Dutasteride |
(5alpha,17beta)-N-{2,5-Bis(trifluoromethyl)phenyl}-3-oxo-4-azaandrost-l-ene-17-carboxamide |
(CAS 164656-23-9) |
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Description: |
Description:
IC50 Value: N/A
Dutasteride(GG745) is a potent inhibitor of both 5alpha-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
in vitro: Dutasteride inhibited (3)H-T conversion to (3)H-DHT and, as anticipated, inhibited T-induced secretion of PSA and proliferation. However the drug also inhibited DHT-induced PSA secretion and cell proliferation (IC(50) approximately 1 microM). Dutasteride competed for binding the LNCaP cell AR with an IC(50) approximately 1.5 microM. High concentrations of dutasteride (10-50 microM), but not finasteride, in steroid-free medium, resulted in enhanced cell death, possibly by apoptosis. Dutasteride reduces cell viability and cell proliferation in both cell lines tested (androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer (PCa))
in vivo: GG745 has a terminal half-life of approximately 240 hr, and single doses of >10 mg decreased DHT levels significantly more than did single 5-mg doses of finasteride. In placebo treated men without prostate cancer there was an 8.3% median increase in PSA at month 24 compared with -59.5% in those who received dutasteride, using doubled values to correct for dutasteride treatment.
Toxicity: Dutasteride may affect male fertility and steroid hormone dynamics. Therefore, a 21-day reproduction study was conducted to determine the effects of dutasteride (10, 32 and 100 μg/L) on fish reproduction. Exposure to dutasteride significantly reduced fecundity of fish and affected several aspects of reproductive endocrine functions in both males and females .
Clinical trial: Bioequivalence Study Of Dutasteride Five 0.1 mg And One 0.5 mg Soft Gelatin Capsules In Healthy Male Volunteers. Phase 1
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Product No. |
KT20493 |
Product Name |
Dutasteride |
Synonyms |
Avodart; Avolve; GG 745; GI 198745 |
Formal Name |
(5alpha,17beta)-N-{2,5-Bis(trifluoromethyl)phenyl}-3-oxo-4-azaandrost-l-ene-17-carboxamide |
CAS Number |
164656-23-9 |
Molecular Formula |
C27H30F6N2O2 |
Formula Weight |
528.53 |
Formulation |
A crystalline solid |
Purity |
98%min |
Stability |
2 years |
Storage |
-20°C |
Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500 |
Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
Price & Availability |
In Stock. Price Negotiated. |
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