2. Membrane Transporter/Ion Channel
  3. NKCC
  4. Triflocin

Triflocin 是一种具有口服活性的利尿剂、Na+-K+-2Cl− 协同转运抑制剂，其 IC50 为 3×10-5 M。Triflocin 抑制近端小管中向外的基底侧电致 Na-(HCO3)n>1 协同转运。Triflocin 不具有引发高血糖的倾向，其升高血糖的作用极其微弱，以至于必须借助葡萄糖负荷等特殊条件，方能检测到血糖水平的升高。Triflocin 更倾向于引发低血糖。

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Triflocin

Triflocin Chemical Structure

CAS No. : 13422-16-7

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Triflocin 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

Triflocin is an orally active diuretic and Na+-K+-2Cl− cotransporter inhibitor with an IC50 of 3×10-5 M. Triflocin inhibits the outward basolateral electrogenic Na-(HCO3) n>1 cotransport in the proximal tubule. Triflocin has no tendency to induce hyperglycemia, and its blood glucose-elevating effect is extremely weak, such that an increase in blood glucose levels can only be detected under special conditions such as glucose loading. Triflocin is more prone to induce hypoglycemia[1][2].

体外研究
(In Vitro)

Triflocin 在粗升支中可抑制 Na-K-2Cl 同向转运，其 IC50 值为 3 × 10⁻⁵ M[1]。
Triflocin 对细胞内氯离子活性无影响[1]。

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

Triflocin 相关抗体:
体内研究
(In Vivo)

Triflocin (10-400 mg/kg；口服；单次) 对非禁食雄性 Wistar 大鼠产生剂量依赖性的血糖影响，在 10 mg/kg (6-hour time point) 和 400 mg/kg (2, 4, 6-hour time points) 时出现显著低血糖，在 50 mg/kg (4-hour time point) 时出现显著高血糖[2]。
Triflocin (10-400 mg/kg；口服；单次；葡萄糖负荷前 2 小时) 可在禁食雄性 Wistar 大鼠中，于 50 mg/kg、100 mg/kg 和 400 mg/kg 剂量下引发低血糖，且在 400 mg/kg 剂量下会延迟高血糖的发生[2]。
Triflocin (100-400 mg/kg；皮下注射；单次给药；葡萄糖负荷前 2 小时、葡萄糖负荷即刻给予) 可在口服葡萄糖耐量试验中使禁食雄性 Wistar 大鼠出现低血糖，仅在葡萄糖负荷前 2 小时给药且剂量为 400 mg/kg 时会出现延迟性高血糖[2]。
Triflocin (100-400 mg/kg；口服；每日；连续给 15 天) 在空腹雄性 Wistar 大鼠的口服葡萄糖耐量试验中，100 mg/kg 和 400 mg/kg 剂量均可引发低血糖，仅 400 mg/kg 剂量会出现延迟性高血糖[2]。

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

Animal Model: Wistar (male, 230-260 g)[2]
Dosage: 10 mg/kg; 25 mg/kg; 50 mg/kg; 100 mg/kg; 200 mg/kg; 400 mg/kg
Administration: p.o.; single dose
Result: Produced significant hypoglycemia at 400 mg/kg at 2, 4, and 6 hours post-administration (97 mg/100 mL, 103 mg/100 mL, 109 mg/100 mL respectively; p < .05 vs. control).
Produced significant hyperglycemia at 50 mg/kg at 4 hours post-administration (120 mg/100 mL; p < .05 vs. control).
Produced significant hypoglycemia at 10 mg/kg at 6 hours post-administration (105 mg/100 mL; p < .05 vs. control).
Caused no significant blood glucose changes with 25 mg/kg, 100 mg/kg, or 200 mg/kg doses at any time point.
分子量

282.22

Formula

C13H9F3N2O2
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

Triflocin 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

Triflocin13422-16-7NKCCNa-K-Cl cotransporterNa(+)-K(+)-Cl(-) cotransporterNa+-K+-Cl− cotransporterproximal convoluted tubule cellsNa-K-2Cl cotransportthick ascending limbs of Henle's loopsATPaseproximal tubulesWistar ratsBeagle dogsgastrointestinal glucose absorptionbasolateral electrogenic Na-(HCO3)n>1 cotransportNecturus maculosusInhibitorinhibitorinhibit

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