Valorphin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Valorphin 具有阿片类镇痛活性，与大鼠 mu-阿片受体结合，IC50 为 14 nM。

Valorphin has opioid analgesic activity binds to rat mu-opioid receptor with an IC50 of 14 nM.

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. 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 ED50s 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.

Valorphin TFAsalt

Endocrinology/Hormones

Opioid Receptor

Opioid Receptor

——

——

144313-54-2

893

C44H60N8O12

>98% (HPLC)

——

CC(C)[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(O)=O

——

(-20℃)

With Ice Pack

≥ 2 years