KI-7 是一种A2B腺苷受体阳性变构调节剂。KI-7 增强非选择性 A2B 腺苷受体激动剂 NECA 诱导的 cAMP 积累 (EC50=445.8 nM)。KI-7 还增强了选择性 A2B 腺苷受体激动剂 BAY 60-6583 和 adenosine 诱导的 cAMP 积累,EC50分别为 2390 nM 和 2550 nM。
生物活性 | KI-7 is anA2Badenosine receptorpositive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2Badenosine receptoragonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2Badenosine receptoragonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively[1][2]. |
体外研究 (In Vitro) | KI-7 (1 μM; 5-21 days; mesenchymal stem cells) induces a significant increase in mRNA expression of Runx2 and Osterix[1]. KI-7 (1 μM; 15-21 days) induced a significant increase in cell viability in both differentiation stages[1]. KI-7, as A2B adenosine receptor positive allosteric modulator in MSCs, demonstrating it is able to potentiate the effects of either adenosine and synthetic orthosteric A2B adenosine receptor agonists in mediating osteoblast differentiation in vitro. NECA, BAY 60-6583 and KI-7 induce a strong increase in IL-6 production. KI-7 is able to potentiate the effects of orthosteric agonists in both differentiation stages, even if the effect became significant only at 21 days[1].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(705.42 mM;Need ultrasonic) 配制储备液 1 mM | 2.8217 mL | 14.1084 mL | 28.2167 mL | 5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL | 10 mM | 0.2822 mL | 1.4108 mL | 2.8217 mL |
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