Navacaprant BTRX-335140; CYM-53093|cas:2244614-14-8|西域试剂

Navacaprant BTRX-335140; CYM-53093,99.71%

产品编号：Bellancom-124754| CAS NO：2244614-14-8| 分子式：C₂₅H₃₂FN₅O₂| 分子量：453.55

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货号	价格	库存与货期
Bellancom-124754	￥3500.00	杭州北京（现货）
Bellancom-124754	￥6000.00	杭州北京（现货）
Bellancom-124754	￥20000.00	杭州北京（现货）

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Navacaprant BTRX-335140; CYM-53093

产品介绍

Navacaprant (BTRX-335140) 是一种选择性的，具有口服活性的 κ opioid receptor (KOR) 拮抗剂，对 κOR，μOR 和 δOR 具有拮抗活性，IC₅₀ 值分别为 0.8 nM，110 nM 和 6500 nM。Navacaprant 在大鼠中具有良好的体外 ADMET 和体内药代动力学特征。Navacaprant 可以很好地分布到 CNS 中，可用于神经病变类的研究。

生物活性

Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC₅₀ values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.

体外研究

Navacaprant (BTRX-335140) (0-10 μM; 4 h) shows selective antagonist activity towards Kappa Opioid Receptor.

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

Cell Viability Assay

Cell Line:	OPRK1-BLA U2OS cells
Concentration:	0-10 μM
Incubation Time:	4 hours
Result:	Exibited antagonist activity to KOR, DOR and MOR with IC₅₀ values of 0.8, 110 and 6500 nM respectively, and showed selective antagonist activity to KOR.

体内研究
(In Vivo)

Navacaprant (BTRX-335140) (0.01-3 mg/kg; p.o. once) reduces U69,593- stimulated plasma prolactin secretion to levels of without U69,593 treatment.
Navacaprant (BTRX-335140) (1 mg/kg; i.p. once) blocks U-50488-induced antinociception from hot water.
1.19 Pharmacokinetic Parameters of BTRX-335140 in rodents.

	Rats IV 1 mg/kg	Mice IV 3 mg/kg	Rats PO 5 mg/kg	Mice PO 10 mg/kg
CL (mL/min/kg)	105	66.5
t_1/2 (h)	1.81	1.91	6.19	2.57
AUC_0-t (h•ng/mL)	153	725	265	232
V_ss (L/kg)	13.8	7.72
F (%)			30.2	12

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

Animal Model:	Rat PRL model
Dosage:	0.01, 0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration:	Oral gavage; 0.01-3 mg/kg once
Result:	Effectively decreased the high level prolactin caused by U69,593 even at a dosage of 0.1 mg/kg.

Animal Model:	Adult male ICR mice with tail dipped into 50°C hot water
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; 1 mg/kg once
Result:	Blocked the U-50488-induced antinociception at 1 h but not at 24 h pretreatment time and showed a medication-like duration of action in blocking the KOR.

体内研究

	Rats IV 1 mg/kg	Mice IV 3 mg/kg	Rats PO 5 mg/kg	Mice PO 10 mg/kg
CL (mL/min/kg)	105	66.5
t_1/2 (h)	1.81	1.91	6.19	2.57
AUC_0-t (h•ng/mL)	153	725	265	232
V_ss (L/kg)	13.8	7.72
F (%)			30.2	12

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

Animal Model:	Rat PRL model
Dosage:	0.01, 0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration:	Oral gavage; 0.01-3 mg/kg once
Result:	Effectively decreased the high level prolactin caused by U69,593 even at a dosage of 0.1 mg/kg.

Animal Model:	Adult male ICR mice with tail dipped into 50°C hot water
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; 1 mg/kg once
Result:	Blocked the U-50488-induced antinociception at 1 h but not at 24 h pretreatment time and showed a medication-like duration of action in blocking the KOR.

体内研究

	Rats IV 1 mg/kg	Mice IV 3 mg/kg	Rats PO 5 mg/kg	Mice PO 10 mg/kg
CL (mL/min/kg)	105	66.5
t_1/2 (h)	1.81	1.91	6.19	2.57
AUC_0-t (h•ng/mL)	153	725	265	232
V_ss (L/kg)	13.8	7.72
F (%)			30.2	12

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

Animal Model:	Rat PRL model
Dosage:	0.01, 0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration:	Oral gavage; 0.01-3 mg/kg once
Result:	Effectively decreased the high level prolactin caused by U69,593 even at a dosage of 0.1 mg/kg.

Animal Model:	Adult male ICR mice with tail dipped into 50°C hot water
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; 1 mg/kg once
Result:	Blocked the U-50488-induced antinociception at 1 h but not at 24 h pretreatment time and showed a medication-like duration of action in blocking the KOR.

性状

Solid

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (36.75 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2048 mL	11.0241 mL	22.0483 mL
5 mM	0.4410 mL	2.2048 mL	4.4097 mL
10 mM	0.2205 mL	1.1024 mL	2.2048 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 90% corn oil
Solubility: ≥ 1.67 mg/mL (3.68 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.68 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1 mg/mL (2.20 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.20 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (2.20 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.20 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 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