Valorphin
Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
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- CAS 番号: 144313-54-2
- 分子式: C44H61N9O11
- 分子量:892.01
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Opioid Receptor アイソフォーム固有の製品をすべて表示
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生物活性
IC50: 14 nM (mu-opioid receptor), 200 nM (δ-opioid receptor)[1]
Valorphin is a derivative of dihydrovaltrate with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM. Valorphin has low affinity for δ-opioid receptor (IC50, 200 nM) and shows no affinity for κ receptor (IC50, >10 μM). Valorphin (>10 μM) decreases spontaneous firing rate of cerebellar rat Purkinje cells[1]. Valorphin (1 μM) treatment 48 h prior to 0.1 μM epirubicin, or 0.1 μM vincristine, or 0.05 μM vincristine, causes 100% tumor cell death[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 144313-54-2
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分子量 892.01
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分子式 C44H61N9O11
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SMILES
O=C(N[C@@H](C(C)C)C(N[C@@H](CC1=CC=C(C=C1)O)C(N2[C@@H](CCC2)C(N[C@@H](CC3=CNC4=CC=CC=C34)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCC(N)=O)C(O)=O)=O)=O)=O)=O)=O)[C@H](C(C)C)N
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配列
Val-Val-Tyr-Pro-Trp-Thr-Gln
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シーケンスの短縮
VVYPWTQ
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
In all series, the cells are incubated for 48 hours beginning with the hour 0. All substances are dissolved in FBS-supplied RPMI-1640 medium. Negative control cells are incubated in the absence of test substances. The reference samples are incubated with epirubicin or Valorphin in the concentrations equivalent to those applied in the experimental seria and for the corresponding time intervals. The effect is evaluated by staining with MTT dye[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
In the basic experiment, 49 mice are randomized in 4 groups: two groups (12 animals each) corresponding to the negative control, the reference group (13 animals) and the experimental group (12 animals). The control and the reference group are treated as in preliminary experiment, the experimental group are injected with the mixture of Valorphin (1 mg/kg) and epirubicin (25 mg/m2), dissolved in 0.9% NaCl solution in distilled water. Three injections (volume 0.2 mL) are made with 6-day intervals. Since no reliable difference in tumor size or lifespan of animals in the two negative control groups are observed, the data obtained in these groups are pooled. At day 20 after the first injection, the size of the tumors are determined. Tumor volumes are calculated, inhibition of tumor growth is determined. Percentages of survival are determined for 1-26 days of treatment. The observation is quitted after the total death of the animals in the negative control group[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
[1]. Maurer R, et al. Valorphin: a novel chemical structure with opioid activity. Neuropeptides. 1985 Feb;5(4-6):387-90. [Content Brief]
[2]. Blishchenko EY, et al. Antitumor effect of valorphin in vitro and in vivo: combined action with cytostatic drugs. Cancer Biol Ther. 2005 Jan;4(1):118-24. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)