A positive allosteric modulator of adenosine A3 receptors; reduces dissociation of I-AB-MECA from A3 receptors and increases the efficacy

LUF6000 – 500 µg

Brand:
Cayman
CAS:
890087-21-5
Storage:
-20
UN-No:
Non-Hazardous - /

LUF6000 is a positive allosteric modulator of adenosine A3 receptors.{42969} 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, IκB, and NF-κB in peripheral blood mononuclear cells (PBMCs) in a rat model of adjuvant-induced arthritis.{42970} 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.  

 

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SKU: 28437 - 500 µg Category:

Description

A positive allosteric modulator of adenosine A3 receptors; reduces dissociation of 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 at 10 μM; reduces joint edema and decreases levels of PI3K, IKK, IκB, and NF-κB in PBMCs in a rat model of adjuvant-induced arthritis at 100 μg/kg, three times per day; reduces knee edema in a rat model of MIA-induced osteoarthritis at 100 μg/kg twice per day

Formal name: 2-cyclohexyl-N-(3,4-dichlorophenyl)-3H-imidazo[4,5-c]quinolin-4-amine

Synonyms: 

Molecular weight: 411.3

CAS: 890087-21-5

Purity: ≥98%

Formulation: A solid

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