CAS NO: | 2380230-73-7 |
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 |
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]. | ||||||||||||||||
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 |
| ||||||||||||||||
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
* 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。 |