Cgp 47645 - CAS 143030-47-1
Catalog number: 143030-47-1
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Cgp 47645 is non-steroidal aromatase inhibitor with anti-tumor and endocrine effects. It is orally active.
Cgp 47645; Cgp47645; Cgp-47645; Leflutrozole; UNII-RCX0IE6EJZ;4,4'-(fluoro-1H-1,2,4-triazol-1-ylmethylene)bis-Benzonitrile
Soluble in DMSO
-20°C Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
1.Effect of long-term treatment with aromatase inhibitor on testicular function of adult male bonnet monkeys (M. radiata).
Shetty G;Krishnamurthy H;Krishnamurthy HN;Bhatnagar AS;Moudgal NR Steroids. 1998 Jul-Aug;63(7-8):414-20.
The role/need for estrogen in regulating testicular function of adult male bonnet monkeys (M. radiata) has been investigated by dosing orally a group of five normal males 2.5 mgs of CGP 47645, a long-acting nonsteroidal aromatase inhibitor (AI), once every 5 days for over 150 days. Such treatment resulted in a 10-fold increment in nocturnal serum testosterone (T) levels, which were sustained for 85 days of treatment, and a twofold increment in basal serum T levels was present throughout the 150 days of treatment. Analysis of ejaculated semen showed a marked reduction (approximately 90%) in sperm counts in four out of five monkeys between Days 55-85 of treatment. During this period, the motility score also was markedly reduced from a normal score of 3-5 to 0-2. Flow cytometric analysis of testicular germ cells obtained from biopsy tissue taken on Days 63 and 120 indicated a marked reduction only in elongating/elongated spermatid population (compared to Day 0 values), suggesting inhibition in spermiogenic process. Epididymal sperm maturation also seemed effected as sperm chromatin, on flow cytometric analysis for decondensability following exposure to 5 mM dithiotreitol, showed to be in a hypercondensed state.
2.Effect of estrogen deprivation on the reproductive physiology of male and female primates.
Shetty G;Krishnamurthy H;Krishnamurthy HN;Bhatnagar S;Moudgal RN J Steroid Biochem Mol Biol. 1997 Apr;61(3-6):157-66.
The availability of CGS 16949A, CGS 20267 and CGP 47645, a series of aromatase inhibitors (AIs) having high specific activity and specificity, made possible this study wherein the need for estrogen (E) for regulating (a) follicular maturation/ovulation, luteal function and pregnancy establishment, and (b) testicular function of the bonnet monkey (Macaca radiata) has been examined. Generally these compounds, used in the range of 500 microg to 2.5 mg/day did not inhibit follicular maturation although they did reduce E levels. Although low doses had no effect on ovulation it appears that relatively high doses of CGS 20267 and CGP 47645 could be inhibiting it. Three oral doses of letrozole (CGS 20267, each dose of 2 mg) during the follicular phase resulted in the formation of multiple follicles in cycling females, and these could be ovulated by exogenous hCG (1000 IU) treatment. Although administration of AI during the early luteal phase had no effect on progesterone (P) production, it prevented pregnancy establishment. Whereas AI administration in the female had no significant effect on luteinizing hormone (LH) and follicle stimulating hormone (FSH) levels (except at high drug dosages), it significantly increased serum testosterone (T) levels in the male.
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