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GRI977143 {[allProObj[0].p_purity_real_show]}

货号:A574284 Ambeed 开学季,买赠积分,赢豪礼

GRI977143是一种特异性 LPA2 受体激动剂,EC50 为 3.3 μM。

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GRI977143 化学结构 CAS号:325850-81-5
GRI977143 化学结构
CAS号:325850-81-5
GRI977143 3D分子结构
CAS号:325850-81-5
GRI977143 化学结构 CAS号:325850-81-5
GRI977143 3D分子结构 CAS号:325850-81-5
规格 价格 会员价 库存 数量
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GRI977143 纯度/质量文件 产品仅供科研

货号:A574284 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 Capase-7 Caspase Caspase-1 Caspase-10 Caspase-2 Caspase-3 Caspase-4 Caspase-5 Caspase-6 Caspase-8 Caspase-9 其他靶点 纯度
Emricasan {[allProObj[0].p_purity_real_show]}
Z-VAD(OMe)-FMK {[allProObj[0].p_purity_real_show]}
Z-VAD-FMK {[allProObj[0].p_purity_real_show]}
Q-VD-OPh {[allProObj[0].p_purity_real_show]}
VX-765 ++++

Caspase-1, Ki: 0.8 nM

++++

Caspase-4, Ki: <0.6 nM

{[allProObj[0].p_purity_real_show]}
Ac-DEVD-CHO +++

caspase-7, Ki: 1.6 nM

+++

Caspase-1, Ki: 18 nM

+++

caspase-10, Ki: 12 nM

+

caspase-2, Ki: 1.71 μM

++++

Caspase-3, Ki: 230 pM

++

Caspase-4, Ki: 132 nM

++

caspase-5, Ki: 205 nM

+++

caspase-6, Ki: 31 nM

++++

caspase-8, Ki: 0.92 nM

++

Caspase-9, Ki: 60 nM

{[allProObj[0].p_purity_real_show]}
Z-DEVD-FMK {[allProObj[0].p_purity_real_show]}
Z-IETD-FMK {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

GRI977143 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].

GRI977143 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.

GRI977143 实验方案

计算器
存储液制备 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

GRI977143 技术信息

CAS号325850-81-5
分子式C22H17NO4S
分子量 391.44
别名
运输蓝冰
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
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