Triticonazole (Synonyms:灭菌唑)
目录号 : KCM11033 CAS No. : 131983-72-7 纯度 : ≥95%
Triticonazole is a triazole fungicide used for the control of common soil and seed-borne diseases on cereals and other crops. The antifungal effects of triticonazole are due to its ability to inhibit ergosterol biosynthesis.
规格 价格 是否有货 数量
100mg
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生物活性

Triticonazole is an orally active triazole fungicide and androgen receptor antagonist. Triticonazole inhibits testosterone-induced androgen receptor activation and reduces basal testosterone secretion. Prenatal exposure to Triticonazole causes shortened anogenital distance in male rat fetuses and induces organ-specific histopathological changes in pigs. Triticonazole can be used for detoxification of seeds contaminated with fungal pathogens, but there is a risk of animal poisoning if the treated seeds are used as animal feed.

体外研究

Triticonazole (0.2-50 μM; 24 h) can effectively antagonize human androgen receptors in AR EcoScreen cells, with an IC50 of 0.3 μM; Non AR mediated luciferase activation was observed at concentrations of 25 μM and 50 μM, and no cytotoxicity was observed at all tested concentrations [1].

Triticonazole (0.78-50 μM; 48 h) can disrupt steroidogenesis in H295R cells by reducing pregnenolone and corticosteroid levels, increasing steroid levels at low doses and reducing them at 50 μ M, and increasing 17 α - hydroxyprogesterone levels at 12.5 μM without altering dehydroepiandrosterone (DHEA) levels. Triticonazole (10 μM; 48 h) can reduce the basal testosterone secretion of MA-10 testicular interstitial cells in mice by 44% after 48 hours of exposure [2].

Triticonazole (0.01-100 μM; 1-48 h) does not significantly alter the generation of reactive oxygen species in mouse MA-10 testicular interstitial cells under conditions of concentration up to 100 μM and exposure for up to 48 hours.

Triticonazole (100 pM-100 μM; 24 h) can concentration dependently inhibit testosterone induced androgen receptor activation in human T47D-ARE cells, with an IC50 of 10.7 μ M after 24 hours of exposure and a relative potency of 0.25 compared to Flutamide.

体内研究

Triticonazole (150-450 mg/kg/day; Oral administration; Daily; From the 7th day of pregnancy to the 21st day of pregnancy, it can induce a dose-dependent decrease in the distance between the anal and reproductive organs (AGD) and AGD index of male fetal rats in Sprague Dawley rats.
Triticonazole (200-2000 mg/kg; oral; A single dose can cause dose related gross and histopathological changes in multiple internal organs of Danube white pigs, including key lesions in the liver, kidneys, lungs, lymph nodes, and central nervous system.

 

Animal Model: Sprague-Dawley rats (Crl:CD(SD), time-mated dams, 10 weeks old at delivery, gestational exposure model)
Dosage: 150 mg/kg bw/day; 450 mg/kg bw/day
Administration: p.o.; daily; gestational day 7 to gestational day 21
Result: Reduced fetal male AGD by 10% in the 450 mg/kg bw group.
Reduced fetal male AGD index by 8% in the 450 mg/kg bw group.
Reduced fetal male AGD index by 4% in the 150 mg/kg bw group.
Did not significantly affect female AGD.
Caused no significant changes to measured fetal male plasma hormone levels (pregnenolone, progesterone, corticosterone, testosterone, androstenedione, estrone).
Detected no histopathological changes in fetal testes.
Reached fetal plasma concentrations of 5.26 μM at 150 mg/kg bw and 9.01 μM at 450 mg/kg bw at gestational day 21.
Reached amniotic fluid concentrations of 1.34 μM at 150 mg/kg bw and 2.98 μM at 450 mg/kg bw at gestational day 21.
 
分子式
C17H20ClN3O
分子量
317.81
CAS号
131983-72-7
中文名称
灭菌唑
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro:

DMSO : 100 mg/mL (314.65 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1465 mL 15.7327 mL 31.4653 mL
5 mM 0.6293 mL 3.1465 mL 6.2931 mL
10 mM 0.3147 mL 1.5733 mL 3.1465 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO → 90% corn oil

    Solubility: ≥ 5 mg/mL (15.73 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (15.73 mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中,混合均匀。

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