中文名 | FADROZOLE |
英文名 | FADROZOLE |
别名 | 法倔唑 AROMATASE抑制剂(FADROZOLE) 4-(5,6,7,8-四氢咪唑[1,5-A]吡啶-5-基)苯腈 4-(5,6,7,8-四氢咪唑并[1,5-Α]吡啶-5-基)苯腈 4-(5,6,7,8-四氢咪唑并[1,5-A]吡啶-5-基)苯腈 4-(5,6,7,8-四氢咪唑并[1,5-A]吡啶-5-基)苯甲腈 |
英文别名 | Afema FADROZOLE CGS-16949 Fadrozole Hydrochloride Hydrate 5,6,7,8-Tetrahydro-5-(4-cyanophenyl)imidazo[1,5-a]pyridine 4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridine-5-yl)benzonitrile 4-[[5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin]-5-yl]benzonitrile 4-[(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin)-5-yl]benzonitrile |
CAS | 102676-47-1 |
化学式 | C14H13N3 |
分子量 | 223.27 |
密度 | 1.20 |
熔点 | 0°C |
沸点 | 0°C |
闪点 | 0°C |
酸度系数 | 7.16±0.40(Predicted) |
存储条件 | 2-8°C |
物化性质 | 熔点117~118℃。盐酸法屈唑(Fadrozole Hydrochloride):C14H13N3?HCl。[102676-96-0]。从异丙醇结晶,熔点231--233℃。溶于水。 |
体外研究 | Fadrozole hydrochloride is a very potent inhibitor of both human placental and rat ovarian aromatase. In hamster ovarian slices, fadrozole hydrochloride inhibits the production of estrogen with an IC 50 of 0.03 μM. The production of progesterone is inhibited with an IC 50 of 120 μM. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of fadrozole hydrochloride. . |
体内研究 | Fadrozole hydrochloride is able to inhibit the aromatase-mediated androstenedione-induced uterine hypertrophy in immature female rats with an ED 50 of 0.03 mg/kg when given orally. In the same model, aminoglutethimide elicits the same effect with an ED 50 of 30 mg/kg when given orally. 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 dta mas in female rats, and reduces the of spontaneous hcu ar tumours in male and female rats. Administration of fadrozole 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 treatment returns these levels to baseline values. |
风险术语 | 20/21/22 - 吸入、皮肤接触及吞食有害。 |
安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 |
危险品运输编号 | 3439 |
上游原料 | 浓硫酸 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.479 ml | 22.394 ml | 44.788 ml |
5 mM | 0.896 ml | 4.479 ml | 8.958 ml |
10 mM | 0.448 ml | 2.239 ml | 4.479 ml |
5 mM | 0.09 ml | 0.448 ml | 0.896 ml |
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