[Ala11,D-Leu15]-Orexin B(human) TFA Chemical Structure
规格
是否有货
100 mg
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250 mg
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500 mg
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生物活性
[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM)[1].
[Ala11,D-Leu15]-Orexin B(human) Chemical Structure
CAS No. : 532932-99-3
规格
是否有货
100 mg
;
询价
;
250 mg
;
询价
;
500 mg
;
询价
;
* Please select Quantity before adding items.
生物活性
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM)[1].
Orexin A human, rat, mouse TFA 是一种 33 氨基酸兴奋性神经肽,参与多种中枢和外周过程。Orexin A human, rat, mouse TFA 是一种特异性、高亲和力的 G 蛋白偶联受体 OX1R 激动剂,在调节摄食行为中起重要作用。Orexin A human, rat, mouse TFA 是一种有效的抗伤害和抗痛觉过敏的药物。
Orexin A (human, rat, mouse) (TFA) Chemical Structure
规格
价格
是否有货
数量
10;mM;*;1 mL in Water
¥145535
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1 mg
¥4400
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5 mg
¥18000
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10 mg
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询价
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50 mg
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Orexin A (human, rat, mouse) (TFA) 相关产品
bull;相关化合物库:
Bioactive Compound Library Plus
Peptide Library
生物活性
Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats[1][2].
体外研究 (In Vitro)
Orexin A human, rat, mouse TFA has high affinity for OX1R, with 38 nM IC50 and 34 nM EC50 values in the the [Ca2﹢]i transient assay[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Orexin A human, rat, mouse TFA (3-30 mg/kg; i.v.; 5 min pre-test) significantly increases the latency to response at 10 and 30 mg/kg i.v. when given 5 min pre-test from 24.8±2.0 s in vehicle-treated mice to 35.0±3.7 s and 45.7±4.5 s, respectively[2]. Orexin A human, rat, mouse TFA (3, 10 and 30 mg/kg; i.v.) is given immediately before phenylp-quinone (PPQ) and increases the latency to the first PPQ-induced constriction from 357.4±35.2 s in vehicle-treated mice to 500.3±31.2 s at 10 mg/kg and 594.5±5.5 s at 30 mg/kg[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
[1]. Sakurai T, et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell. 1998 Feb 20;92(4):573-85.
[2]. Bingham S, et al. Orexin-A, an hypothalamic peptide with analgesic properties. Pain. 2001 May;92(1-2):81-90.
Orexin A human, rat, mouse 是一种 33 氨基酸兴奋性神经肽,参与多种中枢和外周过程。Orexin A human, rat, mouse 是一种特异性、高亲和力的 G 蛋白偶联受体 OX1R 激动剂,在调节摄食行为中起重要作用。Orexin A human, rat, mouse 是一种有效的抗伤害和抗痛觉过敏的药物。
Orexin A (human, rat, mouse) Chemical Structure
CAS No. : 205640-90-0
规格
价格
是否有货
1 mg
¥4400
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5 mg
¥18000
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Orexin A (human, rat, mouse) 的其他形式现货产品:
Orexin A (human, rat, mouse) (TFA)
生物活性
Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats[1][2].
体外研究 (In Vitro)
Orexin A human, rat, mouse has high affinity for OX1R, with 38 nM IC50 and 34 nM EC50 values in the the [Ca2﹢]i transient assay[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Orexin A human, rat, mouse (3-30 mg/kg; i.v.; 5 min pre-test) significantly increases the latency to response at 10 and 30 mg/kg i.v. when given 5 min pre-test from 24.8±2.0 s in vehicle-treated mice to 35.0±3.7 s and 45.7±4.5 s, respectively[2]. Orexin A human, rat, mouse (3, 10 and 30 mg/kg; i.v.) was given immediately before phenylp-quinone (PPQ) and increases the latency to the first PPQ-induced constriction from 357.4±35.2 s in vehicle-treated mice to 500.3±31.2 s at 10 mg/kg and 594.5±5.5 s at 30 mg/kg[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (<0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (<50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Sakurai T, et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell. 1998 Feb 20;92(4):573-85.
[2]. Bingham S, et al. Orexin-A, an hypothalamic peptide with analgesic properties. Pain. 2001 May;92(1-2):81-90.
