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144313-54-2

中文名稱 VAL-VAL-TYR-PRO-TRP-THR-GLN
英文名稱 VALORPHIN
CAS 144313-54-2
分子式 C44H61N9O11
分子量 892.01
MOL 文件 144313-54-2.mol
更新日期 2024/10/20 11:23:30
144313-54-2 結(jié)構(gòu)式 144313-54-2 結(jié)構(gòu)式

基本信息

中文別名
化合物VALORPHIN
英文別名
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-

物理化學(xué)性質(zhì)

沸點1364.0±65.0 °C(Predicted)
密度1.330±0.06 g/cm3(Predicted)
儲存條件-15°C
酸度系數(shù)(pKa)3.21±0.10(Predicted)

常見問題列表

生物活性
Valorphin 是一種內(nèi)源性血紅蛋白 β 鏈第 33-39 位氨基酸殘基,具有阿片類藥品鎮(zhèn)痛活性,可以與 mu-阿片 (mu-opioid) 受體結(jié)合,IC50 值為 14 nM;Valorphin 同時具有抗腫瘤活性。
靶點

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

體外研究

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.

體內(nèi)研究

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.

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