product name BML-190
Description: BML-190, also known as IMMA, LM-4131 or Indomethacin Morpholinylamide, is a potent and selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. The binding affinity for the CB2 receptor is 435 nM compared to >20,000 nM for the cannabinoid receptor, CB1. BML-190 reduces the basal levels of inositol phosphate production in cells expressing the CB(2) receptor and 16z44.
References: FEBS Lett. 2003 Feb 11;536(1-3):157-60; Eur J Pharm Sci. 2010 Sep 11;41(1):163-72.
426.89
Formula
C23H23ClN2O4
CAS No.
2854-32-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 22 mg/mL (51.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
IMMA, LM-4131 or Indomethacin Morpholinylamide
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404313
| In Vitro |
In vitro activity: 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%. BML-190 is an aminoalkylindole. BML-190 is found to yield at least 15 metabolic products. 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. Kinase Assay: Cell Assay: In HEK-293 cells expressing human Cb2 receptor, BML-190 promoted the forskoline-stimulated accumulation of cAMP. BML-190 also reduced the basal level production of inositol phosphate the CB(2) receptor and 16z44-expressing cells. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | FEBS Lett. 2003 Feb 11;536(1-3):157-60; Eur J Pharm Sci. 2010 Sep 11;41(1):163-72. |
Related Posts
product name BML-190
Description: BML-190, also known as IMMA, LM-4131 or Indomethacin Morpholinylamide, is a potent and selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. The binding affinity for the CB2 receptor is 435 nM compared to >20,000 nM for the cannabinoid receptor, CB1. BML-190 reduces the basal levels of inositol phosphate production in cells expressing the CB(2) receptor and 16z44.
References: FEBS Lett. 2003 Feb 11;536(1-3):157-60; Eur J Pharm Sci. 2010 Sep 11;41(1):163-72.
426.89
Formula
C23H23ClN2O4
CAS No.
2854-32-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 22 mg/mL (51.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
IMMA, LM-4131 or Indomethacin Morpholinylamide
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404313
| In Vitro |
In vitro activity: 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%. BML-190 is an aminoalkylindole. BML-190 is found to yield at least 15 metabolic products. 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. Kinase Assay: Cell Assay: In HEK-293 cells expressing human Cb2 receptor, BML-190 promoted the forskoline-stimulated accumulation of cAMP. BML-190 also reduced the basal level production of inositol phosphate the CB(2) receptor and 16z44-expressing cells. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | FEBS Lett. 2003 Feb 11;536(1-3):157-60; Eur J Pharm Sci. 2010 Sep 11;41(1):163-72. |