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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-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
Molecular Weight:
206.28
MDL Number:
MFCD00277704
MOL File:
339068-25-6.mol
Last updated:2024-11-19 15:53:33

HET0016 Properties

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

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P261-P280a-P304+P340-P305+P351+P338-P405-P501a

HET0016 price More Price(21)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Alfa Aesar J67168 HET-0016, 98% 339068-25-6 1mg $21.8 2021-12-16 Buy
Alfa Aesar J67168 HET-0016, 98% 339068-25-6 5mg $107 2021-12-16 Buy
Cayman Chemical 75780 HET0016 ≥98% 339068-25-6 1mg $17 2024-03-01 Buy
Cayman Chemical 75780 HET0016 ≥98% 339068-25-6 5mg $67 2024-03-01 Buy
Alfa Aesar J67168 HET-0016, 98% 339068-25-6 10mg $235 2023-06-20 Buy
Product number Packaging Price Buy
J67168 1mg $21.8 Buy
J67168 5mg $107 Buy
75780 1mg $17 Buy
75780 5mg $67 Buy
J67168 10mg $235 Buy

HET0016 Chemical Properties,Uses,Production

Description

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.

Chemical Properties

Light Pink Solid

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).

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]

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

Global( 61)Suppliers
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32165 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10473 58
Labnetwork lnc.
+86-27-50766799 +8618062016861 contact@labnetwork.com China 19987 58
TargetMol Chemicals Inc.
support@targetmol.com United States 38632 58
Hebei Miaoyin Technology Co.,Ltd
+86-17367732028 +86-17367732028 kathy@hbyinsheng.com China 3512 58
Jilin Chinese Academy of Sciences-yanshen Technology
+undefined18143011203 info@chemextension.com China 42056 58
Aladdin Scientific
+1-+1(833)-552-7181 sales@aladdinsci.com United States 52925 58
J & K SCIENTIFIC LTD. 010-82848833 400-666-7788 jkinfo@jkchemical.com China 96815 76
Chemsky(shanghai)International Co.,Ltd. 021-50135380 shchemsky@sina.com China 32321 50
Shanghai TaoSu Biochemical Technology Co., Ltd. 021-33632979 info@tsbiochem.com China 8065 58

View Lastest Price from HET0016 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
HET0016 pictures 2024-11-19 HET0016
339068-25-6
US $29.00-0.00 / mg 98.84% 10g TargetMol Chemicals Inc.
HET0016 pictures 2024-11-19 HET0016
339068-25-6
US $29.00-0.00 / mg 98.84% 10g TargetMol Chemicals Inc.
  • HET0016 pictures
  • HET0016
    339068-25-6
  • US $29.00-0.00 / mg
  • 98.84%
  • TargetMol Chemicals Inc.
  • HET0016 pictures
  • HET0016
    339068-25-6
  • US $29.00-0.00 / mg
  • 98.84%
  • TargetMol Chemicals Inc.

HET0016 Spectrum

HET0016 N-HYDROXY-N'-(4-N-BUTYL-2-METHYLPHENYL)FORMANIDINE N-(4-BUTYL-2-METHYLPHENYL)-N'-HYDROXY-METHANIMIDAMIDE N-Hydroxy-N(4-butyl-2-methylphenyl)formamidine N-(4-butyl-2-methylphenyl)-N'-hydroxyiminoformamide N’-(4-Butyl-2-methylphenyl)-N-hydroxyformimidamide Methanimidamide, N'-(4-butyl-2-methylphenyl)-N-hydroxy- HET0016,HET-0016 N-Hydroxy-N’-(4-butyl-2-methylphenyl)formamidine 339068-25-6 Aromatics