货号	规格	价格	上海	北京	珠海	重庆	武汉
S87214-5mg促销	99.10%	￥1100.00 ￥880.00 S87214-5mg ￥880.00 现货	5 5	-	-	-	-
S87214-10mg促销	99.10%	￥1780.00 ￥1420.00 S87214-10mg ￥1420.00 现货	6 6	-	-	-	-
S87214-25mg促销	99.10%	￥2960.00 ￥2360.00 S87214-25mg ￥2360.00 现货	5 5	-	-	-	-
S87214-100mg	≥99%	￥4180.00 S87214-100mg ￥4180.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse

靶点：

Ki: 0.26 nM (native human bradykinin B1 receptor);BradykininReceptor

体外研究：

ELN-441958 is selective for primate over rodent B1 receptors with a rank order potency (KB, nanomolar) of human (0.12 ± 0.02) ~ rhesus monkey (0.24 ± 0.01) > rat (1.5 ± 0.4) > mouse (14 ± 4).
ELN-441958 has good permeability and metabolic stability.

体内研究：

ELN-441958 (1-10 mg/kg; s.c.; once) dose-dependently reduces carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model.
ELN-441958 (0-10 mg/kg; i.v. or p.o.) exhibits a favorable pharmacokinetic profile in the rat and rhesus monkey. Animal Model: Adult male and female rhesus monkeys Dosage: 1, 3, or 10 mg/kg Administration: Subcutaneous injection, 30 min before carrageenan injection Result: Increased the tail-withdrawal latencies in a dose-dependent manner. Animal Model: Rhesus monkeys or Sprague-Dawley rats Dosage: 2.5 or 10 mg/kg for rats, 1 mg/kg or 5 mg/kg for rhesus monkeysAdministration: Intravenous injection (2.5 mg/kg and 1 mg/kg) or oral administration (10 mg/kg and 5 mg/kg) (Pharmacokinetic Analysis) Result: In rats: When dosed intravenously, showed a moderate volume of distribution (2.7 L/kg, approximately four times total body water) and a moderate clearance (0.96 L/h/kg, approximately 24% of hepatic blood flow). The terminal plasma half-life of this compound in rats was 1.7 h. When dosed orally, the concentrations increased to a maximum of 1.2 g/mL at 2 h after dosing. The oral availability was 57%.In rhesus monkeys: When dosed intravenously, showed a moderate volume of distribution (2.7 L/kg) and a moderate clearance (0.49 L/h/kg, approximately 32% of hepatic blood flow). The terminal plasma half-life was 3.9 h. When dosed orally, the concentrations increased to a maximum of 3.6 g/mL at 3.3 h after dosing. The calculated oral bioavailability was greate

参考文献：

1. Hawkinson JE, 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):619-630.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.996 ml	9.98 ml	19.959 ml
5 mM	0.399 ml	1.996 ml	3.992 ml
10 mM	0.2 ml	0.998 ml	1.996 ml
50 mM	0.04 ml	0.2 ml	0.399 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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