Aromatase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Aromatase.html AromataseAromatase (estrogen synthetase, CYP19) is a unique cytochrome P450 that catalyzes the removal of the 19-methyl group andaromatization of the A-ring of androgens for the synthesis of estrogens. All human estrogens are synthesized via this

2、 enzymaticaromatization pathway. Aromatase is most widely known for its roles in reproduction and reproductive system diseases, and as atarget for inhibitor therapy in estrogen-sensitive diseases including cancer, endometriosis, and leiomyoma.The selective inhibition of estrogen production by aromat

3、ase inhibitors is an efficient strategy for breast cancer treatment. Thesecompounds are classified as irreversible inhibitors of aromatase (type I), and comprise steroidal compounds. Reversible inhibitors ofaromatase, which comprises non-steroidal compounds are type II aromatase inhibitors. Second a

4、nd third generation aromataseinhibitors are considerably more potent and more specific in their ability to inhibit aromatase, as compared with first generationcompounds (aminoglutethimide).www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Aromatase.html Aromatase HYPERLINK https:/www.MedChemE/Tar

5、gets/Aromatase.html HYPERLINK https:/www.MedChemE/Targets/Aromatase.html Inhibitors HYPERLINK https:/www.MedChemE/alpha-naphthoflavone.html Alpha-NaphthoflavoneCat. No.: HY-125833 HYPERLINK https:/www.MedChemE/Anastrozole.html Anastrozole(ZD1033) Cat. No.: HY-14274Alpha-Naphthoflavone is a synthetic

6、 flavonoid,acts as a potent and competitive aromataseinhibitor with an IC50 and a Ki of 0.5 and 0.2 M,respectively.Anastrozole is a potent, highly selectivearomatase inhibitor, which inhibits humanplacental aromatase with an IC of 15 nM.50Purity: 98.02%Clinical Data: No Development ReportedSize: 10

7、mM 1 mL, 5 mg, 10 mg, 20 mgPurity: 99.99%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/anastrozole-d12.html Anastrozole-d12(ZD1033-d12) Cat. No.: HY-14274S HYPERLINK https:/www.MedChemE/anastrozole-d3-dimer-impurity.html Anastrozole-d3 HYPERLINK https:/w

8、ww.MedChemE/anastrozole-d3-dimer-impurity.html HYPERLINK https:/www.MedChemE/anastrozole-d3-dimer-impurity.html Dimer HYPERLINK https:/www.MedChemE/anastrozole-d3-dimer-impurity.html HYPERLINK https:/www.MedChemE/anastrozole-d3-dimer-impurity.html ImpurityCat. No.: HY-14274S1Anastrozole-d12 (ZD1033-

9、d12) is the deuteriumlabeled Anastrozole. Anastrozole is a potent,highly selective aromatase inhibitor, whichinhibits human placental aromatase with an IC of5015 nM.Anastrozole-d3 Dimer Impurity is the deuteriumlabeled Anastrozole. Anastrozole is a potent,highly selective aromatase inhibitor, whichi

10、nhibits human placental aromatase with an IC of5015 nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 10 mg HYPERLINK https:/www.MedChemE/androsta-1-4-6-triene-3-17-dione.html Androsta-1,4,6-triene-3,17-dione HYPERLINK https:/

11、www.MedChemE/androsta-1-4-6-triene-3-17-dione.html HYPERLINK https:/www.MedChemE/Endoxifen.html EndoxifenCat. No.: HY-136092 Cat. No.: HY-18719EAndrosta-1,4,6-triene-3,17-dione is a lipophilicand specific aromatase inhibitor with a K ofi0.18 M. Androsta-1,4,6-triene-3,17-dione inhibitsestrogen biosy

12、nthesis and shows antifertilityeffects. Androsta-1,4,6-triene-3,17-dione inducesimpairment of spatial memory.Endoxifen is a key active metabolite of tamoxifen(TAM) with higher affinity and specificity toestrogen receptor that also inhibits aromataseactivity. Endoxifen has the potential for breastcan

13、cer study.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Endoxifen-hydrochloride.html Endoxifen HYPERLINK https:/www.MedChemE/Endoxifen-hydrochloride.html HYPERLINK https:/www.MedChemE/E

14、ndoxifen-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Endoxifen-hydrochloride.html HYPERLINK https:/www.MedChemE/endoxifen-d5-1-1-e-z-mixture.html Endoxifen-d5Cat. No.: HY-18719B Cat. No.: HY-18719ESEndoxifen hydrochloride is a key active metaboliteof Tamoxifen (TAM) with higher af

15、finity andspecificity to estrogen receptor that alsoinhibits aromatase activity. Endoxifenhydrochloride has the potential for breast cancerstudy.Endoxifen-d5 is the deuterium labeled Endoxifen.Endoxifen is a key active metabolite of tamoxifen(TAM) with higher affinity and specificity toestrogen rece

16、ptor that also inhibits aromataseactivity. Endoxifen has the potential for breastcancer study.Purity: 98.20%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/eriodictyol-chalcon

