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  3. Fadrozole hydrochloride

Fadrozole hydrochloride (Synonyms: CGS 16949A)

Cat. No.: HY-14247 Purity: 99.64%
Handling Instructions

Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.

For research use only. We do not sell to patients.

Fadrozole hydrochloride Chemical Structure

Fadrozole hydrochloride Chemical Structure

CAS No. : 102676-31-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
25 mg USD 156 In-stock
Estimated Time of Arrival: December 31
50 mg USD 276 In-stock
Estimated Time of Arrival: December 31
100 mg USD 492 In-stock
Estimated Time of Arrival: December 31
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Description

Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.

IC50 & Target

IC50: 6.4 nM (aromatase)[1]

In Vitro

Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM. In hamster ovarian slices, Fadrozole hydrochloride inhibits the production of estrogen with an IC50 of 0.03 μM. The production of progesterone is inhibited with an IC50 of 120 μM. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of Fadrozole hydrochloride[1].

In Vivo

Fadrozole hydrochloride is able to inhibit the aromatase-mediated androstenedione-induced uterine hypertrophy in immature female rats with an ED50 of 0.03 mg/kg when given orally. In the same model, aminoglutethimide elicits the same effect with an ED50 of 30 mg/kg when given orally[1]. Fadrozole hydrochloride prevents the development of both benign and malignant spontaneus mammary neoplasns in female Sprague-Dawley rats. It also slows the spontaneous development of ptuitary pars distalis adenomas in female rats, and reduces the incidence of spontaneous hepatocellular tumours in male and female rats[2]. Administration of Fadrozole hydrochloride in male and female mice suppresses the production of 17b-estradiol, accompanied with a 70% reduction in parasite burden. This protective effect is associated in male mice with a recovery of the specific cellular immune response. Interleukin-6 (IL-6) serum levels, and its production by splenocytes, is augmented by 80%, together with a 10-fold increase in its expression in testes of infected male mice. Fadrozole hydrochloride treatment returns these levels to baseline values[3].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (385.02 mM; Need ultrasonic and warming)

H2O : 100 mg/mL (385.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8502 mL 19.2508 mL 38.5015 mL
5 mM 0.7700 mL 3.8502 mL 7.7003 mL
10 mM 0.3850 mL 1.9251 mL 3.8502 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2][3]

Rats: Rats are treated with daily dosing with Fadrozole hydrochloride in purified water by gavage for 2 years. There are 60 rats in each of four groups given 0, 0.05, 0.25 or 1.25 mg/kg daily. Control rats receive only water. Clinical signs are recorded weekly and the animals are examined for palpable masses every 4 weeks for the first 9 months, then every 2 weeks for the remainder of the study[2].

Mice: Fadrozole hydrochloride is administered in the form of sub-dermal long-term release pellets (20 mg/wt kg, in three-week-release pellets), starting 1 week prior to the infection, using a 10-gauge needle. Three pellets are administrated during the study. Placebo pellets are administered to another group of infected mice, in the same fashion as the inhibitor. After 1 week, mice are infected and killed 8 weeks later[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

259.73

Formula

C₁₄H₁₄ClN₃

CAS No.

102676-31-3

SMILES

N#CC1=CC=C(C2CCCC3=CN=CN23)C=C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Fadrozole hydrochloride
Cat. No.:
HY-14247
Quantity:

Fadrozole hydrochloride

Cat. No.: HY-14247