HET0016
- Product Name
- HET0016
- CAS No.
- 339068-25-6
- Chemical Name
- HET0016
- Synonyms
- HET0016;HET0016,HET-0016;N-Hydroxy-N(4-butyl-2-methylphenyl)formamidine;N-HYDROXY-N'-(4-N-BUTYL-2-METHYLPHENYL)FORMANIDINE;N’-(4-Butyl-2-methylphenyl)-N-hydroxyformimidamide;N-(4-butyl-2-methylphenyl)-N'-hydroxyiminoformamide;N-(4-BUTYL-2-METHYLPHENYL)-N'-HYDROXY-METHANIMIDAMIDE;Methanimidamide, N'-(4-butyl-2-methylphenyl)-N-hydroxy-
- CBNumber
- CB0149064
- Molecular Formula
- C12H18N2O
- Formula Weight
- 206.28
- MOL File
- 339068-25-6.mol
HET0016 Property
- Melting point:
- 138-140°C
- storage temp.
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- solubility
- Chloroform (Slightly), Ethanol (Slightly)
- form
- Light pink solid.
- color
- White to Pale Yellow
- CAS DataBase Reference
- 339068-25-6
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P405Store locked up.
N-Bromosuccinimide Price
- Product number
- J67168
- Product name
- HET-0016, 98%
- Packaging
- 1mg
- Price
- $21.8
- Updated
- 2021/12/16
- Product number
- J67168
- Product name
- HET-0016, 98%
- Packaging
- 5mg
- Price
- $107
- Updated
- 2021/12/16
- Product number
- 75780
- Product name
- HET0016
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $17
- Updated
- 2024/03/01
- Product number
- 75780
- Product name
- HET0016
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $67
- Updated
- 2024/03/01
- Product number
- J67168
- Product name
- HET-0016, 98%
- Packaging
- 10mg
- Price
- $235
- Updated
- 2023/06/20
HET0016 Chemical Properties,Usage,Production
Description
20-
Chemical Properties
Light Pink Solid
Uses
20-HETE is a major biologically active cytochrome P450 (CYP450) metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an IC50 of 8.9 nM, selectively inhibiting CYP4A and 4F isoforms. HET0016 inhibits CYP2C9, CYP2D6, and CYP3A4, enzymes important in drug metabolism, significantly less effectively with IC50s in the μM range. The IC50 values for inhibition of cyclooxygenase and epoxyeicosatrienoic acids (EETs) formation are 2.3 and 2.8 μM, respectively.[Cayman Chemical]
Uses
HET-0016 is a potent and selective inhibitor of the biosynthesis of 20-HETE acting via inhibition of CYP4A (IC50=8.9nM (human), 35nM (rat renal microsome). IC50 cyclooxygenase=2.3uM. IC50 for other CYP’s: CYP2C9-3.3uM, CYP2D6=83.9 uM, CYP3A4=71uM. It inhibits cerebrovascular constriction induced by Ca2+ or archidonate and inhibits angiogenesis and endothelial cell sprouting in various models. Displays protective effect on brain damage after temporary focal ischemia (at 10mg/Kg).
Definition
ChEBI: HET0016 is a member of toluenes.
in vitro
het0016 showed a high degree of selectivity in inhibiting the formation of 20-hete in rat renal microsomes. the ic(50) value averaged 35 nm, whereas the ic(50) value for inhibition of the formation of epoxyeicosatrienoic acids averaged 2800 nm. moreover, in human renal microsomes, het0016 could potently inhibit the formation of 20-hete with an ic(50) value of 8.9 nm. in addition, higher het0016 concentrations could also inhibit the cyp2c9, cyp2d6 and cyp3a4-catalysed substrates oxidation [1].
in vivo
a previous study generated an improved iv formulation of het0016 with hpβcd. administration of a single iv dose led to 7-fold higher levels of het0016 in plasma and 3.6-fold higher levels in tumor than that in ip route. iv treatment with hpβcd-het0016 decreased tumor growth, and altered vascular kinetics in early and late treatment groups. moreover, similar growth inhibition was observed in syngeneic gl261 gbm. in addition, survival studies using patient derived xenografts of gbm811, showed prolonged survival to 26 weeks in animals treated with focal radiation, in combination with het0016 and tmz [2].
IC 50
35 nm for 20-hete formation in rat renal microsomes
References
[1] miyata, n. ,taniguchi, k.,seki, t., et al. het0016, a potent and selective inhibitor of 20-hete synthesizing enzyme. british journal of pharmacology 133, 325-329 (2001).
[2] jain m et al. intravenous formulation of het0016 decreased human glioblastoma growth and implicated survival benefit in rat xenograft models. sci rep. 2017 jan 31;7:41809.
HET0016 Preparation Products And Raw materials
Raw materials
Preparation Products
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