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GRI977143
GRI977143 是特异性的 LPA2 受体的激动剂，其EC50 值为3.3 μM。
GRI977143 Chemical Structure
CAS No. : 325850-81-5
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM [1].
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| IC50 & Target |
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LPA2 Receptor
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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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.
[2]. Gyöngyi Nagyné Kiss, et al. PHARMACOLOGICAL AND CELLULAR CHARACTERIZATION OF GRI977143, A NOVEL NONLIPID LPA2 RECEPTOR AGONIST IDENTIFIED BY VIRTUAL SCREENING.
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