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- 2025年12月05日
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- 详细信息
- 询价记录
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
2380230-73-7
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1089.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥990.0 |
| 规格： | 10 mg | 产品价格： | ￥1680.0 |
| 规格： | 25 mg | 产品价格： | ￥3950.0 |
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NF-56-EJ40
CAS No. : 2380230-73-7
MCE 国际站：NF-56-EJ40
产品活性：NF-56-EJ40 是一种有效，高亲和力和高度选择性的人 SUCNR1 (GPR91) 拮抗剂，IC50 为 25 nM，Ki 为 33.5 nM，对大鼠 SUCNR1 几乎没有活性。 NF-56-EJ40 对人源化大鼠 SUCNR1 具有高亲和力，Ki 值为 17.4 nM。
研究领域：GPCR/G Protein
作用靶点：Succinate Receptor 1
In Vitro: NF-56-EJ40 is bound deep inside the hydrophobic pocket, with the acid group coordinated by the hydroxyl groups of the conserved residues Y832.64 and Y301.39 on one side, and R2817.39 on the other side. The conserved E181.27 is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E221.31 and N2747.32 in human SUCNR1 are replaced by K181.31 and K2697.32 in rat SUCNR1. These two amino acid exchanges could prevent the binding of NF-56-EJ40 to rat SUCNR1 owing to steric hindrance. Radioligand-binding studies with human SUCNR1 showed partial agreement with our homology model: the Y301.39F mutant of human SUCNR1, shows reduced binding of NF-56-EJ40. Similar effects are observed with the E181.27K and E181.27R mutants, probably owing to steric clashes of the Lys and Arg residues with NF-56-EJ40 and the loss of a hydrogen bond to its piperazine ring.
?Human SUCNR1 residues are introduced into rat SUCNR1 to form the double mutant K181.31E/K2697.32N (hereafter denoted humanized rat SUCNR1) (Ki of 17.4 nM and 33.5 nM for human and humanized rat SUCNR1, respectively). NF-56-EJ40 increases the thermal stability of both humanized rat SUCNR1 and human SUCNR1, but not that of rat SUCNR1.
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文献和实验30 4.18 3.59 3.25 3.03 2.87 2.75 2.65 2.57 2.51 2.41 2.31 2.19 2.07 1.94 1.79 30 31 4.16 3.57 3.23 3.01 2.85 2.73 2.63 2.56 2.49 2.40 2.29 2.18 2.06 1.92 1.77 31 32 4.15 3.56 3.22 2.99 2.84 2.71 2.62 2.54 2.48 2.38 2.27 2.16 2.04 1.90 1.75 32
27 40 48 73 51 92 26 16 90 82 66 59 83 62 64 11 12 67 19 00 71 74 60 47 21 29 68 02 02 37 03 31 27 11 27 94 75 06 06 09 19 74 66 02 94 37 34 02 76 70 90 30 86 38 45 94 30 38 28 35 24 10 16 20 33 32 51 26 38 79 78 45 04 91 16 92 53 56 16 02 75 50 95
2.79 2.77 2.76 2.73 2.72 2.71 9 10 2.75 2.74 2.72 2.71 2.70 2.68 2.66 2.65 2.64 2.62 2.60 2.59 2.56 2.55 0.54 10 11 2.63 2.61 2.59 2.58 2.57 2.55 2.53 2.52 2.51 2.49 2.47 2.46 2.43 2.42 2.40 11 12 2.52 2.51 2.49 2.48 2.47 2.44 2.43 2.41 2.40 2.38
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