AM 6545

Pricing Availability Delivery Time Qty
Cat.No. 5443 - AM 6545 | C26H23Cl2N5O3S | CAS No. 1245626-05-4
Description: High affinity and selective CB1 antagonist
Chemical Name: 5-[4-(4-Cyano-1-butyn-1-yl)phenyl]-1-(2,4-dichlorophenyl)-N-(1,1-dioxido-4-thiomorpholinyl)-4-methyl-1H-pyrazole-3-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

High affinity and selective CB1 antagonist (Ki = 3.3 nM). Exhibits >100-fold selectivity for CB1 over CB2 receptors. Improves glucose homeostasis, reverses hepatic steatosis and reduces body weight in diet-induced obese mice. Orally available and non-brain penetrant.

Technical Data

M. Wt 556.46
Formula C26H23Cl2N5O3S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1245626-05-4
PubChem ID 46912919
InChI Key XBHQLFVDGLPBCK-UHFFFAOYSA-N
Smiles O=C(NN3CCS(CC3)(=O)=O)C1=NN(C2=CC=C(Cl)C=C2Cl)C(C4=CC=C(C#CCCC#N)C=C4)=C1C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.13 20

Preparing Stock Solutions

The following data is based on the product molecular weight 556.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.8 mL 8.99 mL 17.97 mL
5 mM 0.36 mL 1.8 mL 3.59 mL
10 mM 0.18 mL 0.9 mL 1.8 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Tam et al (2010) Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity. J.Clin.Invest. 120 2953 PMID: 20664173

Bowles et al (2015) A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome. Proc.Natl.Acad.Sci.U.S.A. 112 285 PMID: 25535367


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Keywords: AM6545 CB1 receptors antagonists high affinity selective obesity lipids glucose CB1 Receptors

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