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NF-56-EJ40
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NF-56-EJ40图片
CAS NO:2380230-73-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
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。
生物活性

NF-56-EJ40 is a potent, high-affinity, and highly selectivehuman SUCNR1 (GPR91)antagonist with anIC50of 25 nM and aKiof 33 nM, and shows almost no activity towards ratSUCNR1. NF-56-EJ40 has high affinity forhumanized rat SUCNR1with aKivalue of 17.4 nM[1].

IC50& Target

SUCNR1 (GPR91)[1]

体外研究
(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 Y832.64and Y301.39on one side, and R2817.39on the other side. The conserved E181.27is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E221.31and N2747.32in human SUCNR1 are replaced by K181.31 and K2697.32in 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[1].
Human SUCNR1 residues are introduced into rat SUCNR1 to form the double mutant K181.31E/K2697.32N (hereafter denoted humanized rat SUCNR1) (Kiof 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[1].

分子量

443.54

性状

Solid

Formula

C27H29N3O3

CAS 号

2380230-73-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL(11.27 mM;Need ultrasonic)

H2O : 4.55 mg/mL(10.26 mM;ultrasonic and adjust pH to 9 with NaOH)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2546 mL11.2729 mL22.5459 mL
5 mM0.4509 mL2.2546 mL4.5092 mL
10 mM0.2255 mL1.1273 mL2.2546 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。