LUF6000

LUF6000 is a positive allosteric modulator of adenosine A3 receptors. It reduces dissociation of the agonist I-AB-MECA from A3 receptors and increases the efficacy, but not potency, of 2-Cl-IB-MECA-induced inhibition of forskolin-stimulated cAMP accumulation by 45% in CHO cells expressing the human receptor when used at a concentration of 10 µM. LUF6000 (100 µg/kg, three times per day) reduces joint edema and decreases levels of PI3K, IKK, IkappaB, and NF-kappaB in peripheral blood mononuclear cells (PBMCs) in a rat model of adjuvant-induced arthritis. It reduces knee edema in a rat model of osteoarthritis induced by monosodium iodoacetate (MIA) when administered at a dose of 100 µg/kg twice per day.Formal Name: 2-cyclohexyl-N-(3,4-dichlorophenyl)-3H-imidazo[4,5-c]quinolin-4-amine. CAS Number: 890087-21-5. Molecular Formula: C22H20Cl2N4. Formula Weight: 411.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 228, 264, 324, 337 nm. SMILES: ClC(C=C1)=C(Cl)C=C1NC2=NC3=C(C=CC=C3)C4=C2N=C(C5CCCCC5)N4. InChi Code: InChI=1S/C22H20Cl2N4/c23-16-11-10-14(12-17(16)24)25-22-20-19(15-8-4-5-9-18(15)26-22)27-21(28-20)13-6-2-1-3-7-13/h4-5,8-13H,1-3,6-7H2,(H,25,26)(H,27,28). InChi Key: UWJVRSIGHHSDSJ-UHFFFAOYSA-N.