生物活性 | Orexin B, human (TFA) is an endogenous agonist atOrexinreceptor withKis 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 IC50of 36 nM in the binding assay and an EC50of 60 nM in the [Ca2+]i transient assay. Human Orexin B has significantly lower affinity for the human OX1: the calculated IC50in the competitive binding assay and the EC50in the [Ca2+]i transient assay are 420 nM and 2500 nM for human orexin-B, respectively[2].
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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].
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. | Result: | Significantly augmented food intake. |
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分子量 | |
性状 | |
Formula | |
Sequence | Arg-Ser-Gly-Pro-Pro-Gly-Leu-Gln-Gly-Arg-Leu-Gln-Arg-Leu-Leu-Gln-Ala-Ser-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2 |
Sequence Shortening | RSGPPGLQGRLQRLLQASGNHAAGILTM-NH2 |
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. |
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