Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewTM 38837
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)
Biological Activity for TM 38837
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.
Compound Libraries for TM 38837
TM 38837 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for TM 38837
| 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 Data for TM 38837
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 12.35 | 20 | |
| ethanol | 12.35 | 20 |
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 will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 8.1 mL | 40.49 mL | 80.97 mL |
| 1 mM | 1.62 mL | 8.1 mL | 16.19 mL |
| 2 mM | 0.81 mL | 4.05 mL | 8.1 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets for TM 38837
References for TM 38837
References are publications that support the biological activity of the product.
Hung et al (2010) 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. 5 1439 PMID: 20652930
Takano et al (2014) Low brain CB1 receptor occupancy by a second generation CB1 receptor antagonist TM38837 in comparison with rimonabant in nonhuman primates: a PET study. Synapse. 68 89 PMID: 24293119
Micale et al (2019) The cannabinoid CB1 antagonist TM38837 with limited penetrance to the brain shows reduced fear-promoting effects in mice. Front.Pharmacol. 10 PMID: 30949045
If you know of a relevant reference for TM 38837, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: TM 38837, TM 38837 supplier, TM38837, cannabinoid, CB1, receptor, inverse, agonist, highly, potent, peripherally, restricted, Receptors, 7131, Tocris Bioscience
Citations for TM 38837
Citations are publications that use Tocris products.
Currently there are no citations for TM 38837. Do you know of a great paper that uses TM 38837 from Tocris? Please let us know.
Reviews for TM 38837
There are currently no reviews for this product. Be the first to review TM 38837 and earn rewards!
Have you used TM 38837?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cannabinoid Receptor Ligands Scientific Review
Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.
Addiction Poster
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.