TM 38837

Name: TM 38837
Brand: tocris
SKU: 7131

Catalog # 7131

Datasheet / COA / SDS

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$35 to United States

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Key Product Details

Description:	Highly potent CB₁ inverse agonist; peripherally restricted
Chemical Name:	1-(2,4-Dichlorophenyl)-4-ethyl-N-1-piperidinyl-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]-1H-pyrazole-3-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	617.51

View Full Technical Details for TM 38837

Biological Activity

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.

Technical Data

M. Wt	617.51
Formula	C₃₀H₂₅Cl₂F₃N₄OS
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1253641-65-4
PubChem ID	49779607
InChi Key	VQOCBFYUDSBDCZ-UHFFFAOYSA-N
Smiles	CCC1=C(C2=CC=C(C#CC3=CC=C(C(F)(F)F)C=C3)S2)N(C4=C(C=C(C=C4)Cl)Cl)N=C1C(NN5CCCCC5)=O

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	12.35	20
	ethanol	12.35	20

Preparing Stock Solutions

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 will affect the solvent volumes required to prepare stock solutions.

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

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References

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

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
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