Home GPCR & G Protein Cannabinoid Receptor agonist BML-190

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BML-190 Cannabinoid Receptor agonist

Cat.No.S2854

BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
BML-190 Cannabinoid Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 426.89

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Quality Control

Batch: S285401 DMSO]22 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.76%
99.76

Solubility

In vitro
Batch:

DMSO : 22 mg/mL (51.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 426.89 Formula

C23H23ClN2O4

 Storage (From the date of receipt)
CAS No. 2854-32-2 Download SDF Storage of Stock Solutions

Synonyms IMMA Smiles CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)N4CCOCC4

Mechanism of Action

Targets/IC50/Ki
CB2
435 nM(Ki)
In vitro
BML-190 has 50-fold selectivity for CB2 receptors over CB1 receptors. In HEK-293 cells stably expressing the human CB2 receptor, this compound potentiates the forskolin-stimulated accumulation of cAMP. It reduces the basal levels of inositol phosphate production in cells expressing the CB2 receptor. 10 μM of this chemical decreases inositol phosphates accumulation by 38%. This compound is an aminoalkylindole. It is found to yield at least 15 metabolic products. It diminishes LPS-induced NO and IL-6 production in a concentration-dependent manner. This compound also inhibits LPS-induced PGE2 production and COX-2 induction.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01123655 Completed
Rheumatoid Arthritis
VA Office of Research and Development
 October 2009 Phase 1

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