AM6545 - CAS:1245626-05-4

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AM6545

目录号 : KCM10800 CAS No. : 1245626-05-4 纯度 : ≥98%

Data Sheet 产品使用指南

Peripherally-restricted cannabinoid receptor 1 (CB) selective antagonists have the potential to inhibit food intake while also escaping centrally-mediated neuropsychiatric side effects. AM6545 is a novel CB selective neutral antagonist with low CNS penetration, exhibiting K values of 1.7 and 523 nM for CB and CB receptors, respectively. It reduces food intake and food-reinforced behavior, such as time spent feeding, in a dose-dependent manner, resulting in decreased body weight. AM6545 produces improvements in glucose homeostasis, fatty liver, and plasma lipid profiles in mice with diet-induced obesity. It does not affect behavior responses that are associated with activation of CB receptors in the brain.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
10 mM * 1 mL in DMSO		In-stock

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生物活性

AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications.

体外研究

AM6545 (3 μM; cAMP assay) does not affect Forskolin induced cAMP levels in HEK293 cells and exhibits neutral antagonist properties.

Cell Viability Assay

Cell Line:	HEK293 (hCB1/hCB2-transfected)
Concentration:	1.7 nM (CB1 binding), 3 mM (cAMP assay)
Incubation Time:
Result:	Showed high CB1 affinity (Ki=1.7 nM) and no effect on forskolin-stimulated cAMP accumulation in hCB1-expressing cells, acting as a neutral antagonist.

体内研究

AM6545 (5-20 mg/kg; i.p.; once per day; When Sprague Dawley is subjected to chronic or acute treatment for 7 days or a single dose, both 10 and 20 mg/kg reduce food intake and continue to decrease body weight.
After treatment with AM6545 (10 mg/kg; ip; single dose) in C57BL/6 J mice, specific activation of PKA signaling was induced in adipose tissue, and Akt mTOR and ERK phosphorylation levels were upregulated.
AM6545 (10 mg/kg; i.p.; once per day; 4 weeks) significantly improved renal function, inhibited proteinuria, uric acid excretion, and renal fibrosis in a large model of metabolic syndrome.

Animal Model:	Sprague Dawley rats (male, 250-275 g; normal/high-fat diet models)
Dosage:	5 mg/kg, 10 mg/kg, 20 mg/kg (4% DMSO, 1% Tween 80 in saline)
Administration:	Intraperitoneal injection, daily for 7 days or single dose.
Result:	Reduced food intake (30% inhibition at 3 h) and body weight gain (days 4-7) at 10 mg/kg dose, without inducing conditioned taste avoidance or gaping.

Animal Model:	Metabolic syndrome rats (male, Wistar; high-fructose/high-salt diet-induced)
Dosage:	10 mg/kg (0.5% carboxymethylcellulose)
Administration:	Intraperitoneal injection, daily for 4 weeks
Result:	Reduced proteinuria (50%) and urinary uric acid (attenuated 10-fold increase), alleviated glomerular hypertrophy, tubular injury, and collagen deposition, and suppressed renal TGF β1 expression

Animal Model:	C57BL/6 mice (male, 18.5-21.0 g; normal diet)
Dosage:	10 mg/kg (4% DMSO, 10% Tween 80, 80-95% saline)
Administration:	Intraperitoneal injection, single.
Result:	Significantly modified p-PKA substrates in adipose and liver tissue, but the responsive substrates are tissue-specific and remain to be determined Upregulated ERK1 phosphorylation at Thr202 in WAT, liver, TA. Upregulated p-Akt(Ser473) and p-mTOR(Ser2448) in liver.

分子式

C₂₆H₂₃Cl₂N₅O₃S

分子量

556.5

CAS号

1245626-05-4

中文名称

AM 6545

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (179.71 mM)

* "≥" means soluble, but saturation unknown

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7971 mL	8.9854 mL	17.9707 mL
5 mM	0.3594 mL	1.7971 mL	3.5941 mL
10 mM	0.1797 mL	0.8985 mL	1.7971 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 (4.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.49 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。
2.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.49 mM); Clear solution

此方案可获得 ≥ 2.5 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： ≥98%

Data Sheet

产品使用指南

暂无相关参考文献

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器