Orexin B, human TFA;(Synonyms: Human orexin B TFA) 纯度: 98.08%
Orexin B, human (TFA) 是 Orexin 受体的内源性激动剂,与OX1和OX2结合的 Ki 值分别为 420 和 36 nM。
Orexin B, human TFA Chemical Structure
规格
价格
是否有货
数量
500 μg
¥2200
In-stock
1 mg
¥3400
In-stock
5 mg
¥13000
In-stock
10 mg
;
询价
;
50 mg
;
询价
;
* Please select Quantity before adding items.
生物活性
Orexin B, human (TFA) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
IC50 Target
Ki: 420 nM (OX1), 36 nM (OX2)[1].
体外研究 (In Vitro)
Orexin B is derived by proteolytic amino acid precursor, prepro-orexin, which is encoded by a gene localized to chromosome 17q21 in humans. In radioligand binding studies, Orexin B has a higher affinity for the OX2 receptor[1]. Human Orexin B has two amino acid substitutions when compared with the rodent sequence. OX2 receptor is indeed a high-affinity receptor for human orexin B, with an IC50 of 36 nM in the binding assay and an EC50 of 60 nM in the [Ca2+]i transient assay. Human Orexin B has significantly lower affinity for the human OX1: the calculated IC50 in the competitive binding assay and the EC50 in the [Ca2+]i transient assay are 420 nM and 2500 nM for human orexin-B, respectively[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Human Orexin B significantly augments food intake; at the 2 hr time point, 5- and 12-fold stimulation of food consumption is observed by 3 nM and 30 nM orexin-B, respectively[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Wistar rats (180-200 g)[2].
Dosage:
3 nM and 30 nM.
Administration:
Administered in a 5 mL bolus through a catheter placed in the left lateral ventricle in early light phase.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Smart D, et al. Orexins: a new family of neuropeptides. Br J Anaesth. 1999 Nov;83(5):695-7.
[2]. Sakurai T, et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell. 1998 Feb 20;92(4):573-85.
Orexin B, rat, mouse TFA;(Synonyms: Rat orexin B TFA; Orexin B (mouse) (TFA)) 纯度: 98.49%
Orexin B, rat, mouse (Rat orexin B) TFA 是一种内源性增食欲素受体 (Orexin receptor) 激动剂。Orexin B, rat, mouse TFA 结合并激活两个密切相关的孤儿 G 蛋白偶联受体 OX1-R 和 OX2-R。Orexin B, rat, mouse TFA 刺激食物摄入和能量消耗,并在睡眠-觉醒调节中发挥重要作用。
Orexin B, rat, mouse TFA Chemical Structure
规格
价格
是否有货
数量
1 mg
¥3000
In-stock
5 mg
¥7500
In-stock
10 mg
;
询价
;
50 mg
;
询价
;
* Please select Quantity before adding items.
生物活性
Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation[1][2][3].
体外研究 (In Vitro)
OX2 receptor is indeed a high-affinity receptor for human orexin B, with an IC50 of 36 nM in the binding assay and an EC50 of 60 nM in the [Ca2+]i transient assay. Human Orexin B has significantly lower affinity for the human OX1: the calculated IC50 in the competitive binding assay and the EC50 in the [Ca2+]i transient assay are 420 nM and 2500 nM for human orexin-B, respectively[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Orexin-B modulates the activity of rod bipolar cells (RBCs) located in the outer retina of rat. Intravitreal injection of orexin-B increased the amplitude of the scotopic electroretinographic b-wave, a reflection of RBC activity, recorded in vivo[4].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
3050.42
Formula
C₁₂₈H₂₁₆F₃N₄₅O₃₆S
Sequence Shortening
RPGPPGLQGRLQRLLQANGNHAAGILTM-NH2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Smart D, et al. Orexins: a new family of neuropeptides. Br J Anaesth. 1999 Nov;83(5):695-7.
[2]. Sakurai T, et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell. 1998 Feb 20;92(4):573-85.
[3]. Ziolkowska A, et al. Orexin B inhibits proliferation and stimulates specialized function of cultured rat calvarial osteoblast-like cells. Int J Mol Med. 2008;22(6):749-755.
[4]. Zhang G, et al. Orexin-B modulates synaptic transmission of rod bipolar cells in rat retina. Neuropharmacology. 2018;133:38-50.