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.

For research use only. We do not sell to patients.

AM6545 Chemical Structure

AM6545 Chemical Structure

CAS No. : 1245626-05-4

Size Price Stock Quantity
1 mg Get quote 3 - 4 weeks 4 - 5 weeks 2 - 3 weeks
5 mg   Get quote  
10 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

AM6545 Related Antibodies

Top Publications Citing Use of Products

View All Cannabinoid Receptor Isoform Specific Products:

View All Isoforms
CB1 CB2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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 : 11.13 mg/mL (20.00 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
Calculation results:
Working solution concentration: mg/mL
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AM6545
Cat. No.:
HY-110206
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (392 KB) Français - FR (392 KB) Deutsch - DE (392 KB) Norwegian - NO (392 KB) Español - ES (392 KB) Swedish - SV (392 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.