GRI977143

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GRI977143 

GRI977143 是特异性的 LPA2 受体的激动剂,其EC50 值为3.3 μM。

GRI977143

GRI977143 Chemical Structure

CAS No. : 325850-81-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* 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].

IC50 & Target

LPA2 Receptor

3.3 μM (EC50)

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.

分子量

391.44

Formula

C22H17NO4S

CAS 号

325850-81-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

    [2]. Gyöngyi Nagyné Kiss, et al. PHARMACOLOGICAL AND CELLULAR CHARACTERIZATION OF GRI977143, A NOVEL NONLIPID LPA2 RECEPTOR AGONIST IDENTIFIED BY VIRTUAL SCREENING.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

GRI977143

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GRI977143 

GRI977143 是特异性的 LPA2 受体的激动剂,其EC50 值为3.3 μM。

GRI977143

GRI977143 Chemical Structure

CAS No. : 325850-81-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* 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].

IC50 & Target

LPA2 Receptor

3.3 μM (EC50)

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].

上海金畔生物科技有限公司 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.

分子量

391.44

Formula

C22H17NO4S

CAS 号

325850-81-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

    [2]. Gyöngyi Nagyné Kiss, et al. PHARMACOLOGICAL AND CELLULAR CHARACTERIZATION OF GRI977143, A NOVEL NONLIPID LPA2 RECEPTOR AGONIST IDENTIFIED BY VIRTUAL SCREENING.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

GRI977143

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GRI977143 

GRI977143 是特异性的 LPA2 受体的激动剂,其EC50 值为3.3 μM。

GRI977143

GRI977143 Chemical Structure

CAS No. : 325850-81-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* 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].

IC50 & Target

LPA2 Receptor

3.3 μM (EC50)

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.

分子量

391.44

Formula

C22H17NO4S

CAS 号

325850-81-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

    [2]. Gyöngyi Nagyné Kiss, et al. PHARMACOLOGICAL AND CELLULAR CHARACTERIZATION OF GRI977143, A NOVEL NONLIPID LPA2 RECEPTOR AGONIST IDENTIFIED BY VIRTUAL SCREENING.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务