[DArg10, Aib20] TLQP-21
[DArg10, Aib20] TLQP-21 is a functional antagonist of the complement 3a receptor (C3aR), with EC50 values of 854 nM, 1007 nM, and 1715 nM against human C3aR. [DArg10, Aib20] TLQP-21 recruits β-arrestin, activates Gi3, mediates β-arrestin-dependent receptor internalization, and does not induce calcium influx. [DArg10, Aib20] TLQP-21 inhibits the adrenergic‑induced lipolysis enhancement mediated by TLQP-21 (HY-P1345) and also inhibits the β-hexosaminidase secretion induced by C3a63-77. [DArg10, Aib20] TLQP-21 can be used in research related to asthma and inflammatory diseases.
For research use only. We do not sell to patients.
- Formula: C108H172N40O26
- Molecular Weight:2446.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Arrestin Isoforms
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Biological Activity
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C3aR 854-1715 nM (EC50) |
β-arrestin |
Gi3 |
β-hexosaminidase |
[DArg10, Aib20] TLQP-21 (1 mM) shows drastically improved stability in mouse plasma with a half-life of 253 minutes[1].
[DArg10, Aib20] TLQP-21 induces β-arrestin recruitment in HTLA cells expressing human C3aR1 with an EC50 of 854 nM and an Emax of 93.65% of basal levels[1].
[DArg10, Aib20] TLQP-21 activates Gi3 signaling in HEK293T cells expressing human C3aR1 with an EC50 of 1715 nM and an Emax of 62.6% of C3a63-77 activity[1].
[DArg10, Aib20] TLQP-21 promotes β-arrestin association with human C3aR1 in HEK293T cells with an EC50 of 1007 nM and an Emax of 71% of C3a63-77 activity[1].
[DArg10, Aib20] TLQP-21 does not induce calcium influx in 3T3-L1 cells, but acts as a functional antagonist with an IC50 of 1.7 μM for inhibiting TLQP-21-mediated calcium influx via a β-arrestin-dependent mechanism[1].
[DArg10, Aib20] TLQP-21 (1-100 μM) does not induce degranulation in LAD2 human mast cells at doses up to 100 μM, but dose-dependently inhibits C3a63-77- and compound 48/80-mediated degranulation[1].
[DArg10, Aib20] TLQP-21 (100 nM-10 μM; 1-3 hours) does not potentiate isoproterenol-induced lipolysis in 3T3-L1-derived adipocytes, but inhibits TLQP-21-mediated potentiation of this lipolytic response at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 2446.77
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Formula C108H172N40O26
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Sequence
Thr-Leu-Gln-Pro-Pro-Ala-Ser-Ser-Arg-{d-Arg}-Arg-His-Phe-His-His-Ala-Leu-Pro-Pro-Aib-Arg
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Sequence Shortening
TLQPPASSR-{d-Arg}-RHFHHALPP-{Aib}-R
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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
[1]. Rodriguez P, et al. A Novel Class of Complement 3a Receptor Agonists and Antagonists Derived from the TLQP-21 Peptide. Journal of medicinal chemistry. 2025 Sep 25;68(18):19107-19121. [Content Brief]
[2]. Wang L, et al. Cyclic Heptapeptide FZ1 Acts as an Integrin αvβ3 Agonist to Facilitate Diabetic Skin Wound Healing by Enhancing Angiogenesis. Journal of medicinal chemistry. 2025 Sep 25;68(18):19503-19520. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)