2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. AM6545

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.

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AM6545 Chemical Structure

AM6545 Chemical Structure

CAS No. : 1245626-05-4

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AM6545 Related Antibodies

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Description

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[1][2][3].

In Vitro

AM6545 (3 μM; cAMP assay) does not affect forskolin (HY-15371)-induced cAMP levels in HEK293 cells, exhibiting neutral antagonist properties[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AM6545 Related Antibodies

Cell Viability Assay[1]

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.
In Vivo

AM6545 (5-20 mg/kg; i.p.; once daily; 7 days or single dose) reduces food intake and sustaines body weight in Sprague Dawley rats at 10 and 20 mg/kg when treated chronically or acutely[1].
AM6545 (10 mg/kg; ip; single dose) treatment of C57BL/6 J mice specifically induces PKA signaling activation in adipose tissue and upregulated Akt-mTOR and ERK phosphorylation levels[2].

AM6545 (10 mg/kg; i.p.; once daily; 4 weeks) significantly improves renal function, inhibited proteinuria, uric acid excretion and renal fibrosis in a rat model of metabolic syndrome[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague Dawley rats (male, 250-275 g; normal/high-fat diet models)[1]
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)[3]
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 TGFβ1 expression.
Animal Model: C57BL/6 mice (male, 18.5-21.0 g; normal diet)[2]
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.
Molecular Weight

556.46

Formula

C26H23Cl2N5O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C2=CC=C(C#CCCC#N)C=C2)N(C3=C(C=C(Cl)C=C3)Cl)N=C1C(NN4CCS(CC4)(=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (179.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7971 mL 8.9854 mL 17.9707 mL 44.9269 mL
5 mM 0.3594 mL 1.7971 mL 3.5941 mL 8.9854 mL
10 mM 0.1797 mL 0.8985 mL 1.7971 mL 4.4927 mL
15 mM 0.1198 mL 0.5990 mL 1.1980 mL 2.9951 mL
20 mM 0.0899 mL 0.4493 mL 0.8985 mL 2.2463 mL
25 mM 0.0719 mL 0.3594 mL 0.7188 mL 1.7971 mL
30 mM 0.0599 mL 0.2995 mL 0.5990 mL 1.4976 mL
40 mM 0.0449 mL 0.2246 mL 0.4493 mL 1.1232 mL
50 mM 0.0359 mL 0.1797 mL 0.3594 mL 0.8985 mL
60 mM 0.0300 mL 0.1498 mL 0.2995 mL 0.7488 mL
80 mM 0.0225 mL 0.1123 mL 0.2246 mL 0.5616 mL
100 mM 0.0180 mL 0.0899 mL 0.1797 mL 0.4493 mL
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AM6545 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AM65451245626-05-4AM 6545AM-6545Cannabinoid Receptorperipherally activecannabinoid receptorlimited brain penetrationCB1 receptor antagonistfood intakeconditioned gapingconditioned taste avoidanceInhibitorinhibitorinhibit

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