Fig. 1 · Structure

Cat. No.: A11088
CAS No.: 102676-47-1
Formula: C₁₄H₁₃N₃
Mol. Weight: 223.27

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Fadrozole

Name: Fadrozole
Brand: Adooq Bioscience
SKU: A11088
Availability: InStock
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Cat. No. A11088 CAS 102676-47-1

Aromatase inhibitor

Fadrozole is a nonsteroidal aromatase inhibitor exhibiting a very potent and selective inhibitory effect of the aromatase enzyme system in vivo and estrogen biosynthesis in vivo.

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Biological Activity

Bioactivity / Mechanism

Fadrozole directly inhibited aromatase activity in brain S9 fractions from 18 freshwater fish species. Reported IC50 values ranged from 0.0019 μM in American paddlefish to 0.10 μM in zebrafish. Most species were represented by one pooled tissue sample with technical triplicates, so these values describe the tested enzyme preparations and do not establish corresponding in vivo or human potency. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

In Vitro Studies

Species-dependent inhibition of fish brain aromatase

Biochemical assay · Composite brain post-mitochondrial supernatant (S9) from 18 freshwater fish species; adults or juveniles depending on species. [1]

Fadrozole inhibited aromatase concentration-dependently in all 18 species. IC50 values differed by more than 52-fold. Most species had one composite sample assayed once in triplicate technical wells; these are not independent animal replicates. Japanese medaka was additionally assessed using two independent composite pools. This is an enzyme activity experiment, not an in vivo treatment study.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Inhibition of aromatase activity in brain S9	IC50 (95% confidence interval) American paddlefish: 0.0019 (0.0016-0.0022) μM; lake sturgeon: 0.0020 (0.0016-0.0024) μM; fathead minnow: 0.082 (0.071-0.094) μM; zebrafish: 0.10 (0.096-0.11) μM	[1]

Literature-Reported Treatment Conditions

Treatment concentration: Concentration-response series; shared assay method states 0 to 300 μM of selected chemical across the tested inhibitor panel. This is not asserted as a fadrozole-specific upper concentration.
Exposure duration: 90 min
Method: In vitro incubation of brain S9 at 25°C; tritiated androstenedione aromatase activity assay.
Vehicle: Stocks prepared in methanol; final methanol fraction not specified in the read assay description.
Reported limits: Fadrozole-specific concentration grid and final solvent fraction are not enumerated in the read methods. The shared maximum is not a treatment recommendation.

Methods and source locations

Compound reported in the paper: Fadrozole; Compound label in the paper: Fadrozole (CAS 102676-47-1)

Fish enzyme activity only. IC50 values are assay endpoints, not exposure doses or human aromatase potency.

Materials and Methods: Dosing solutions, Aromatase activity assay and Data analysis; Results: Relative Species Sensitivity to Aromatase Inhibition by Fadrozole; Figure 1; Supplementary Tables S1 and S4

Inhibition of aromatase activity in brain S9: Tritiated water release from tritiated androstenedione; four-parameter logistic fit; three technical replicates per concentration. — Supplementary Table S4, Fadrozole column and footnote a; Figure 1A-C; Data analysis

In Vivo Studies

In adult zebrafish, 21-day waterborne exposure to nominal 0.1, 1 and 10 μg/L fadrozole reduced fertilization rate relative to dilution-water controls. Female plasma vitellogenin decreased significantly at 10 μg/L, while cumulative fertilized egg output was significantly reduced at 1 and 10 μg/L. No mortality occurred, and gonadal maturity-index changes were nonsignificant. The study reports Adooq-supplied fadrozole without identifying a catalog lot. [2]

Reproductive and vitellogenin responses in adult zebrafish

Animal study · Adult wild-type zebrafish (Danio rerio); 5 males and 5 females per vessel, four replicate vessels per concentration and dilution-water control. [2]

