2. 疾病领域
  3. 消化系统疾病
  4. 肝脏疾病
  5. 肝毒性
  6. Fluindarol

Fluindarol 是一种茚满二酮衍生物和具有口服活性的抗凝剂。Fluindarol 是一种毒物，可在大鼠中诱发器官和组织出血以及肝实质坏死。Fluindarol 在大鼠、家兔和犬中表现出急性和累积性临床前毒性，且雌性大鼠的毒性高于雄性大鼠。Fluindarol 无镇痛作用，仅会产生轻微的血压影响，且不会改变循环、呼吸、中枢神经系统 (CNS) 或心脏活动。基于临床前数据，Fluindarol 被认为毒性过高，不适于临床应用。

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Fluindarol

Fluindarol Chemical Structure

CAS No. : 6723-40-6

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Fluindarol 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fluindarol is a phenylindandione derivative and an orally active anticoagulant. Fluindarol acts as a toxicant that induces organ and tissue haemorrhages and liver parenchymal necrosis in rats. Fluindarol exhibits acute and cumulative preclinical toxicity in rats, rabbits, and dogs, with higher toxicity in female rats than male rats. Fluindarol lacks analgesic action, produces only minor blood pressure effects, and does not alter circulation, respiration, CNS, or cardiac activity. Fluindarol is considered too toxic for clinical use based on preclinical data[1].

体内研究
(In Vivo)

Fluindarol (100-350 mg/kg；口服；单次给药) 在白化 Wistar TNO 大鼠中的急性口服 LD50 为 198 mg/kg，雌性动物的死亡率更高[1]。
Fluindarol (100-200 mg/kg；腹腔注射；单次给药) 在白化 Wistar TNO 大鼠中的急性腹腔注射 LD50 为 125 mg/kg，雌雄动物的死亡率无差异[1]。
Fluindarol (单剂量口服) 在家兔中的急性口服 LD50 为 123 mg/kg，未存活动物出现夜间猝死[1]。
Fluindarol (2810 mg/kg；口服；单次给药) 不会导致杂种犬死亡，但会引发胃肠道不适和活动减少[1]。
Fluindarol (口服；每日 1 次；连续 4 天) 在杂种犬中连续 4 天给药后的累计口服 LD50 为 118 mg/kg，可引发嗜睡、厌食、严重失血及器官充血[1]。
Fluindarol (7-108 mg/kg；口服；每日 1 次；连续 28 天) 会在白化 Wistar TNO 大鼠中引发剂量依赖性死亡 (雌性大鼠死亡率更高)、严重贫血、器官出血及肝脏坏死，所有测试剂量组的总死亡率达 76 只动物中有 47 只死亡[1]。
Fluindarol (13.5-54 mg/kg；口服；每日 1 次；连续 28 天) 会在白化 Wistar TNO 大鼠中引发剂量依赖性死亡、血液学异常和肝坏死，在 54 mg/kg 剂量下，大鼠在 12 天内的死亡率达 100%[1]。
Fluindarol (35 mg/kg；口服；每日 1 次；连续 10 天) 可导致白化 Wistar TNO 大鼠出现 40%的死亡率[1]。

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

Animal Model: Albino Wistar TNO rat (young males and females, weight 90-120 g)[1]
Dosage: 100 mg/kg; 350 mg/kg
Administration: p.o.; single dose
Result: Determined acute oral LD50 as 198 mg/kg (95% confidence limits 161-244).
Determined acute oral LD10 as 100 mg/kg (95% confidence limits 73-160).
Observed greater mortality in female animals, with highest mortality on the 3rd day after administration and no deaths on the final 4 days of observation.
Animal Model: Albino Wistar TNO rat (young males and females, weight 90-120 g)[1]
Dosage: 100 mg/kg; 200 mg/kg
Administration: i.p.; single dose
Result: Determined acute intraperitoneal LD50 as 125 mg/kg (95% confidence limits 117-134).
Determined acute intraperitoneal LD10 as 113 mg/kg (95% confidence limits 103-124).
Observed no difference in mortality between males and females, with death occurring on the 1st and 2nd day after administration.
Animal Model: Mongrel dog (weight 3.5-10.7 kg)[1]
Dosage: 2810 mg/kg
Administration: p.o.; single dose
Result: Observed no mortality occurred.
Observed dogs exhibited vomiting, anorexia, blood-stained mucus in feces, and inactivity.
Animal Model: Albino Wistar TNO rat (males and females, starting weight 112-154 g [females], 140-199 g [males] in Experiment I; 76-101 g [females], 90-121 g [males] in Experiment II)[1]
Dosage: 108 mg/kg; 54 mg/kg; 27 mg/kg; 28 mg/kg; 14 mg/kg; 7 mg/kg
Administration: p.o.; once daily; 28 days
Result: Observed total mortality across all dose groups as 47 out of 76 rats, with females dying sooner and in greater numbers than males.
Observed clinical signs including blindness, white ears, shallow/irregular respiration, and weakness.
Detected severe anemia (erythrocyte counts <1 million/mm3 in some rats), reduced hemoglobin content, increased blood urea nitrogen levels, and burr-shaped erythrocytes in highest-dose groups via blood tests.
Identified extensive hemorrhages in subcutaneous tissue and organs, and liver parenchymal cell damage, necrosis, and inflammatory foci via post-mortem analysis, with severity and incidence increasing with dose.
Animal Model: Albino Wistar TNO rat (males and females)[1]
Dosage: 54 mg/kg; 27 mg/kg; 13.5 mg/kg
Administration: p.o.; once daily; 28 days
Result: Observed all rats receiving 54 mg/kg died within 12 days.
Observed 80% of rats receiving 27 mg/kg died within 28 days.
Observed 50% of rats receiving 13.5 mg/kg died within 28 days.
Observed clinical signs including weight loss 1-2 days before death, blindness, white ears/extremities, nasal/urinary blood loss, and weakness.
Detected anemia, reduced hemoglobin, increased blood urea nitrogen levels (up to 180 mg% in 27 mg/kg group), presence of myeloblasts, erythroblasts, multinucleated polynuclear erythroblasts, and burr-shaped erythrocytes, and rapid rises in SGPT and alkaline phosphatase values preceding death via blood tests.
Identified widespread organ hemorrhages, frequent haemothorax, and dose-related liver necrosis (highest incidence and severity in highest-dose groups) via post-mortem analysis.
Animal Model: Albino Wistar TNO rat (males and females, weight 90-120 g [females], 110-135 g [males])[1]
Dosage: 35 mg/kg
Administration: p.o.; once daily; 10 days
Result: Observed fluindarol caused death in 8 out of 20 rats (40% mortality) over the 10-day period.
分子量

290.24

Formula

C16H9F3O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Fluindarol 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fluindarol6723-40-6Othersorgan haemorrhagesdogsmongrel dogscumulative toxicityacute toxicityrabbitsratsliver parenchymal necrosistame rabbitsalbino Wistar TNO ratsInhibitorinhibitorinhibit

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