Contulakin G 是一种 O-糖基化无脊椎动物神经紧张素。Contulakin-G 是一种较弱的神经紧张素受体 (neurotensin receptor) 激动剂。Contulakin G 还是一种有效的镇痛剂。
| 生物活性 | Contulakin G is an O-glycosylated invertebrate neurotensin. Contulakin-G is a weaker agonist for theneurotensin receptor. Contulakin G is also a potent antinociceptive agent[1][2]. |
体内研究
(In Vivo) | Contulakin G exhibits potent analgesic activity in three pain models in rats following intrathecal delivery, namely in tail-flick (acute pain), formalin test, and CFA-induced allodynia inflammatory pain[1].
Contulakin G (0-3 nmoL, Intrathecally) significantly decreases flinching behavior in rats[2].
Contulakin G (50-500 nmoL, Intrathecally) produces a dose-dependent increase in the thermally evoked skin twitch latency by 30 min after administration in dogs[2].
| Animal Model: | Male Holtzman rats (300-375 g)[2] | | Dosage: | 0.03, 0.1, 0.3, and 3 nmol | | Administration: | Intrathecally, administered as a 10-μL bolus followed by a 10-μL saline flush | | Result: | Produced a significant decrease in flinching in all phases of the formalin test in rats. |
| Animal Model: | Purpose-bred beagle dogs (9-12 kg)[2] | | Dosage: | 50, 150, or 500 nmol | | Administration: | Intrathecally | | Result: | Produced a dose-dependent increase in the thermally evoked skin twitch latency at 30 min after dosing in dogs, which reached statistical difference as compared to vehicle at 500 nmol. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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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