An LTA4 hydrolase inhibitor
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DG-051

Item No. 21688

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-pyrrolidinebutanoic acid, monohydrochloride
CAS Number
929915-58-2
Molecular Formula
C21H24ClNO4 • HCl
Formula Weight
426.3
Purity
≥98%
Formulation
A 10 mg/ml solution in ethanol
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 12.5 mg/mlEthanol: 12.5 mg/mlPBS (pH 7.2): 2 mg/ml
λmax
231, 279 nm
SMILES
ClC1=CC=C(OC2=CC=C(OC[C@@H]3CCCN3CCCC(O)=O)C=C2)C=C1.Cl
InChi Code
InChI=1S/C21H24ClNO4.ClH/c22-16-5-7-19(8-6-16)27-20-11-9-18(10-12-20)26-15-17-3-1-13-23(17)14-2-4-21(24)25;/h5-12,17H,1-4,13-15H2,(H,24,25);1H/t17-;/m0./s1
InChi Key
UCPVOTSNNAVKNE-LMOVPXPDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    25 mg

    $587

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    Product Description

    DG-051 is a potent, orally bioavailable leukotriene A4 hydrolase (LTA4H) inhibitor (Kd = 25 nM; IC50 = 47 nM), the enzyme that catalyzes the rate-determining step in the synthesis of LTB4 (Item No. 20110).1 However, it also inhibits the aminopeptidase activity of LTA4H with IC50 values of 72 and 150 nM when tested using the substrates L-alanine p-nitroanaline and prolyl-glycyl-proline peptide (PGP; Item No. 11188), respectively, potentially leading to PGP accumulation in vivo.1,2 DG-051 does not show any inhibitory activity against a panel of more than 50 additional aminopeptidases, ion channels, or HERG.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sandanayaka, V., Mamat, B., Mishra, R.K., et al. Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis. J. Med. Chem. 53(2), 573-585 (2010).

    2. Low, C.M., Akthar, S., Patel, D.F., et al. The development of novel LTA4H modulators to selectively target LTB4 generation. Sci. Rep. 7, 44449 (2017).