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KMN-80

CAS No. : 1628759-75-0

MCE 站：KMN-80

产品活性：KMN-80，PGE1 (HY-B0131) 的衍生物，是 EP₄ receptor 选择性强效激动剂，IC₅₀ 和 K_i 分别为 3 nM 和 2.35 nM。KMN-80 对EP₃ 的 IC₅₀ 值为 1.4 μM，对其他所有的前列腺素受体的 IC₅₀ 值 >10 μM。

研究领域：GPCR/G Protein

作用靶点：Prostaglandin Receptor

In Vitro: KMN-80 is tested for binding of EP4 receptor and for activation of the rat EP2 and EP4 receptors, exhibits a K_i 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 K_i values of 880 nM and 2.349 nM for hEP₃ and hEP₄, respectively.

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