Potent, selective inhibitor of iNOS (NOS II). The Ki values for inhibition of iNOS (NOS II), nNOS (NOS I), and eNOS (NOS III) by ENIPO are 17, 10.3 and 58.2 µM, respectively, as determined using initial rate binding kinetics. However, ENIPO is a time-dependent inhibitor that, with longer incubations, demonstrates reversible tight binding inhibition that is selective for iNOS (NOS II) over nNOS (NOS I) or eNOS (NOS III). This selectivity results from iNOS (NOS II) exhibiting a 4-fold faster binding and 10-fold slower dissociation with ENIPO compared to nNOS (NOS I). Ki values for ENIPO binding to iNOS (NOS II) and nNOS (NOS I) are 0.56 and 6 µM, respectively. Accurate determination of the Ki value of ENIPO for eNOS (NOS III) has not been determined but is expected to be 50-fold less than iNOS (NOS II).
Product Details
| Alternative Name: | N5-[(3E)-1-Imino-3-pentenyl]-L-ornithine . HCl, ENIPO . HCl |
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| Formula: | C10H19N3O2 . HCl |
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| MW: | 213.3 . 36.5 |
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| Purity: | ≥97% (TLC) |
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| Identity: | Determined by IR, MS and 1H-NMR. |
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| Appearance: | White to off-white crystalline powder. |
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| Solubility: | Soluble in PBS, pH 7.2 (10mg/ml), 100% ethanol (10mg/ml), DMSO (2mg/ml) or dimethyl formamide (2mg/ml). |
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| Shipping: | Blue Ice |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 2 years after receipt when stored at -20°C.We do not recommend storing aqueous solutions for more than one day. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Structural characterization and kinetics of nitric-oxide synthase inhibition by novel N5-(iminoalkyl)- and N5-(iminoalkenyl)-ornithines: L.E. Bretscher, et al.; J. Biol. Chem.
278, 46789 (2003),
Abstract;
Full Text
General Literature References
Design of isoform-selective inhibitors of nitric oxide synthase: B.R. Babu & O.W. Griffith; Curr. Opin. Chem. Biol.
2, 491 (1998),
Abstract;
