Potent cPLA2α inhibitor
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CAY10650

Item No. 10743

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(2-methyl-1-oxopropyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid
CAS Number
1233706-88-1
Molecular Formula
C28H25NO6
Formula Weight
471.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
SMILES
O=C(CN1C(C=CC(C(O)=O)=C2)=C2C(C(C(C)C)=O)=C1)COC3=CC=C(OC4=CC=CC=C4)C=C3
InChi Code
InChI=1S/C28H25NO6/c1-18(2)27(31)25-16-29(26-13-8-19(28(32)33)14-24(25)26)15-20(30)17-34-21-9-11-23(12-10-21)35-22-6-4-3-5-7-22/h3-14,16,18H,15,17H2,1-2H3,(H,32,33)
InChi Key
HTOJZPHWNDZOPQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $50

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    5 mg

    $186

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    10 mg

    $273

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    25 mg

    $557

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    Product Description

    Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.1 CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor.2 It demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.2 The phase I metabolite of this compound, CAY10641 (Item No. 10662), is also available.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schaloske, R.H., and Dennis, E.A. The phospholipase A2 superfamily and its group numbering system. Biochim. Biophys. Acta 1761(11), 1246-1259 (2006).

    2. Drews, A., Bovens, S., Roebrock, K., et al. 1-(5-carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α with reduced lipophilicity: Synthesis, biological activity, metabolic stability, solubility, bioavailability, and topical in vivo activity. J. Med. Chem. 53(14), 5165-5178 (2010).