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ELN-441958

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Chemical Structure| 913064-47-8 同义名 : -
CAS号 : 913064-47-8
货号 : A306621
分子式 : C29H29ClN4O2
纯度 : 99%+
分子量 : 501.019
MDL号 : MFCD27665467
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: 105 mg/mL(209.57 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：
生物活性
描述 The bradykinin B1 receptor in tissues is significantly upregulated in response to inflammation and tissue injury. ELN-441958 is a bradykinin B1 receptor antagonist that potently and competitively inhibits the binding of the B1 agonist ligand [3H] DAKD to IMR-90 human fibroblast membranes with a Ki value of 0.26±0.02 nM. In IMR-90 cells expressing native bradykinin B1 receptor, ELN-441958 led to a dose-dependent antagonism of DAKD-induced calcium mobilization with a KB value of 0.12±0.02 nM. The rank order potency for ELN-441958 antagonism of bradykinin B1 receptors was human ~ rhesus (KB = 0.24±0.01 nM) > rat (KB = 1.5±0.4 nM) > mouse (KB = 14±4 nM). In MDR1 knockout mice, ELN-441958 achieved low micromolar brain levels five minutes after an i.v. administration of 2.5 mg/kg. ELN441958 at 2.5 mg/kg also showed a moderate volume of distribution (2.7 L/kg) and a moderate clearance (0.96 L/h/kg) in rats. A 30-min pretreatment with ELN441958 (10 mg/kg, s.c.) completely inhibited carrageenan-Induced hyperalgesia after 1–1.5 h post injection[2].
作用机制 ELN-441958 is a potent antagonist of bradykinin B1 receptor activation. It competitively inhibits the binding of the B1 agonist ligand to B1 receptor and antagonized agonist-induced calcium mobilization in native and recombinant cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

9.98mL

2.00mL

1.00mL

19.96mL

3.99mL

2.00mL
参考文献

[1]Hawkinson JE, Szoke BG, et al. Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958. J Pharmacol Exp Ther. 2007 Aug;322(2):619-30.

[2]Hawkinson JE, Szoke BG, Garofalo AW, et al. Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958. J Pharmacol Exp Ther. 2007;322(2):619‐630. doi:10.1124/jpet.107.120352