A stearoyl-CoA desaturase inhibitor
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MK-8245

Item No. 29421

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[3-[4-(2-bromo-5-fluorophenoxy)-1-piperidinyl]-5-isoxazolyl]-2H-tetrazole-2-acetic acid
CAS Number
1030612-90-8
Molecular Formula
C17H16BrFN6O4
Formula Weight
467.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
229 nm
SMILES
BrC1=CC=C(F)C=C1OC2CCN(C3=NOC(C4=NN(CC(O)=O)N=N4)=C3)CC2
InChi Code
InChI=1S/C17H16BrFN6O4/c18-12-2-1-10(19)7-13(12)28-11-3-5-24(6-4-11)15-8-14(29-22-15)17-20-23-25(21-17)9-16(26)27/h1-2,7-8,11H,3-6,9H2,(H,26,27)
InChi Key
UJEAABFSXKCSGI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

    $295

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    10 mg

    $479

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    25 mg

    $920

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    Product Description

    MK-8245 is a liver-targeted inhibitor of stearoyl-CoA desaturase (SCD; IC50s = 3, 3, and 1 nM for rat, mouse, and human SCD1, respectively).1 It is selective for SCD1 over Δ5- and Δ6-desaturases (IC50s = >100,000 nM). MK-8245 (20-60 mg/kg) reduces the hepatic, but not Harderian gland, ratio of oleic acid to stearic acid, a marker of chronic SCD activity, and blood glucose levels, without inducing the formation of skin lesions or eye squinting behavior, in a mouse model of high-fat diet-induced obesity. It also inhibits hepatitis C virus (HCV) replication without inducing cytotoxicity in LucNeo2 cells (IC50 = 39.8 nM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Oballa, R.M., Belair, L., Black, W.C., et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J. Med. Chem. 54(14), 5082-5096 (2011).

    2. Nio, Y., Hasegawa, H., Okamura, H., et al. Liver-specific mono-unsaturated fatty acid synthase-1 inhibitor for anti-hepatitis C treatment. Antiviral Res. 132, 262-267 (2016).