L-798106 是强效且高度选择性的前列腺素类EP3受体拮抗剂 (Ki=0.3 nM)，它在 EP4，EP1 和 EP2 受体上也具有微摩尔活性，Ki值分别为 916 nM，>5000 nM 和 >5000 nM。
| 生物活性 | L-798106 is potent and highly selectiveprostanoidEP3receptorantagonist (Ki=0.3 nM), it also has micromolar activities at theEP4,EP1andEP2receptors withKivalues of 916 nM, >5000 nM and >5000 nM, respectively[1]. |
| IC50& Target | EP3 0.3 nM (IC50) | EP4 916 nM (IC50) | EP1 >5000 nM (IC50) | EP2 >5000 nM (IC50) |
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体外研究
(In Vitro) | L-798106 (200 nM) inhibits electrical field stimulation-induced contractile responses[2].
L-798106 (10 μM) inhibits electrical field stimulation-evoked ACh release[2].
Cell Viability Assay[2] | Cell Line: | Guinea-pig vas deferens | | Concentration: | 200 nM | | Incubation Time: | | | Result: | Showed an apparent pA2 of 7.48±0.25. |
Cell Viability Assay[2] | Cell Line: | Guinea-pig tracheal smooth muscle | | Concentration: | 10 μM | | Incubation Time: | | | Result: | Attenuated significantly the inhibitory effect of all agents tested (in % inhibition of EFS-induced release: 8-iso-PGE1 from 56.9 to 8.6; 8-iso-PGE2 from 51.6 to 9.2; PGE2 from 61.2 to 2.9; sulprostone from 55.9 to 18.8). |
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体内研究
(In Vivo) | L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation indb/dbmice[3].
| Animal Model: | Maledb/dbmice[3] | | Dosage: | 50 and 100 μg/kg | | Administration: | Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks | | Result: | Suppressed the increased fasting blood glucose levels in thedb/dbmice.
Suppressed increased proinflammatory gene expressions in the adipocytes isolated from the epididymal AT of thedb/dbmice. |
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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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 10 mg/mL(18.64 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.8641 mL | 9.3207 mL | 18.6414 mL | | 5 mM | 0.3728 mL | 1.8641 mL | 3.7283 mL | | 10 mM | 0.1864 mL | 0.9321 mL | 1.8641 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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