TM 38837

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.

Product information

CAS Number: 1253641-65-4

Molecular Weight: 617.51

Formula: C30H25Cl2F3N4OS

Synonym:

TM-38837

TM38837

Chemical Name: 1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-1H-pyrazole-3-carboxamide

Smiles: CCC1C(=NN(C=1C1=CC=C(C#CC2C=CC(=CC=2)C(F)(F)F)S1)C1=CC=C(Cl)C=C1Cl)C(=O)NN1CCCCC1

InChiKey: VQOCBFYUDSBDCZ-UHFFFAOYSA-N

InChi: InChI=1S/C30H25Cl2F3N4OS/c1-2-23-27(29(40)37-38-16-4-3-5-17-38)36-39(25-14-11-21(31)18-24(25)32)28(23)26-15-13-22(41-26)12-8-19-6-9-20(10-7-19)30(33,34)35/h6-7,9-11,13-15,18H,2-5,16-17H2,1H3,(H,37,40)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Micale V, et al. The Cannabinoid CB1 Antagonist TM38837 With Limited Penetrance to the Brain Shows ReducedFear-Promoting Effects in Mice. Front Pharmacol. 2019 Mar 20;10:207.
2. Klumpers LE, et al. Peripheral selectivity of the novel cannabinoid receptor antagonist TM38837 in healthy subjects. Br J Clin Pharmacol. 2013 Dec;76(6):846-57.

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