BML-190

Catalog No.S2854 Batch:S285401

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Technical Data

Formula

C23H23ClN2O4
Molecular Weight 426.89 CAS No. 2854-32-2
Solubility (25°C)* In vitro DMSO 22 mg/mL (51.53 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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]

Protocol (from reference)

Cell Assay:[1]
  • 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.

Customer Product Validation

, , University of Alberta, 2014.

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

Fast-Acting and Receptor-Mediated Regulation of Neuronal Signaling Pathways by Copaiba Essential Oil. [ Int J Mol Sci, 2020, 21(7)] PubMed: 32218156
Novel Therapeutic Approaches for Inflammatory Bowel Disease. [Yahya Muhammad Fiteih , et al. University of Alberta, 2014, Yahya Muhammad Fiteih ]

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.