A potent agonist of GPR35 and a mast cell stabilizer
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Lodoxamide

Item No. 23994

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,2'-[(2-chloro-5-cyano-1,3-phenylene)diimino]bis[2-oxo-acetic acid]
CAS Number
53882-12-5
Molecular Formula
C11H6ClN3O6
Formula Weight
311.6
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 5 mg/mlPBS (pH 7.2): 2 mg/mL
SMILES
ClC1=C(NC(C(O)=O)=O)C=C(C#N)C=C1NC(C(O)=O)=O
InChi Code
InChI=1S/C11H6ClN3O6/c12-7-5(14-8(16)10(18)19)1-4(3-13)2-6(7)15-9(17)11(20)21/h1-2H,(H,14,16)(H,15,17)(H,18,19)(H,20,21)
InChi Key
RVGLGHVJXCETIO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

    $107

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    50 mg

    $203

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    100 mg

    $381

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    250 mg

    $845

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    Cayman Chemical
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    Product Description

    Lodoxamide is a potent agonist of GPR35 with an EC50 value of 1.61 nM in a β-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor.1 It inhibits histamine release induced by compound 48/80 (Item No. 22173), anti-IgE, or A23187 (Item No. 11016) in isolated rat peritoneal mast cells (IC50s = 0.1-50 µM) and inhibits A23187-induced calcium influx in mast cells.2 It reduces antigen-induced histamine release from rat conjunctival tissue by 46% in vitro when used at a concentration of 10 µg/ml.3 Lodoxamine (0.1 and 10%, w/v) reduces the immediate hypersensitivity response in rat conjunctiva in vivo in a dose-dependent manner and reduces mast cell degranulation in a topical ovalbumin challenge.3,4 Formulations containing lodoxamide have been used in the treatment of vernal conjunctivitis and keratitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. MacKenzie, A.E., Caltabiano, G., Kent, T.C., et al. The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35. Mol. Pharmacol. 85(1), 91-104 (2014).

    2. Johnson, H.G., and Sheridan, A.Q. The characterization of lodoxamide, a very active inhibitor of mediator release, in animal and human models of asthma. Agents Actions 18(3-4), 301-305 (1986).

    3. Yanni, J.M., Weimer, L.K., Glaser, R.L., et al. Effect of lodoxamide on in vitro and in vivo conjunctival immediate hypersensitivity responses in rats. Int. Arch. Allergy. Immunol. 101(1), 102-106 (1993).

    4. Bayer, A., Uludağ, H.A., Sobaci, G., et al. Comparison of antiallergic drugs in an experimental model of ocular anaphylaxis. Ophthalmologica 217(2), 119-123 (2003).