Cgp 47645 - CAS 143030-47-1
Catalog number: 143030-47-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C17H10FN5
Molecular Weight:
303.30
COA:
Inquire
Targets:
Aromatase
Description:
Cgp 47645 is non-steroidal aromatase inhibitor with anti-tumor and endocrine effects. It is orally active.
Purity:
98%
Appearance:
Powder
Synonyms:
Cgp 47645; Cgp47645; Cgp-47645; Leflutrozole; UNII-RCX0IE6EJZ;4,4'-(fluoro-1H-1,2,4-triazol-1-ylmethylene)bis-Benzonitrile
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
anti-tumor
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
PZDLRBUQYWMNBR-UHFFFAOYSA-N
InChI:
1S/C17H10FN5/c18-17(23-12-21-11-22-23,15-5-1-13(9-19)2-6-15)16-7-3-14(10-20)4-8-16/h1-8,11-12H
Canonical SMILES:
c1cc(ccc1C#N)C(c2ccc(cc2)C#N)(n3cncn3)F
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Aromatase Products


CAS 125-84-8 Aminoglutethimide

Aminoglutethimide
(CAS: 125-84-8)

Aminoglutethimide is an anticancer drug that belongs to the family of drugs called nonsteroidal aromatase inhibitors. Aminoglutethimide is used to decrease the ...

CAS 115575-11-6 Liarozole

Liarozole
(CAS: 115575-11-6)

This active molecular has a potential antineoplastic activity. As a retinoic acid metabolism blocking agent (RAMBA), liarozole inhibits P450-dependent ATRA-4-hy...

CAS 566-48-3 Formestane

Formestane
(CAS: 566-48-3)

Formestane is a second generation selective aromatase inhibitor with an IC50 of 80 nM.

CAS 99957-90-1 Org30958

Org30958
(CAS: 99957-90-1)

ORG 30958 is a potent aromatase inhibitor in vivo. ORG 30958 proved to be devoid of antiestrogenic activity which indicates that the absence of cornification of...

FR 901537
(CAS: 161162-21-6)

FR-901537, a naphthothiazin compound, has been found to be an aromatase inhibitor that could be used as a cytostatic antibiotic and was once studied in breast c...

CAS 148869-05-0 YM 511

YM 511
(CAS: 148869-05-0)

YM 511 is a potent aromatase (CYP19) inhibitor (IC50 = 0.4 and 0.12 nM at rat ovary and human placenta cells, respectively) that weakly inhibits the synthesis o...

LY 43578
(CAS: 26766-35-8)

LY 43578 is an aromatase inhibitor.

Cgp 45688
(CAS: 134520-88-0)

Cgp 45688 is an non-steroidal aromatase inhibitor originated byNovartis. It has anti-tumor effects, but no development for treatment of cancer was reported.

Quick Inquiry

Verification code

Featured Items