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AB141293

Letrozole, Aromatase inhibitor

Letrozole, Aromatase inhibitor

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MW 285.3 Da, Purity >99%. Highly potent, reversible, selective aromatase inhibitor (IC50 = 11.5 nM). Inhibits estradiol synthesis. Potent antitumor effects in vivo. Cytochrome P450 inhibitor.

別名を表示する

1,8-cineole 2-exo-monooxygenase, ALDOS, ARO, ARO1, Albendazole monooxygenase, Albendazole sulfoxidase, Aldosterone synthase, Aldosterone-synthesizing enzyme, Aromatase, C11B2_HUMAN, CP19A_HUMAN, CP33, CP34, CP3A4_HUMAN, CPV1, CYAR, CYP11B, CYP11B2, CYP19, CYP3, CYP3A, CYP3A3, CYP3A4, CYPIIIA3, CYPIIIA4, CYPXIB1, CYPXIB2, CYPXIX, Cyp19a1, Cytochrome P 450c11, Cytochrome P-450AROM, Cytochrome P-450Aldo, Cytochrome P-450C18, Cytochrome P450 11B1, mitochondrial, Cytochrome P450 11B2, Cytochrome P450 11B2, mitochondrial, Cytochrome P450 19A1, Cytochrome P450 3A3, Cytochrome P450 3A4, Cytochrome P450 HLp, Cytochrome P450 NF-25, Cytochrome P450 family 3 subfamily A polypeptide 4, Cytochrome P450 subfamily IIIA polypeptide 4, Cytochrome P450, family 11, subfamily B, polypeptide 1, Cytochrome P450, family 19, subfamily A, polypeptide 1, Cytochrome P450, subfamily XIB (steroid 11 beta hydroxylase), polypeptide 1, Cytochrome P450, subfamily XIB, polypeptide 1, Cytochrome P450, subfamily XIX (aromatization of androgens), Cytochrome P450-PCN1, Cytochrome p450 XIB1, Estrogen synthase, Estrogen synthetase, FHI, Glucocorticoid inducible P450, HLP, MGC104309, MGC126680, Microsomal monooxygenase, NF 25, Nifedipine oxidase, OTTHUMP00000162543, OTTHUMP00000198350, P 450AROM, P 450C11, P-450Aldo, P-450C18, P450 III steroid inducible, P450 PCN1, P450, family III, P450C3, Quinine 3-monooxygenase, S11BH, Steroid 11 beta hydroxylase, Steroid 11 beta monooxygenase, Steroid 18-hydroxylase, Taurochenodeoxycholate 6-alpha-hydroxylase, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 3, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4, flavoprotein-linked monooxygenase, mitochondrial

1 Images
Chemical Structure - Letrozole, Aromatase inhibitor (AB141293)
  • Chemical Structure

Lab

Chemical Structure - Letrozole, Aromatase inhibitor (AB141293)

2D chemical structure image of ab141293, Letrozole, Aromatase inhibitor

Key facts

CAS番号

112809-51-5

精製度

>99%

製品の状態

Solid

form

分子量

285.3 Da

分子式

C<sub>1</sub><sub>7</sub>H<sub>1</sub><sub>1</sub>N<sub>5</sub>

PubChem

3902

由来

Synthetic

化学名

Letrozole

生物学的記述

Highly potent, reversible, selective aromatase inhibitor (IC50 = 11.5 nM). Inhibits estradiol synthesis. Potent antitumor effects in vivo. Cytochrome P450 inhibitor.

Canonical smiles

C1=CC(=CC=C1C#N)C(C2=CC=C(C=C2)C#N)N3C=NC=N3

InChi

InChI=1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H

InChiKey

HPJKCIUCZWXJDR-UHFFFAOYSA-N

IUPAC名

4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile

出荷温度及び保存条件

出荷温度
Ambient - Can Ship with Ice
短期保存温度
+4°C
長期保存温度
+4°C
保管に関する情報
The product can be stored for up to 12 months

補足情報

This supplementary information is collated from multiple sources and compiled automatically.

Cytochrome P450 3A4 commonly referred to as CYP3A4 is an important enzyme within the cytochrome P450 family. It catalyzes the oxidation of small organic molecules in the liver affecting drug metabolism. CYP3A4 has a molecular weight of about 57 kDa and expresses primarily in the liver and intestines. Aromatase also known as CYP19A1 plays an important role in estrogen biosynthesis by converting androgens to estrogens. Meanwhile CYP11B1 and CYP11B2 are involved in corticosteroid biosynthesis pathways with expression in the adrenal cortex.
Biological function summary

Enzymes like CYP3A4 and aromatase significantly impact steroid metabolism and drug clearance in humans. Aromatase is part of the aromatase complex which includes NADPH-cytochrome P450 reductase facilitating its function in hormone synthesis. CYP11B1 and CYP11B2 participate in corticoid and mineralocorticoid production influencing various physiological processes. These enzymes regulate hormone levels ensuring homeostasis and influencing responses to pharmacological treatments such as those involving aromatase inhibitors.

Pathways

Enzymes like CYP3A4 are vital in the cytochrome P450-mediated drug metabolism pathway and participate in the steroid hormone biosynthesis pathway. Aromatase connects to estrogen biosynthesis interacting with proteins such as CYP17A1 further linking to the biosynthesis of sex steroids. Both cytochrome P450 pathways and steroid hormone biosynthesis pathways contribute to physiological homeostasis and drug efficacy interacting with compounds like letrozole a well-known aromatase inhibitor.

CYP3A4 and related enzymes like aromatase have implications in drug interactions and hormone-related cancers such as breast cancer. Aromatase inhibitors including letrozole are important in treating hormone-receptor-positive breast cancer by reducing estrogen levels. Disorders related to corticosteroid biosynthesis involve CYP11B1 and CYP11B2 with links to conditions like congenital adrenal hyperplasia and hypertension. The enzyme interactions involved such as those between aromatase and its inhibitors highlight the therapeutic potential in managing hormone-dependent conditions.

製品プロトコール

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