent antinociception with an ED50 of 0.35 nmol/kg.
Chemical Information
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CAS No. 3081054-21-6
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Molecular Weight 814.90
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Formula C42H51FN8O8
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Sequence
Tyr-Cyclo({d-Lys}-{Phe(p-F)}-Phe-Asp)-{d-Pro}-NH2
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Sequence Shortening
Y-Cyclo({d-Lys}-{Phe(p-F)}-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-F-Phe-Phe-Asp]-D-Pro-NH2 Related Classifications
HY-P11895 Related Classifications
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