A nonspecific CYP450 inhibitor
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SKF 525A (hydrochloride)

Item No. 15040

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α-phenyl-α-propyl-benzeneacetic acid, 2-(diethylamino)ethyl ester, monohydrochloride
CAS Number
62-68-0
Synonyms
  • RP 5171
  • U 5446
Molecular Formula
C23H31NO2 • HCl
Formula Weight
390.0
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/mlPBS (pH 7.2): 0.14 mg/ml
SMILES
O=C(OCCN(CC)CC)C(C1=CC=CC=C1)(CCC)C2=CC=CC=C2.Cl
InChi Code
InChI=1S/C23H31NO2.ClH/c1-4-17-23(20-13-9-7-10-14-20,21-15-11-8-12-16-21)22(25)26-19-18-24(5-2)6-3;/h7-16H,4-6,17-19H2,1-3H3;1H
InChi Key
FHIKZROVIDCMJA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    100 mg

    $63

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    250 mg

    $99

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    500 mg

    $183

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    1 g

    $303

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    Product Description

    SKF 525A is a widely used, nonspecific cytochrome P (CYP)450 inhibitor that demonstrates 100% inhibition of the various CYP450 isoforms at 1-100 μM.1 It therefore potentiates the effects of many different drugs by inhibiting their metabolism (IC50 values in the μM range when tested using human liver microsomes).2 SKF 525A inhibits CYP450-dependent arachidonic acid conversion to active EET metabolites, antagonizing the recovery of functional calcium pools.3 It also acts as a noncompetitive inhibitor of acetylcholine nicotinic receptors (IC50 = 19 μM in mouse skeletal muscle).4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Franklin, M.R., and Hathaway, L.B. 2-Diethylaminoethyl-2,2-diphenylvalerate-HCl (SKF525A) revisited: Comparative cytochrome P450 inhibition in human liver microsomes by SKF525A, its metabolites, and SKF-acid and SKF-alcohol. Drug Metab. Dispos. 36(12), 2539-2546 (2008).

    2. Emoto, C., Murase, S., Sawada, Y., et al. In vitro inhibitory effect of 1-aminobenzotriazole on drug oxidations in human liver microsomes: A comparison with SKF-525A. Drug Metab. Pharmacokinet. 20(5), 351-357 (2005).

    3. Graber, M.N., Alfonso, A., and Gill, D.L. Recovery of Ca2+ pools and growth in Ca2+ pool-depleted cells is mediated by specific epoxyeicosatrienoic acids derived from arachidonic acid. The Journal of Biological Chemisty 272(47), 29546-29553 (1997).

    4. Kagota, S., Yamaguchi, Y., Nakamura, K., et al. Characterization of nitric oxide- and prostaglandin-independent relaxation in response to acetylcholine in rabbit renal artery. Clin. Exp. Pharmacol. Physiol. 26(10), 790-796 (1999).

    5. Spitzmaul, G., Gumilar, F., Dilger, J.P., et al. The local anaesthetics proadifen and adiphenine inhibit nicotinic receptors by different molecular mechanisms. Br. J. Pharmacol. 157(5), 804-817 (2009).