KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist ofEP₄receptorwith anIC₅₀and aK_iof 3 nM and 2.35 nM, respectively. KMN-80 is againstEP₃receptor with anIC₅₀of 1.4 μM and >10 μM for all other prostanoid receptors^[1].

KMN-80 is tested for binding of EP4 receptor and for activation of the rat EP2 and EP4 receptors, exhibits a K_iof 1.11 nM for rat EP4 receptor, EC₅₀values of 2.66 nM and 0.17 nM for rat EP4 receptor cAMP levels and rat EP4 receptor CREB activation, respectively^[1].
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 EC₅₀values significant different than those corresponding to PGE2 and PGE1, the EC₅₀values 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^[1].
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^[2].
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^[2].
KMN-80 binds to human EP receptor subtypes with K_ivalues of 880 nM and 2.349 nM for hEP₃and hEP₄, respectively^[2].

363.49

C₂₁H₃₃NO₄

1628759-75-0

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