| 名称 | KMN-80 |
| 描述 | The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has 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 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMF : 20 mg/mL (55.02 mM), Sonication is recommended.
Ethanol : 25 mg/mL (68.78 mM), Sonication is recommended.
Ethanol:PBS(pH 7.2) (1:1) : 0.5 mg/mL (1.38 mM), Sonication is recommended.
DMSO : 15 mg/mL (41.27 mM), Sonication is recommended.
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| 关键字 | KMN80 | KMN-80 | KMN 80 |
| 相关产品 | Evodiamine | Rutin | Lornoxicam | p-Hydroxycinnamic acid | Ethamsylate | Tranilast | Ufenamate | Angoroside C | Ozagrel | Amtolmetin guacil | Tetrahexyldecyl ascorbate | Pranoprofen |
