RLX-33|cas:2784577-71-3|西域试剂

RLX-33,99.79%

产品编号：Bellancom-150700| CAS NO：2784577-71-3| 分子式：C₂₄H₁₉ClN₄O₄| 分子量：462.89

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货号	价格	库存与货期
Bellancom-150700	￥3800.00	杭州北京（现货）
Bellancom-150700	￥6000.00	杭州北京（现货）
Bellancom-150700	￥11500.00	杭州北京（现货）

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RLX-33

产品介绍

RLX-33 是一种有效且具有选择性和血脑屏障透过性的松弛素家族肽 3 (RXFP3) 拮抗剂，也阻断松弛素 3 (relaxin 3) 诱导的 ERK1/2 磷酸化，对 RXFP3、以及 ERK1 和 ERK2 磷酸化的 IC₅₀ 分别为 2.36 μM、7.82 μM 和 13.86 μM。RLX-33 能阻断 RXFP3 选择性激动剂 R3/I5 诱导的大鼠食物摄取增加。RLX-33 可用于代谢综合征的研究。

生物活性

RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC₅₀ values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome.

体外研究

体内研究

RLX-33 (10 mg/kg; IP, single dosage) attenuates the RXFP3-selective agonist R3/I5-induced increase in feeding in male Wistar rats.
RLX-33 (10 mg/kg; IP, single dosage) exhibits a good brain penetration and highly protein-bound in rats plasma.
Pharmacokinetic Parameters of RLX-33 in male Wistar rats (IP, 10 mg/kg).

	plasma	brain
C_max (ng/mL)	1401	1552
t_max (h)	0.5	2.0
t_1/2 (h)	1.9	4.9
AUC_inf (ng/mL·h)	5352	12519
CL_F (mL/min/kg)	43.8

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

Animal Model:	Male Wistar rats (intracerebroventricular administration of R3/I5 stimulated food intake
Dosage:	10 mg/kg
Administration:	IP, single dosage
Result:	Attenuated the R3/I5-induced increase in food intake.

Animal Model:	Male Wistar rats
Dosage:	10 mg/kg
Administration:	IP, single dosage (Pharmacokinetic Analysis)
Result:	Exhibited a good brain penetration and highly protein-bound, with protein binding of 99.8% in rat plasma.

体内研究

	plasma	brain
C_max (ng/mL)	1401	1552
t_max (h)	0.5	2.0
t_1/2 (h)	1.9	4.9
AUC_inf (ng/mL·h)	5352	12519
CL_F (mL/min/kg)	43.8

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

Animal Model:	Male Wistar rats (intracerebroventricular administration of R3/I5 stimulated food intake
Dosage:	10 mg/kg
Administration:	IP, single dosage
Result:	Attenuated the R3/I5-induced increase in food intake.

Animal Model:	Male Wistar rats
Dosage:	10 mg/kg
Administration:	IP, single dosage (Pharmacokinetic Analysis)
Result:	Exhibited a good brain penetration and highly protein-bound, with protein binding of 99.8% in rat plasma.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (270.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1603 mL	10.8017 mL	21.6034 mL
5 mM	0.4321 mL	2.1603 mL	4.3207 mL
10 mM	0.2160 mL	1.0802 mL	2.1603 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: ≥ 2.08 mg/mL (4.49 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.49 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。