(Ala11, D-Leu15)-Orexin B human RSGPPGLQGRAQRL-(D-Leu)-QASGNHAAGILTM-amide

Description

Orexin B is one of two closely related peptides; the orexins (also known as hypocretins). These small neuropeptides are secreted from orexin-containing neurons, located mainly in the lateral hypothalamus (LH). Orexins function via the binding and activation of two G-protein–coupled receptors (GPCRs); orexin receptor type 1 (OX1) and 2 (OX2).

[Ala(11), D-Leu(15)]orexin-B is a highly potent and selectiveOX2 receptor agonist which can discriminate between the OX1 and OX2 receptors, with a 400-fold selectivity for the OX2 over OX1. [Ala(11), D-Leu(15)]orexin-B is therefore a beneficial tool for addressing the functional roles of OX2.

The L-leucine residue at position 11 of orexin B is important for selectivity to OX2 over OX1. L-Alanine substitution at position 11 and D-leucine substitution at positions 15 maintain the potency of orexin-B to OX2, while significantly reducing the potency for OX1.

Orexins play several vital roles in a range of physiological activities, including: circadian rhythm; feeding behaviour; energy balance; glucose metabolism; neuroendocrine functions; stress-adaptive responses and reward and addiction. Orexins have also been linked to the pathological processes of neurological diseases such as: narcolepsy; depression; ischemic stroke; drug addiction and Alzheimer’s disease

Highly potent and selective OX2 receptor agonist

(Ala11, D-Leu15)-Orexin B human 0.5mg

$112.50
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(Ala11, D-Leu15)-Orexin B human 1mg

$150.00
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Catalogue number crb1000496
Sequence (one letter code) RSGPPGLQGRAQRL-(D-Leu)-QASGNHAAGILTM-amide
Sequence (three letter code) H-Arg-Ser-Gly-Pro-Pro-Gly-Leu-Gln-Gly-Arg-Ala-Gln-Arg-Leu-(D-Leu)-Gln-Ala-Ser-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2
Purity >95%
Storage -20°C
Molecular Weight 898.5
References

Asahi, S., Egashira, S., Matsuda, M., Iwaasa, H., Kanatani, A., Ohkubo, M., Ihara, M., Morishima, H. (2003). Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B. Bioorg Med Chem Lett, 13(1), 111-3. PMID: 12467628

Shahid, I., Rahman, A. and Pilowsky, P. (2012). Orexin A in rat rostral ventrolateral medulla is pressor, sympatho-excitatory, increases barosensitivity and attenuates the somato-sympathetic reflex. Br J Pharmacol, 165(7), 2292-2303. PMID: 21951179

Wang, C., Wang, Q., Ji, B., Pan, Y., Xu, C., Cheng, B., Bai, B. and Chen, J. (2018). The Orexin/Receptor System: Molecular Mechanism and Therapeutic Potential for Neurological Diseases. Front Mol Neurosci, 11. PMID: 30002617

Orexin B is one of two closely related peptides; the orexins (also known as hypocretins). These small neuropeptides are secreted from orexin-containing neurons, located mainly in the lateral hypothalamus (LH). Orexins function via the binding and activation of two G-protein–coupled receptors (GPCRs); orexin receptor type 1 (OX1) and 2 (OX2).


[Ala(11), D-Leu(15)]orexin-B is a highly potent and selectiveOX2 receptor agonist which can discriminate between the OX1 and OX2 receptors, with a 400-fold selectivity for the OX2 over OX1. [Ala(11), D-Leu(15)]orexin-B is therefore a beneficial tool for addressing the functional roles of OX2.


The L-leucine residue at position 11 of orexin B is important for selectivity to OX2 over OX1. L-Alanine substitution at position 11 and D-leucine substitution at positions 15 maintain the potency of orexin-B to OX2, while significantly reducing the potency for OX1.


Orexins play several vital roles in a range of physiological activities, including: circadian rhythm; feeding behaviour; energy balance; glucose metabolism; neuroendocrine functions; stress-adaptive responses and reward and addiction. Orexins have also been linked to the pathological processes of neurological diseases such as: narcolepsy; depression; ischemic stroke; drug addiction and Alzheimer’s disease