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  3. Fadrozole hydrochloride

Fadrozole hydrochloride (Synonyms: CGS 16949A)

製品番号: HY-14247 純度: 99.64%
取扱説明書

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

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Fadrozole hydrochloride 構造式

Fadrozole hydrochloride 構造式

CAS 番号 : 102676-31-3

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 55 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 80 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 156 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 276 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 492 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Fadrozole hydrochloride:

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製品説明

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]

体外実験

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].

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

体内実験

Fadrozole hydrochloride is able to inhibit the aromatase-mediated 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 accompanies 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].

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

分子量

259.73

分子式

C₁₄H₁₄ClN₃

CAS 番号

102676-31-3

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.01 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.01 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.01 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
動物実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

FadrozoleCGS 16949AAromataseInhibitorinhibitorinhibit

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製品名:
Fadrozole hydrochloride
製品番号:
HY-14247
数量:
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