Letrozole

Short Summary : Non-steroidal aromatase inhibitor

Category : Endocrinology and Hormones|Aromatase

Purity : 0.9966

CAS Number : 112809-51-5

Formula : C17H11N5

Molecular Weight : 285.3

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

Solubility : >14.3mg/mL in DMSO

Storage : Store at -20°C

Description : Letrozole is a novel and potent type (II) aromatase inhibitor with IC50 of 11.5 nM. It belongs to the reversible non-steroidal compound family which can inhibit Arom. However, there is no evidence that it can affect the adrenal steroidogenesis.[1]Normally, Type II inhibitors have a common feature of heterocyclic azole moiety, which can be binded to the hemeCiron in aromatase. It contains a structure of 1,2,4-triazole moieties which can coordinate the hemeCiron of cytochrome P450. Meanwhile, benzonitrile substituted letrozole can mimic a unique enzyme structure of the substrate androstenedione.[2]Letrozole administration can reduce spine synapse and axon outgrowth and it also will decrease the expression of estrogen receptor (ER ). While, the synaptic proteins including GAP-43 can impaire the long-termpotentiation.[1] Letrozole is proved to promote FSH release from the hypothalamic pituitary axis by responding to decreased estrogen (E) feedback.[3]References:[1] Chen Bian, Yangang Zhao, Qiang Guo, Ying Xiong, Wenqin Cai, Jiqiang Zhang. Aromatase inhibitor letrozole downregulates steroid receptor coactivator-1 in specific brain regions that primarily related to memory, neuroendocrine and integration. The Journal of Steroid Biochemistry and Molecular Biology. May 2014. 141: 37-43.[2] Hakki Trker Ak ay, Riza Bayrak. Computational studies on the anastrozole and letrozole, effective chemotherapy drugs against breast cancer. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy. 25 March 2014. 122: 142-152.[3] Lindsay Malloch, Alice Rhoton-Vlasak. An assessment of current clinical attitudes toward letrozole use in reproductive endocrinology practices. Fertility and Sterility. December 2013. 100(6): 1740-1744.

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