343268-91-7
Chemical Structure
OXA(17-33)
Synonym(s): Orexin A (17-33) (human, mouse, rat, bovine)
- CAS No.: 343268-91-7
- Formula:C79H125N23O22
- Molecular Weight:1748.98
SMILES: OC(C=C1)=CC=C1C[C@H](N)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CC2=CN=CN2)C(NCC(N[C@@H](C)C(NCC(N[C@@H](CC(N)=O)C(N[C@H](C(N[C@@H](C)C(N[C@@H](C)C(NCC(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC(C)C)C(N[C@@H]([C@H](O)C)C(N[C@H](C(N)=O)CC(C)C)=O)=O)=O)=O)=O)=O)=O)CC3=CN=CN3)=O)=O)=O)=O)=O)=O)=O)=O)=O
Biological Activity: OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC50=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca2+ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy[1][2][3].
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OXA(17-33) | 97.48% | OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC50=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca2+ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy. | ||||||||||||||||||||
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- [1]. German NA, et al. Truncated Orexin Peptides: Structure-Activity Relationship Studies. ACS Med Chem Lett. 2013;4(12):1224-1227. [Content Brief]
- [2]. Barr J L, et al. Choline-Sigma-1R as an additional mechanism for potentiation of orexin by cocaine[J]. International Journal of Molecular Sciences, 2021, 22(10): 5160.
- [3]. Einsiedel J, et al. Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors. Bioorg Med Chem. 2022;61:116720. [Content Brief]
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