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    Dutasteride (GG 745; GI 198745)
    Dutasteride (GG 745; GI 198745)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1808
    CAS #: 164656-23-9Purity ≥98%

    Description: 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.

    References: Curr Top Med Chem. 2006;6(5):405-21.

    Related CAS#: 164656-22-8 (Dihydro Dutasteride); 957229-52-6 (5β-Dutasteride)

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    Molecular Weight (MW)528.53
    FormulaC27H30F6N2O2
    CAS No.164656-23-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 62 mg/mL (117.3 mM)
    Water: <1 mg/mL
    Ethanol: 6 mg/mL (11.4 mM)
    Other InfoChemical 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
    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
    SMILES Code: C[[email protected]]12CCC3[[email protected]@H](CC[[email protected]@H]4[[email protected]]3(C)C=CC(N4)=O)[[email protected]@H]1CC[[email protected]@H]2C(NC(C=C(C=C5)C(F)(F)F)=C5C(F)(F)F)=O
    SynonymsGI-198745, GG-745; GI198745, GG745; GI 198745, GG 745; LS-173584; LS 173584; LS173584; trade names: Avodart; Avidart; Avolve; Duagen; Dutas; Dutagen; Duprost.


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    In Vitro

    In vitro activity: Dutasteride inhibits type-1 5AR and type-2 5AR with IC50 of 6 nM and 7 nM, respectively. Dutasteride is 60-fold more potent than Finasteride in its initial Ki versus type 1 5AR and ~5-fold more rapid in inactivating the enzyme. Dutasteride inhibits (3)H-T conversion to (3)H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation in LNCaP cells. Dutasteride also inhibits DHT-induced PSA secretion and cell proliferation with IC50 of 1 μM in LNCaP cells. Dutasteride competes for binding the LNCaP cell AR with an IC50 of 1.5 μM. Dutasteride (10–50 μM) results in enhanced cell death, possibly by apoptosis, in steroid-free medium. Dutasteride reduces cell viability and cell proliferation in androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer(PCa) cell lines. Dutasteride results in overexpressed genes included genes encoding for proteins involved in biosynthesis and metabolism of androgen (HSD17B1;HSD17B3;CYP11B2), androgen receptor and androgen receptor co-regulators (AR;CCND1), and signal transduction(ERBB2; V-CAM; SOS1) whereas, underexpressed genes (KLK3; KLK2; DHCR24) are androgen-regulated genes (ARGs) in androgen-responsive (LNCaP) cell. Dutasteride inhibits FASN mRNA, protein expression and enzymatic activity in prostate cancer cells.


    Kinase Assay: Dutasteride (GG745) is a potent inhibitor of both 5 alpha-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT. IC50 Value: Target: 5 alpha-reductase 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. 


    Cell Assay: Dutasteride has been reported to inhibit conversion of 3H-testosterone to 3H-DHT by more than 99% in LNCaP cells. Dutasteride 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.

    In VivoDutasteride (100 mg/kg/day) has prostates about half as large as those in intact male rats treated with vehicle alone. Dutasteride is orally bioavailable and because of its mechanism of action it easily overcomes the potential liability of being >99% plasma protein bound.
    Animal model Rats
    Formulation & Dosage 100 mg/kg
    ReferencesCurr Top Med Chem. 2006;6(5):405-21.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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