A 21-day water exposure reduced fertilization rate at all three concentrations and female plasma vitellogenin significantly at 10 μg/L. Cumulative fertilized egg output was significantly reduced at 1 and 10 μg/L. No mortality occurred. Gonadal maturity-index changes were nonsignificant. These endpoints support endocrine disruption under the tested conditions but do not directly measure aromatase catalytic inhibition.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Mean fertilization rate over 21-day exposure	Mean ± SEM 0, 0.1, 1 and 10 μg/L: 95.3 ± 0.6%, 88.3 ± 1.6%, 89.0 ± 2.5% and 54.7 ± 6.4%, respectively.	[2]
Female plasma vitellogenin normalized to protein	Mean ± SEM 0, 0.1, 1 and 10 μg/L: 211 ± 62.8, 192.9 ± 25.4, 88.4 ± 26.4 and 27.59 ± 10.5 μg VTG/mg protein, respectively.	[2]

Conditions shared by the study groups

Route: Waterborne
Frequency: Continuous flow-through exposure; SI section 1 describes five-fold daily water exchange.
Treatment course: 21 days
Vehicle: Water

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Fadrozole exposure series versus dilution-water control Nominal 0.1, 1.0 and 10.0 μg/L	Dilution-water control; four replicate vessels.	Fertilization rate decreased significantly at all three concentrations; female plasma VTG decreased significantly only at 10 μg/L. No mortality in controls or exposed groups. Maturity-index changes were nonsignificant.	[2]

Fadrozole exposure series versus dilution-water control: Model: Adult zebrafish; 10 fish per vessel (5 per sex), four vessels per condition.; Reported limits: No compound lot or explicit stereochemical composition given.

Methods and source locations

Compound reported in the paper: Fadrozole; Compound label in the paper: Adooq-supplied fadrozole; named neutral structure

Results apply to reported fadrozole exposure in zebrafish; supplier attribution does not validate current catalog lots.

Results: Effects of fadrozole on FSTRA endpoints and Vitellogenin measurement; Figure 1C-D; Materials and Methods: Test substance, Determination of FSTRA endpoints and Statistical analyses for FSTRA endpoints

Mean fertilization rate over 21-day exposure: Daily egg counts; four vessel replicates per condition. Dunnett comparisons: p < 0.01 at 0.1 and 1 μg/L; p < 0.0001 at 10 μg/L. — Results: Effects of fadrozole on FSTRA endpoints; Figure 1C; Statistical analyses for FSTRA endpoints

Female plasma vitellogenin normalized to protein: ELISA; two females sampled per vessel, four vessel replicates; fish values averaged within vessel. Significant only at 10 μg/L (p < 0.01). — Results: Vitellogenin measurement; Figure 1D and caption; Determination of FSTRA endpoints; Statistical analyses for FSTRA endpoints

Fadrozole exposure series versus dilution-water control · Results: Effects of fadrozole on FSTRA endpoints and Vitellogenin measurement; Figure 1C-D; Materials and Methods: Test substance, Determination of FSTRA endpoints and Statistical analyses for FSTRA endpoints; Supporting Manuscript section 1 (General exposure conditions)

Specifications

Manufacturer	Adooq Bioscience
Actions	Inhibitor
CAS Number	102676-47-1
Applications	Aromatase inhibitor
Formula	C₁₄H₁₃N₃
Molecular Weight	223.27
SMILES	C1CC(N2C=NC=C2C1)C3=CC=C(C=C3)C#N

Storage & Solubility

In Vitro Solubility

Reported Solubility

Solvent	Reported Solubility
DMSO	42 mg/mL (188.1 mM)
Water	Insoluble
Ethanol	42 mg/mL

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] Doering JA, Villeneuve DL, Fay KA, et al. Differential Sensitivity to In Vitro Inhibition of Cytochrome P450 Aromatase (CYP19) Activity Among 18 Freshwater Fishes. Toxicological sciences : an official journal of the Society of Toxicology (2019). PMID: 31099392 DOI: 10.1093/toxsci/kfz115 Source material
[2] Ayobahan SU, Eilebrecht E, Kotthoff M, et al. A combined FSTRA-shotgun proteomics approach to identify molecular changes in zebrafish upon chemical exposure. Scientific reports (2019). PMID: 31036921 DOI: 10.1038/s41598-019-43089-7 Source material

Publications

3 publications citing this product

Steve U. Ayobahan, .et al. , Sci Rep, 2019, 9, Article number: 6599 PMID: 31036921
Muth-Köhne E, .et al. , Aquat Toxicol, 2016, Jul;176:116-27 PMID: 27130971
Ma YN, .et al. , Aquat Toxicol, 2016, Oct;179:55-64 PMID: 27571716