Orexin A (human, rat, mouse) (Hypocretin-1 (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。
生物活性 | Orexin A (human, rat, mouse) (Hypocretin-1 (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 receptorOX1R. 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]. |
IC50& Target | |
体外研究 (In Vitro) | Orexin A (human, rat, mouse) has high affinity for OX1R, with 38 nM IC50and 34 nM EC50values in the the [Ca2﹢]i transient assay[1].
|
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].
Animal Model: | Female mice (mouse carrageenan-induced thermal hyperalgesia test)[2] | Dosage: | 3, 10 and 30 mg/kg | Administration: | i.v.; 5 min pre-test | Result: | Significantly increased the latency to response at 10 and 30 mg/kg. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
Sequence Shortening | {Glp}-PLPDCCRQKTCSCRLYELLHGAGNHAAGILTL-NH2 (Disulfide bridge: Cys6-Cys12, Cys7-Cys14) |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 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. |
|