A positive allosteric modulator of adenosine A3 receptors
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LUF6000

Item No. 28437

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMSO: soluble
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $90

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    1 mg

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    5 mg

    $783

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    Cayman Chemical
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    Product Description

    LUF6000 is a positive allosteric modulator of adenosine A3 receptors.1 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.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Göblyös, A., Gao, Z.-G., Brussee, J., et al. Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor. J. Med. Chem. 49(11), 3354-3361 (2006).

    2. Cohen, S., Barer, F., Bar-Yehuda, S., et al. A3 adenosine receptor allosteric modulator induces an anti-inflammatory effect: In vivo studies and molecular mechanism of action. Mediators Inflamm. 2014:708746, (2014).