GRI977143 是特异性的LPA2受体的激动剂，其EC50值为3.3 μM。
| 生物活性 | GRI977143 is a specificLPA2receptoragonist, with anEC50of 3.3 μM[1]. |
| IC50& Target | LPA2Receptor 3.3 μM (EC50) |
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体外研究
(In Vitro) | GRI977143 (10 μM, 24-72 h) is effective in reducing activation of caspases 3, 7, 8, and 9 and inhibits poly(ADP-ribose)polymerase 1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis[1].
GRI977143 is an effective stimulator of extracellular signal-regulated kinase 1/2 activation and promotes the assembly of a macromolecular signaling complex consisting of LPA2, Na+-H+ exchange regulatory factor 2, and thyroid receptor interacting protein 6[1].
Cell Proliferation Assay[1] | Cell Line: | Vector- and LPA2-transduced MEF cells (2 × 104)[1]. | | Concentration: | 10 μM. | | Incubation Time: | 24-72 h. | | Result: | Did not cause a significant increase in vector cell proliferation except at 72 h (p< 0.05). |
Apoptosis Analysis[1]. | Cell Line: | Doxorubicin-induced apoptotic signaling in vector-transduced or LPA2-transduced MEF. | | Concentration: | 10 μM. | | Incubation Time: | 24 h. | | Result: | Reduced caspase 3 and 7 activation on LPA2-transduced MEF cells by 51 ± 3% and was approximately as potent as 3 μM LPA or OTP.
Protected against doxorubicin-induced apoptosis by inhibiting caspase 3, 7, 8, and 9 and reducing DNA fragmentation.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(127.73 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5547 mL | 12.7733 mL | 25.5467 mL | | 5 mM | 0.5109 mL | 2.5547 mL | 5.1093 mL | | 10 mM | 0.2555 mL | 1.2773 mL | 2.5547 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 (protect from light)。-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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