TM 38837

Product Description

TM 38837 is a highly potent cannabinoid 1 receptor (CB₁) inverse agonist (IC₅₀ values are 8.5 nM and 605 nM for inhibition of [³H]-CP 55940 binding at CB₁ and CB₂ receptors, respectively). Displays 71-fold selectivity for CB₁ receptors over CB₂ receptors. Inhibits GTP binding to CB₁-overexpressing cell membranes in vitro (EC₅₀ = 18.5 nM). Peripherally restricted. Promotes fear behaviors when given by intracerebrovascular (icv) injection in mice.

Solubility

Preparing Stock Solutions for TM 38837

The following data is based on the product molecular weight 617.51

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	8.10 mL	40.49 mL	80.97 mL
1 mM	1.62 mL	8.10 mL	16.19 mL
2 mM	0.81 mL	4.05 mL	8.10 mL
10 mM	0.16 mL	0.81 mL	1.62 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Takano Low brain CB₁ receptor occupancy by a second generation CB₁ receptor antagonist TM38837 in comparison with rimonabant in nonhuman primates: a PET study. Synapse. 2014 PMID: 24293119
• Micale The cannabinoid CB₁ antagonist TM38837 with limited penetrance to the brain shows reduced fear-promoting effects in mice. Front.Pharmacol. 2019 PMID: 30949045
• Hung Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist. Chem.Med.Chem. 2010 PMID: 20652930