ChemicalBook--->CAS DataBase List--->1253641-65-4

1253641-65-4

1253641-65-4 Structure

1253641-65-4 Structure
IdentificationBack Directory
[Name]

TM38837
[CAS]

1253641-65-4
[Synonyms]

TM38837
[Molecular Formula]

C30H25Cl2F3N4OS
[MDL Number]

MFCD26406003
[MOL File]

1253641-65-4.mol
[Molecular Weight]

617.51
Chemical PropertiesBack Directory
[Melting point ]

171-172 °C
[density ]

1.38±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO: 41.67 mg/mL (67.48 mM)
[form ]

Solid
[pka]

11.17±0.20(Predicted)
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Uses]

CB1 antagonist 4 (compound 8) is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. CB1 antagonist 4 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. CB1 antagonist 4 reduces propensity for psychiatric side effects[1][2].
[Biological Activity]

TM38837 is a peripherally selective cannabinoid receptor type 1 (CB1) receptor antagonist. It has limited brain penetration to minimize or prevent CNS adverse effects and retain potential anti-obesity effects. Also it can reduces the propensity for psychotic side effects.
[in vivo]

TM38837 (10-100 mg/kg; po) induces a significant increase in freezing behavior at 100 mg/kg.

< td class="col2"> 7-8 weeks old male C57BL/6 N mice (B6N)
Animal Model:
Dosage: 10, 30, or 100 mg/kg
Administration: po < /td>
Result: High dose (100 mg/kg) induced a significant increase in freezing behavior. < /td>
[target]

CB1

[IC 50]

CB1
[storage]

Store at -20°C
[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. DOI:10.3389/fphar.2019.00207
[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. DOI:10.1111/bcp.12141
Spectrum DetailBack Directory
[Spectrum Detail]

TM38837(1253641-65-4)1HNMR
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