VAL-VAL-TYR-PRO-TRP-THR-GLN
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- CAS号:
- 144313-54-2
- 英文名:
- VALORPHIN
- 英文别名:
- VALORPHIN;Valorphin TFAsalt;VAL-VAL-TYR-PRO-TRP-THR-GLN;H-VAL-VAL-TYR-PRO-TRP-THR-GLN-OH;Valorphin H-Val-Val-Tyr-Pro-Trp-Thr-Gln-OH;L-Glutamine, L-valyl-L-valyl-L-tyrosyl-L-prolyl-L-tryptophyl-L-threonyl-
- 中文名:
- VAL-VAL-TYR-PRO-TRP-THR-GLN
- 中文别名:
- 化合物VALORPHIN
- CBNumber:
- CB4472322
- 分子式:
- C44H61N9O11
- 分子量:
- 892.01
- MOL File:
- 144313-54-2.mol
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VAL-VAL-TYR-PRO-TRP-THR-GLN化学性质
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沸点:
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1364.0±65.0 °C(Predicted)
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密度:
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1.330±0.06 g/cm3(Predicted)
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储存条件:
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-15°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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3.21±0.10(Predicted)
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VAL-VAL-TYR-PRO-TRP-THR-GLN性质、用途与生产工艺
Valorphin 是一种内源性血红蛋白 β 链第 33-39 位氨基酸残基，具有阿片类药品镇痛活性，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。
IC50: 14 nM (mu-opioid receptor), 200 nM (δ-opioid receptor)
Valorphin is a derivative of dihydrovaltrate with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC
50
of 14 nM. Valorphin has low affinity for δ-opioid receptor (IC
50
, 200 nM) and shows no affinity for κ receptor (IC
50
, >10 μM). Valorphin (>10 μM) decreases spontaneous firing rate of cerebellar rat Purkinje cells. 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.
Valorphin exhibits pronounced analgesic activity in mice, rats and rhesus monkeys via s.c, with ED
50
s of ≤5.2 mg/kg, but barely active after oral administration. Valorphin (1 mg/kg) causes 42% of tumor growth inhibition in female BLRB mice bearing syngeneic mammary carcinoma cells.
VAL-VAL-TYR-PRO-TRP-THR-GLN
上下游产品信息
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VAL-VAL-TYR-PRO-TRP-THR-GLN
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144313-54-2, VAL-VAL-TYR-PRO-TRP-THR-GLN 相关搜索:
- 原料药
- C44H61N9O11
- 化合物VALORPHIN
- 144313-54-2
- Valorphin H-Val-Val-Tyr-Pro-Trp-Thr-Gln-OH
- L-Glutamine, L-valyl-L-valyl-L-tyrosyl-L-prolyl-L-tryptophyl-L-threonyl-
- Valorphin TFAsalt
- H-VAL-VAL-TYR-PRO-TRP-THR-GLN-OH
- VAL-VAL-TYR-PRO-TRP-THR-GLN
- VALORPHIN