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Difelikefalin TFA is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin TFA is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively).
Difelikefalin TFA is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin TFA is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 13,900 | 8-10周 | |
50 mg | ¥ 18,300 | 8-10周 | |
100 mg | ¥ 23,500 | 8-10周 |
产品描述 | Difelikefalin TFA is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin TFA is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively). |
分子量 | 1021.92 |
分子式 | C42H56F9N7O12 |
CAS No. | 2742623-88-5 |
存储 | Shipping with blue ice. |
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