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GRI977143

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Chemical Structure| 325850-81-5 同义名 : -
CAS号 : 325850-81-5
货号 : A574284
分子式 : C22H17NO4S
纯度 : 95%
分子量 : 391.44
MDL号 : -
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(127.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 GRI977143, a targeted LPA2 receptor agonist, has an EC50 of 3.3 μM. At a concentration of 10 μM over 24-72 hours, GRI977143 effectively diminishes the activation of caspases 3, 7, 8, and 9, and prevents cleavage of PARP1 and DNA fragmentation in various models of apoptosis. It also acts as a potent enhancer of extracellular signal-regulated kinase 1/2 activation and facilitates the formation of a large signaling complex that includes LPA2, Na+-H+ exchange regulatory factor 2, and thyroid receptor interacting protein 6. At 10 μM, GRI977143 does not significantly increase vector cell proliferation until 72 hours. In MEF cells subjected to doxorubicin-induced apoptotic signaling, either vector-transduced or LPA2-transduced, a 10 μM concentration of GRI977143 reduces the activation of caspase 3 and 7 by 51 ± 3% and is nearly as effective as 3 μM LPA or OTP in protecting against doxorubicin-induced apoptosis by inhibiting caspases 3, 7, 8, and 9 and lessening DNA fragmentation[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.26mL

12.77mL

2.55mL

1.28mL

25.55mL

5.11mL

2.55mL
参考文献

[1]Gyöngyi N. Kiss, et al. Virtual Screening for LPA2-Specific Agonists Identifies a Nonlipid Compound with Antiapoptotic Actions. Mol Pharmacol. 2012 Dec; 82(6): 1162–1173.