ML-00253764 (hydrochloride) - CAS:1706524-94-8

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ML-00253764 (hydrochloride)

目录号 : KCM11943 CAS No. : 1706524-94-8 纯度 : ≥98%

Data Sheet 产品使用指南

ML-00253764 is a melanocortin receptor 4 (MC4R) antagonist (K = 0.16 µM). It is selective for MC4R over MC3R and MC5R (ICs = 0.32, 0.81, and 2.12 µM, respectively). ML-00253764 (100 µM) decreases cAMP production induced by [NLE,D-Phe]-α-melanocyte stimulating hormone ([NDP]-α-MSH; ) by 20% in MC4R-expressing HEK293 cell membranes, but has no effect on cAMP levels in MC3R- or MC5R-expressing membranes. It prevents the loss of lean body mass and enhances light-phase food consumption in a Lewis lung carcinoma (LLC) mouse model but does not reduce tumor size when administered at a dose of 15 mg/kg.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg		In-stock

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生物活性

ML-00253764 (hydrochloride) is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC₅₀ of 0.16 μM and 0.103 μM, respectively. ML-00253764 can cross blood-brain barrier.

体外研究

ML-00253764 can inhibit the binding of NDP - α - MSH, with average IC₅₀ values of 0.32 μM, 0.81 μM, and 2.12 μM for hMC4-R, hMC3-R, and hMC5-R, respectively.
ML-00253764 (100 μM) can reduce cAMP production induced by [NFE4, D-Phe7] - α - melanocyte stimulating hormone ([NDP] - α - MSH) by 20% in HEK293 cell membranes expressing MC4R, but has no effect on cAMP levels in cell membranes expressing MC3R or MC5R.

体内研究

ML-00253764 (subcutaneous injection; 3. 10 or 30 mg/kg; Chronic peripheral administration once a day in BALB/c mice carrying CT-26 tumors can effectively prevent tumor induced weight loss.

Animal Model:	CT-26 tumor bearing BALB/c mice
Dosage:	3, 10, or 30 mg/kg
Administration:	Subcutaneous injection; 3, 10, or 30 mg/kg; once daily
Result:	Reduced tumor-induced weight loss in a mouse model.

分子式

C₁₈H₁₈BrFN₂O^.HCl

分子量

413.71

CAS号

1706524-94-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (30.21 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4172 mL	12.0858 mL	24.1715 mL
5 mM	0.4834 mL	2.4172 mL	4.8343 mL
10 mM	0.2417 mL	1.2086 mL	2.4172 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 (sealed storage, away from moisture)。-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: ≥ 1.25 mg/mL (3.02 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.02 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 12.5 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。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.25 mg/mL (3.02 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.02 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 12.5 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。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 1.25 mg/mL (3.02 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.02 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 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。