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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-Ki16425
Ki16425

Chemical Structure : Ki16425

CAS No.: 355025-24-0

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Ki16425 (Debio 0719, Ki 16425)

货号: PC-43463Not For Human Use, Lab Use Only.

Ki16425 (Debio 0719) is a potent, subtype-selective, competitive antagonist of lysophosphatidic acid receptor LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, shows no activity at LPA4, LPA5, LPA6.

规格 价格 库存 数量
5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Ki16425 (Debio 0719) is a potent, subtype-selective, competitive antagonist of lysophosphatidic acid receptor LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, shows no activity at LPA4, LPA5, LPA6.
Ki16425 inhibits the LPA-induced response in the decreasing order of LPA1>LPA3>LPA2, inhibits LPA-induced guanosine 5'-O-(3-thio)triphosphate binding as well as LPA receptor binding to membrane fractions in intact cells.
Ki16425 also inhibits LPA-induced long-term responses, including DNA synthesis and cell migration in A431 cells, selectively inhibits LPA receptor-mediated actions, especially through LPA1 and LPA3.
Ki16425 reduces both ethanol-induced sedation and ethanol reward in mice, prevents the effects of ethanol on basal c-Fos expression in the medial prefrontal cortex and on adult neurogenesis in the hippocampus.

物理化学性质&存储条件

分子量 474.96
分子式 C23H23ClN2O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Propanoic acid, 3-[[[4-[4-[[[1-(2-chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]phenyl]methyl]thio]-

参考文献

1. Ohta H, et al. Mol Pharmacol. 2003 Oct;64(4):994-1005.

2. Yamada T, et al. J Biol Chem. 2004 Feb 20;279(8):6595-605.

3. Zhao J, et al. Transl Res. 2015 Jul;166(1):80-8.

4. Sánchez-Marín L, et al. Neuropharmacology. 2018 May 1;133:189-201.

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