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Orexin B (human) Sale

(Synonyms: 食欲肽B(人),Human orexin B) 目录号 : GC14887

Orexin B (human)是一种由28个氨基酸残基组成的肽,对OX1和OX2受体具有亲和力,Ki值分别为420nM和 3nM。

Orexin B (human) Chemical Structure

Cas No.:205640-91-1

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500µg
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Sample solution is provided at 25 µL, 10mM.

Description

Orexin B (human), a 28-residue peptides, has affinity for the OX1 and OX2 receptor with Ki of 420 and 36nM, respectively[1].

Orexin B induces depolarization in both type 1 and type 2 neurons of the PVN with dose-dependent, and the changes in membrane potential are larger in type 2 neurons than in type 1[2]. Orexin B can inhibit the uptake of fAβ in BV2 cell line, reducing the levels of p-p38, p-Akt, and PI3K[3].

Orexin B was acutely administered into the lateral ventricle of male rats through preimplanted indwelling catheters, Orexin B significantly augmented food intake; at the 2h time point, observed 5-and 12-fold stimulation of food consumption by 3nmol and 30nmol Orexin B, respectively, as compared with vehicle controls[4]. Orexin B will be rapidly degraded in blood, so no 125I-Orexin B could be detected in intact form in brain when injected peripherally in male albino ICR mice at a dose of 6pmol/mouse through the isolated left jugular vein[5].

References:
[1] Smart D. Orexins: a new family of neuropeptides[J]. British journal of anaesthesia, 1999, 83(5): 695-697.
[2] Shirasaka T, Miyahara S, Kunitake T, et al. Orexin depolarizes rat hypothalamic paraventricular nucleus neurons[J]. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 2001, 281(4): R1114-R1118.
[3] An H, Cho M H, Kim D H, et al. Orexin impairs the phagocytosis and degradation of amyloid-β fibrils by microglial cells[J]. Journal of Alzheimer’s Disease, 2017, 58(1): 253-261.
[4] Sakurai T, Amemiya A, Ishii M, et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior[J]. Cell, 1998, 92(4): 573-585.
[5] Kastin A J, Akerstrom V. Orexin A but not orexin B rapidly enters brain from blood by simple diffusion[J]. The Journal of pharmacology and experimental therapeutics, 1999, 289(1): 219-223.

Orexin B (human)是一种由28个氨基酸残基组成的肽,对OX1和OX2受体具有亲和力,Ki值分别为420nM和 3nM[1]

Orexin B呈剂量依赖性地诱导室旁核(PVN)的1型和2型神经元发生去极化,并且2型神经元的膜电位变化大于1型神经元[2]。Orexin B能够抑制BV2细胞系对纤维状β淀粉样蛋白(fAβ)的摄取,降低p-p38、p-Akt和PI3K的水平[3]

Orexin B急性注入雄性大鼠的侧脑室能够显著增加食物摄入量;在注射后2h的时间点,与对照组相比,3nmol和30nmol的Orexin B分别使食物消耗量增加了5倍和12倍[4]。Orexin B在血液中会迅速降解,每只雄性白化ICR小鼠 6pmol的剂量进行外周注射时,在小鼠大脑中无法检测到完整形式的125I标记的Orexin B[5]

实验参考方法

Cell experiment [1]:

Cell lines

Microglial BV2 cells

Preparation Method

Microglial BV2 cells were seeded on 12 well plates. After the cells settled, they were treated with either fibrillary Aβ (fAβ) (1μM) and Orexin A (OXA); fAβ (1μM) and Orexin B (OXB); or fAβ only. Then they were cultured for 5min, 30min, 2h, or 24h. OXA and OXB were added 30min before fAß to assure it had enough time to be absorbed by the cells prior to treatment by fAβ. Both OXA and OXB were used to investigate differences between the Orexin receptors.

Reaction Conditions

1μM; 30min

Applications

Orexin A and Orexin B can suppresses the uptake of fAβ in BV2 microglial cells.

Animal experiment [2]:

Animal models

Male albino ICR mice

Preparation Method

The 125I-Orexin A or 125I-Orexin B was injected in a dose of 6pmol/mouse (2×106cpm) through the isolated left jugular vein along with 2μCi/mouse of 99mTc-albumin in 200μl of lactated Ringer’s solution containing 1% albumin. At 2, 3, 4, 5, 6, 8, 10, 20, and 30min after i.v. injection, blood was collected from a cut in the right carotid artery, and then the mouse was immediately decapitated. Serum and brain samples were obtained and counted in a dual channel γ-counter. The ratio of the radioactivity of brain tissue and serum was calculated, and multiple time-regression analysis was applied to determine the relationship between the ratios and exposure time.

Dosage form

6pmol/mouse; 30min; i.v.

Applications

No 125I-Orexin B could be detected in intact form in brain when injected peripherally in male albino ICR mice at a dose of 6pmol/mouse through the isolated left jugular vein, while most of the injected 125I-Orexin A reached the brain as intact peptide.

References:
[1]. An H, Cho M H, Kim D H, et al. Orexin impairs the phagocytosis and degradation of amyloid-? fibrils by microglial cells[J]. Journal of Alzheimer’s Disease, 2017, 58(1): 253-261.
[2]. Kastin A J, Akerstrom V. Orexin A but not orexin B rapidly enters brain from blood by simple diffusion[J]. The Journal of pharmacology and experimental therapeutics, 1999, 289(1): 219-223.

化学性质

Cas No. 205640-91-1 SDF
别名 食欲肽B(人),Human orexin B
化学名 (S,Z)-N'1-((5S,6Z,8S,9Z,11S,12Z,14S,15Z,18Z,20S,21Z,23S,24Z,26S,27Z,29S,30Z,33Z,35S,36Z,38S,39Z,41S,42Z,44S,45Z,47S,48Z,50S,51Z,53S,54Z,56S,57Z,59S,60Z)-26-((1H-imidazol-5-yl)methyl)-14-((S)-sec-butyl)-50,59-bis(3-guanidinopropyl)-7,10,13,16,19,22,25,28,3
Canonical SMILES CC[C@]([C@@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@
分子式 C123H212N44O35S 分子量 2899.36
溶解度 Soluble to 1 mg/ml in Water 储存条件 Desiccate at -20°C
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1 mM 0.3449 mL 1.7245 mL 3.449 mL
5 mM 0.069 mL 0.3449 mL 0.6898 mL
10 mM 0.0345 mL 0.1725 mL 0.3449 mL
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