| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Dutasteride (also known as GI198745, GG-745; trade names: Avodart, Avidart) is a potent dual 5-α reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT). Dutasteride inhibited conversion of 3H-testosterone to 3H-DHT by more than 99% in LNCaP cells.It can also strongly reduces growth, proliferation, and viability of LNCaP cells as well. Dutasteride increased the enzymatic activities of caspase 7 and caspase 8 dose-dependently at 48 hours, providing functional significance and confirming that the apoptotic and survival pathways are being activated by dutasteride treatment in LNCaP cells.
| ln Vitro |
As expected, dutasteride prevents the conversion of 3H-T to 3H-DHT and T-induced PSA production and proliferation. Nevertheless, the medication also prevented cell division and PSA secretion triggered by DHT (IC50 = 1 μM)[1]. Dutasteride has an IC50 of about 1.5 μM and competes with LNCaP cell AR binding. Elevated levels of dutasteride (10-50 μM) in steroid-free media led to increased cell death, potentially through apoptosis, but not finasteride[1]. In both of the studied cell lines for androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer (PCa), dutasteride decreases cell viability and proliferation [2].
|
||
|---|---|---|---|
| ln Vivo |
With a terminal half-life of almost 240 hours, GG745 considerably reduced DHT levels in single doses more than 10 mg, compared to finasteride single doses of 5 mg[3]. Using doubled results to account for dutasteride treatment, there was an 8.3% median increase in PSA in men without prostate cancer who were treated with a placebo at month 24, compared to -59.5% in those who got the medication[4]. Toxicity: The dynamics of steroid hormones and male fertility may be impacted by dutasteride. In order to ascertain the impact of dutasteride (10, 32, and 100 μg/L) on fish reproduction, a 21-day reproduction research was carried out. Fish exposed to dutasteride saw a considerable reduction in fecundity and experienced various effects on their reproductive endocrine systems, affecting both male and female fish[5].
|
||
| Animal Protocol |
|
||
| References |
[1]. Lazier CB, et al. Dutasteride, the dual 5alpha-reductase inhibitor, inhibits androgen action and promotes cell death in the LNCaP prostate cancer cell line. Prostate. 2004 Feb 1;58(2):130-44.
[2]. Biancolella M, et al. Effects of dutasteride on the expression of genes related to androgen metabolism and related pathway in human prostate cancer cell lines. Invest New Drugs. 2007 Oct;25(5):491-7. [3]. Bramson HN, et al. Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR. J Pharmacol Exp Ther. 1997 Sep;282(3):1496-502. [4]. Andriole GL, et al. Clinical usefulness of serum prostate specific antigen for the detection of prostate cancer is preserved in men receiving the dual 5alpha-reductase inhibitor dutasteride. J Urol. 2006 May;175(5):1657-62. [5]. Margiotta-Casaluci L, et al. Mode of action of human pharmaceuticals in fish: the effects of the 5-alpha-reductase inhibitor, dutasteride, on reproduction as a case study. Aquat Toxicol. 2013 Mar 15;128-129:113-23. |
| Molecular Formula |
C27H30F6N2O2
|
|---|---|
| Molecular Weight |
528.53
|
| CAS # |
164656-23-9
|
| Related CAS # |
Dutasteride-13C6;1217685-27-2
|
| SMILES |
C[C@]12CCC3[C@@H](CC[C@@H]4[C@]3(C)C=CC(N4)=O)[C@@H]1CC[C@@H]2C(NC(C=C(C=C5)C(F)(F)F)=C5C(F)(F)F)=O
|
| InChi Key |
JWJOTENAMICLJG-VYZSUTEISA-N
|
| InChi Code |
InChI=1S/C27H30F6N2O2/c1-24-11-9-17-15(4-8-21-25(17,2)12-10-22(36)35-21)16(24)6-7-19(24)23(37)34-20-13-14(26(28,29)30)3-5-18(20)27(31,32)33/h3,5,10,12-13,15-17,19,21H,4,6-9,11H2,1-2H3,(H,34,37)(H,35,36)/t15-,16-,17?,19+,21+,24-,25+/m0/s1
|
| Chemical Name |
(4aR,6aS,7S,9aS,9bS,11aR)-N-(2,5-bis(trifluoromethyl)phenyl)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide
|
| Synonyms |
GI-198745, GG-745; GI198745, GG745; GI 198745, GG 745; LS-173584; LS 173584; LS173584; trade names: Avodart; Avidart; Avolve; Duagen; Dutas; Dutagen; Duprost.
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8920 mL | 9.4602 mL | 18.9204 mL | |
| 5 mM | 0.3784 mL | 1.8920 mL | 3.7841 mL | |
| 10 mM | 0.1892 mL | 0.9460 mL | 1.8920 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA