Aromatase/CYP19A1 Inhibitor

Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC₅₀ of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.

Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.

Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC₅₀s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.

Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC₅₀ of 15 nM.

Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase with the IC₅₀ and K_i values are 0.5 and 0.2 μM. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis.

Exemestane (Standard) is the analytical standard of Exemestane. This product is intended for research and analytical applications. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC₅₀s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.

Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.

(R)-4-Benzyl-2-oxazolidinone is an oxazolidinone-type auxiliary that enables highly stereoselective asymmetric alkylation reactions. (R)-4-Benzyl-2-oxazolidinone is applied in the total synthesis of natural products and pharmaceutical preparations. Especially in pharmaceutical research and development, (R)-4-Benzyl-2-oxazolidinone not only serves as a key precursor for the synthesis of aromatase inhibitors, but also can be used in studies related to estrogen-dependent breast cancer.

Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC₅₀ of 6.4 nM.

Aminoglutethimide (DL-Aminoglutethimide) is an orally active anticonvulsant with various endocrine-related side effects. Aminoglutethimide blocks multiple steroid hormone synthesis pathways by inhibiting several cytochrome P-450-dependent hydroxylases, such as aromatase, cholesterol side-chain cleavage enzyme, 11-hydroxylase, and 18-hydroxylase, with IC₅₀ values of 0.3, 3.5, 120, and 20 μM, respectively. Aminoglutethimide reduces cortisol levels. Aminoglutethimide can be used in research on Cushing's syndrome, breast cancer, and other conditions.

Clitorin is an orally active flavonoid compound that can be isolated from Carica papaya. Clitorin is an inhibitor of EGFR (IC₅₀: 89.58 nM) and aromatase (IC₅₀: 77.41 nM). Clitorin has antioxidant and anti-tumor activities. In the DPPH and ABTS radical scavenging assays, Clitorin has IC₅₀ values of 91.96 ppm and 250.45 ppm, respectively. In addition, Clitorin can regulate lipogenesis and fatty acid oxidation and can be used in the research of non-alcoholic fatty liver disease.

Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.

Fadrozole (CGS 16949A free base) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC₅₀ of 6.4 nM.

Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). Flavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy.

CYP19A1-IN-2 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC₅₀=0.09 nM). CYP19A1-IN-2 has potential for breast cancer research. CYP19A1-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

(R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer.

Endoxifen-d₅ is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.

7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19) activity with the IC₅₀ of 65 μM. 7-Hydroxyflavanone exerts various biological effects, including anticarcinogenic, antioxidant and (anti-)estrogenic effects, and modula

Dexfadrostat ((R)-Fadrozole) is an orally active and selective aromatase inhibitor, with human aromatase IC₅₀ values of 6.4 nM. Dexfadrostat suppresses estrogen synthesis, reduces circulating estradiol levels and suppresses aldosterone production. Dexfadrostat can be used for the research of breast cancer, primary aldosteronism, and hypertension.

YM511 is a highly specific non-steroidal aromatase inhibitor. YM511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM511 slightly inhibits production of other steroid hormones. YM511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones.