ELN-441958|cas:913064-47-8|西域试剂

ELN-441958,99.84%

产品编号：Bellancom-15043| CAS NO：913064-47-8| 分子式：C₂₉H₂₉ClN₄O₂| 分子量：501.02

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货号	价格	库存与货期
Bellancom-15043	￥3500.00	杭州北京（现货）
Bellancom-15043	￥5000.00	杭州北京（现货）
Bellancom-15043	￥15000.00	杭州北京（现货）

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ELN-441958

产品介绍

ELN-441958 是一种有效的、中性的、竞争性的和选择性的缓激肽 B₁ 受体 (bradykinin B₁ receptor) 拮抗剂，K_i 值为 0.26 nM。ELN-441958 具有较高的口服生物利用度，在小鼠中 CNS 透过性低。

生物活性

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

体外研究

ELN-441958 is selective for primate over rodent B₁ receptors with a rank order potency (K_B, 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 monkeys
Administration:	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 greater than 100%.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 monkeys
Administration:	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 greater than 100%.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (199.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9959 mL	9.9796 mL	19.9593 mL
5 mM	0.3992 mL	1.9959 mL	3.9919 mL
10 mM	0.1996 mL	0.9980 mL	1.9959 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.99 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.99 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.99 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。