产品
编 号：F195684
分子式：C21H33NO4
分子量：363.49
分子式：C21H33NO4
分子量：363.49
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CAS No: 1628759-75-0
产品详情
生物活性：
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors. KMN-80 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体外研究：
KMN-80 is tested for binding of EP4 receptor and for activation of the rat EP2 and EP4 receptors, exhibits a Ki of 1.11 nM for rat EP4 receptor, EC50 values of 2.66 nM and 0.17 nM for rat EP4 receptor cAMP levels and rat EP4 receptor CREB activation, respectively.BMCs are isolated from young female rats are treated once at plating with varying doses of KMN-80 and ALP enzyme activity determined on day 9. KMN-80 (0-100 nM) shows ALP EC50 values significant different than those corresponding to PGE2 and PGE1, the EC50 values are 82.1 nM and 29.3 nM in activation of ALP enzyme activity in young female rat BMCs or old female or young male rat BMCs, respectively.KMN-80has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50?value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2?and TP, respectively.KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts?in vitro?(EC50s=20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4?agonist L-902,688 is highly cytotoxic at similar concentrations in these cells.KMN-80 binds to human EP receptor subtypes with Ki values of 880 nM and 2.349 nM for hEP3 and hEP4, respectively.
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors. KMN-80 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体外研究：
KMN-80 is tested for binding of EP4 receptor and for activation of the rat EP2 and EP4 receptors, exhibits a Ki of 1.11 nM for rat EP4 receptor, EC50 values of 2.66 nM and 0.17 nM for rat EP4 receptor cAMP levels and rat EP4 receptor CREB activation, respectively.BMCs are isolated from young female rats are treated once at plating with varying doses of KMN-80 and ALP enzyme activity determined on day 9. KMN-80 (0-100 nM) shows ALP EC50 values significant different than those corresponding to PGE2 and PGE1, the EC50 values are 82.1 nM and 29.3 nM in activation of ALP enzyme activity in young female rat BMCs or old female or young male rat BMCs, respectively.KMN-80has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50?value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2?and TP, respectively.KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts?in vitro?(EC50s=20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4?agonist L-902,688 is highly cytotoxic at similar concentrations in these cells.KMN-80 binds to human EP receptor subtypes with Ki values of 880 nM and 2.349 nM for hEP3 and hEP4, respectively.
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