BML-190

ArtNr	S2854-1000
Hersteller	Selleckchem
CAS-Nr.	2854-32-2
Menge	1 g
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 50 mg 5 g
Kategorie	Metabolism Diabetes Glucose Homeostasis Inhibitors & Compound Libraries Small Molecules
Typ	Inhibitors
Specific against	other
Smiles	CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)N4CCOCC4
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	IMMA
Similar products	BML-190
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	426, 89
Cell lines	293/CB2 cells with [3H]adenine (1 uCi/mL)
Concentrations	0 uM -100 uM
IC50	435 nM (Ki) [1], 435 nM (Ki) [1], 435 nM (Ki) [1], 435 nM (Ki) [1], 435 nM (Ki) [1], 435 nM (Ki) [1]
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 uM 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]
Incubation Time	20 hoursâ€“24 hours
Method	293/CB2 cells are labeled with [3H]adenine (1 uCi/mL) in MEM with 1% FBS for 20 hours-24 hours. Labelled cells are challenged with 50 uM forskolin and appropriate BML-190 for 30 minutes at 37C 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.
Solubility (25C)	DMSO 22 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
Chemical Name	Ethanone, 2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-1-(4-morpholinyl)-

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