1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. Valorphin

Valorphin 是一种内源性血红蛋白 β 链第 33-39 位氨基酸残基,具有阿片类药活性,可以与 mu-阿片 (mu-opioid) 受体结合,IC50 值为 14 nM;Valorphin 同时具有抗肿瘤活性,也可用于缓解疼痛的研究。

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Valorphin Chemical Structure

Valorphin Chemical Structure

CAS No. : 144313-54-2

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target

IC50: 14 nM (mu-opioid receptor), 200 nM (δ-opioid receptor)[1]

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Valorphin exhibits pronounced analgesic activity in mice, rats and rhesus monkeys via s.c, with ED50s of ≤5.2 mg/kg, but barely active after oral administration[1]. Valorphin (1 mg/kg) causes 42% of tumor growth inhibition in female BLRB mice bearing syngeneic mammary carcinoma cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

892.01

Formula

C44H61N9O11

CAS 号
Sequence

Val-Val-Tyr-Pro-Trp-Thr-Gln

Sequence Shortening

VVYPWTQ

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.

纯度 & 产品资料
参考文献
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
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  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Valorphin
目录号:
HY-P1599
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