TECHNICAL SPECIFICATIONS
| Item | Specification |
|---|---|
| Product Name | [Tyr⁵,D-Trp⁶,⁸,⁹,Arg-NH₂¹⁰]-Neurokinin A (4-10) |
| CAS NO. | / |
| Appearance | White to off-white lyophilized powder |
| Molecular Formula | C57H68N14O10 |
| Molecular Weight | 1109.3/mol |
| Purity (RP-HPLC) | ≥98% |
| Solubility | Soluble in water (≥1 mg/mL), 0.1% TFA in aqueous solution, dilute acetic acid and DMSO |
| Endotoxin | ≤1.0 EU/mg |
| Biological Activity | Potent, selective and metabolically stable agonist for neurokinin-2 (NK2) receptors. |
| Storage Conditions | Store at ≤ -20°C in a dry, dark, sealed container. |
| Stock Location | Stock in USA |
| MOQ | 1g |
This multi-substituted analog is a potent agonist for tachykinin receptors, with high affinity for the Neurokinin 2 (NK2) receptor. The incorporation of three D-tryptophan residues provides remarkable resistance to proteolytic degradation, drastically prolonging its in vitro and in vivo half-life. The specific substitutions also optimize its interaction with the NK2 receptor binding pocket, leading to strong and sustained activation. Upon receptor binding, it stimulates the Gq protein pathway, activating phospholipase C (PLC), generating inositol trisphosphate (IP₃) and diacylglycerol (DAG), and ultimately causing a significant and prolonged increase in intracellular calcium that drives sustained smooth muscle contraction.
[Tyr⁵, D-Trp⁶,⁸,⁹, Arg-NH₂¹⁰]-NKA (4-10) is a sophisticated research tool, not a clinical drug. Its efficacy lies in its role as a proof-of-concept molecule that demonstrates how strategic peptide engineering (e.g., D-amino acid incorporation) can overcome key limitations like rapid degradation. Studies utilizing this and similar analogs provide critical insights for designing stable, potent peptide therapeutics.
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