An LTC4 synthase inhibitor
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TK05

Item No. 19793

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[5-[(4-chlorophenyl)(cyclopropylmethyl)amino]-2-pyridinyl]carbonyl]-2-(4-methoxybenzoyl)-benzoic acid
CAS Number
1245734-61-5
Molecular Formula
C31H25ClN2O5
Formula Weight
541.0
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleMethanol: soluble
SMILES
OC(C1=CC(C(C2=NC=C(N(CC3CC3)C4=CC=C(Cl)C=C4)C=C2)=O)=CC=C1C(C5=CC=C(OC)C=C5)=O)=O
InChi Code
InChI=1S/C31H25ClN2O5/c1-39-25-12-4-20(5-13-25)29(35)26-14-6-21(16-27(26)31(37)38)30(36)28-15-11-24(17-33-28)34(18-19-2-3-19)23-9-7-22(32)8-10-23/h4-17,19H,2-3,18H2,1H3,(H,37,38)
InChi Key
GRDDFJXOEAJYCT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $124

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    1 mg

    $235

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    Product Description

    TK05 is an inhibitor of leukotriene C4 (LTC4) synthase (IC50 = 95 nM).1 It is selective for LTC4 synthase over microsomal prostaglandin E synthase-1 (mPGES-1), microsomal glutathione S-transferase 2 (GST2), and 5-lipoxygenase (5-LO) at 10 µM. TK05 (1 µM) inhibits LTC4 synthase in Mono-Mac-6 leukemia cells and isolated human eosinophils, monocytes, and platelets but not cord blood-derived mast cells. In vivo, TK05 (0.12 and 6 mg/kg) prevents zymosan A-induced increases in peritoneal fluid levels of LTE4 and LTB4 in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kleinschmidt, T.K., Haraldsson, M., Basavarajappa, D., et al. Tandem benzophenone amino pyridines, potent and selective inhibitors of human leukotriene C4 synthase. J. Pharmacol. Exp. Ther. 355(1), 108-116 (2015).