Home GPCR & G Protein Cannabinoid Receptor agonist BML-190 For research use only.

BML-190

Synonyms: IMMA

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 Chemical Structure

BML-190 Chemical Structure

CAS: 2854-32-2

Selleck's BML-190 has been cited by 2 Publications

1 Customer Review

Purity & Quality Control

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

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Signaling Pathway

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Biological Activity

Description BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
Targets
CB2 [1]
435 nM(Ki)
In vitro
In vitro BML-190 has 50-fold selectivity for CB2 receptors over CB1 receptors. In HEK-293 cells stably expressing the human CB2 receptor, BML-190 potentiates the forskolin-stimulated accumulation of cAMP. BML-190 reduces the basal levels of inositol phosphate production in cells expressing the CB2 receptor. 10 μM of BML-190 decreases inositol phosphates accumulation by 38%. [1] BML-190 is an aminoalkylindole. BML-190 is found to yield at least 15 metabolic products. [2] BML-190 diminishes LPS-induced NO and IL-6 production in a concentration-dependent manner. BML-190 also inhibits LPS-induced PGE2 production and COX-2 induction. [3]
Cell Research Cell lines 293/CB2 cells with [3H]adenine (1 μCi/mL)
Concentrations 0 μM -100 μM
Incubation Time 20 hours–24 hours
Method 293/CB2 cells are labeled with [3H]adenine (1 μCi/mL) in MEM with 1% FBS for 20 hours-24 hours. Labelled cells are challenged with 50 μM forskolin and appropriate BML-190 for 30 minutes at 37°C and assayed for cAMP accumulation. For IP assays, 2 × 105 293/CB2 cells are transiently transfected with 16z44 and/or pcDNA3 using transfection reagents. Cells are labelled, challenged with BML-190 and assayed for IP production. Triplicates are performed for each data point and at least three separate trials are done for each ligand.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01123655 Completed
Rheumatoid Arthritis
VA Office of Research and Development
 October 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 426.89 Formula

C23H23ClN2O4
CAS No. 2854-32-2 SDF Download BML-190 SDF
Smiles CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)N4CCOCC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 22 mg/mL ( (51.53 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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