17、e.html Eriodictyol HYPERLINK https:/www.MedChemE/eriodictyol-chalcone.html HYPERLINK https:/www.MedChemE/eriodictyol-chalcone.html chalcone HYPERLINK https:/www.MedChemE/eriodictyol-chalcone.html HYPERLINK https:/www.MedChemE/Exemestane.html ExemestaneCat. No.: HY-N9551(FCE 24304; EXE) Cat. No.: HY-

18、13632Eriodictyol chalcone possesses bothanti-aromatase and an anti-17-HSD activity.Exemestane (FCE 24304) is a selective,irreversible and orally active steroidalaromatase inhibitor with IC s of 30 nM and 4050nM for human placental and rat ovarianaromatase, respectively. Exemestane can be usedfor hor

19、mone-dependent breast cancer research.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.95%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/exemestane-13c3.html Exem

20、estane-13C3Cat. No.: HY-13632S1 HYPERLINK https:/www.MedChemE/exemestane-d2.html Exemestane-D2(FCE 24304-D2; EXE-D2) Cat. No.: HY-13632SExemestane-13C3 is the 13C-labeled Exemestane.Exemestane (FCE 24304) is a selective,irreversible and orally active steroidalaromatase inhibitor with IC s of 30 nM a

21、nd 4050nM for human placental and rat ovarianaromatase, respectively.Exemestane-D2 (FCE 24304-D2) is the deuteriumlabeled Exemestane. Exemestane (FCE 24304) is aselective, irreversible and orally activesteroidal aromatase inhibitor with IC s of 3050nM and 40 nM for human placental and ratovarian aro

22、matase, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/exemestane-d3.html Exemestane-d3(FCE 24304-d3; EXE-d3) Cat. No.: HY-13632S2 HYPERLINK https:/www.MedChemE/Fadro

23、zole.html Fadrozole(CGS 16949A free base; (Rac)-FAD286) Cat. No.: HY-14247AExemestane-d3 (FCE 24304-d3) is the deuteriumlabeled Exemestane. Exemestane (FCE 24304) is aselective, irreversible and orally activesteroidal aromatase inhibitor with IC s of 3050nM and 40 nM for human placental and ratovari

24、an aromatase, respectively.Fadrozole (CGS 16949A free base) is a potent,selective and nonsteroidal inhibitor ofaromatase with an IC of 6.4 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.69%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HY

25、PERLINK https:/www.MedChemE/Fadrozole_hydrochloride.html Fadrozole HYPERLINK https:/www.MedChemE/Fadrozole_hydrochloride.html HYPERLINK https:/www.MedChemE/Fadrozole_hydrochloride.html hydrochloride(CGS 16949A; (Rac)-FAD286 hydrochloride) Cat. No.: HY-14247 HYPERLINK https:/www.MedChemE/flavanone.ht

26、ml FlavanoneCat. No.: HY-N7128Fadrozole hydrochloride (CGS 16949A) is a potent,selective and nonsteroidal inhibitor ofaromatase with an IC of 6.4 nM.50Flavanone is a naturally occurring flavone.Flavanone has inhibitory activity for humanestrogen synthetase (aromatase).Purity: 99.22%Clinical Data: La

27、unchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/isolimonexic-acid.html Isolimonexic HYPERLINK https:/www.MedChemE/isolimonexic-acid.html HYPERLINK https:/www.MedChemE/isolimonexic-acid

28、.html acid HYPERLINK https:/www.MedChemE/isolimonexic-acid.html HYPERLINK https:/www.MedChemE/Letrozole.html LetrozoleCat. No.: HY-N8405(CGS 20267) Cat. No.: HY-14248Isolimonexic acid is a limonoid isolated fromlemon (Citrus lemon L. Burm) seed, hasanti-cancer and anti-aromatase (IC =25.6050M) prope

29、rties.Letrozole (CGS 20267) is a potent, selective,reversible and orally active non-steroidalinhibitor of aromatase, with an IC of 11.550nM. Letrozole selective inhibits estrogenbiosynthesis, and can be used for the research ofbreast cancer.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg

30、, 10 mg, 25 mgPurity: 99.92%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/letrozole-d4.html Letrozole-d4 HYPERLINK https:/www.MedChemE/letrozole-d4.html HYPERLINK https:/www.MedChemE/oleuropein.html OleuropeinCat. No.: HY-14248S Cat. No.: HY-N0292Letro

31、zole-d4 (CGS 20267-d4) is the deuteriumlabeled Letrozole. Letrozole (CGS 20267) is apotent, selective, reversible and orally activenon-steroidal inhibitor of aromatase, with anIC of 11.5 nM.50Oleuropein, found in olive leaves and oil, exertsantioxidant, anti-inflammatory andanti-atherogenic effects

32、through direct inhibitionof PPAR transcriptional activity.Purity: 98%Clinical Data:Size: 1 mg, 10 mgPurity: 98.54%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Org30958.html Org30958 HYPERLINK https:/www.MedChemE/Org30958.html HYPERLINK https:/www.MedChemE/syn20028567.html SYN20028567Cat. No.: HY-U00176 Cat. No.: HY-146688Org30958 is