S3226 - CAS:215183-03-2

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S3226

目录号 : KM32616 CAS No. : 215183-03-2 纯度 : 99%

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S3226 是一种高选择性的 NHE-3 抑制剂 (IC₅₀<1 μM)，能特异性阻断 NHE-3 介导的钠转运。S3226 显著抑制小鼠胚胎的囊胚形成与扩张，并剂量依赖性地减少大鼠近曲小管对液体和电解质的重吸收。S3226 通过改善肾功能指标、减轻肾小管损伤及恢复细胞内 pH 稳态，能有效缓解缺血诱导的急性肾衰竭，且不干扰正常的管-球反馈反应。S3226 被广泛用于急性肾衰竭及相关病理机制的研究。

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5mg		In-stock

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生物活性

S3226 is a highly selective NHE-3 inhibitor (IC₅₀<1 μM) that specifically blocks NHE-3-mediated sodium transport. S3226 significantly inhibits blastocyst formation and expansion in mouse embryos, and reduces fluid and electrolyte reabsorption in rat proximal tubules in a dose-dependent manner. S3226 effectively alleviates ischemia-induced acute renal failure by improving renal function parameters, reducing renal tubular injury and restoring intracellular pH homeostasis, without interfering with the normal tubuloglomerular feedback response. S3226 is widely used in studies of acute renal failure and related pathological mechanisms.

体外研究

S3226 is a selective inhibitor of NHE3 transfected into mouse fibroblast L cells, negative mouse kidney cells, and porcine renal brush border membrane vesicles.

S3226 can effectively inhibit rat NHE3 in fibroblasts transfected with rat NHE3, with an IC₅₀ of 0.2 μM.

体内研究

S3226 (4-30 μM; renal tubular perfusion; Single administration per nephron; Balancing for 5 minutes before measurement can inhibit fluid and Na⁺reabsorption in the proximal tubules of anesthetized rats, with an IC₅₀ of 4-5 μM and a maximum inhibition rate of about 30%, but it does not affect loop reabsorption or tube ball feedback.
S3226 (20 mg/kg; intravenous injection; Lasting for 30 minutes, it can improve glomerular filtration rate, renal electrolyte processing function, and renal histological presentation, and achieve a survival rate of 100% in ischemic induced acute renal failure rats.
S3226 (20 mg/kg; intravenous injection; Lasting for 30 minutes; Administration twice can significantly reduce the intracellular pH of renal cells by 0.15 units during reperfusion in ischemic induced acute kidney failure rats undergoing unilateral nephrectomy.

Animal Model:	Munich-Wistar-Fromter (adult male, 270-350 g, anesthetized with superficial nephrons)
Dosage:	4-5 µM; 10 µM; 30 µM
Administration:	intratubular microperfusion; single application per nephron; 5-minute equilibration before measurement
Result:	Caused a dose-dependent inhibition of fluid, Na⁺, and Cl^- reabsorption in proximal convoluted tubules with an IC₅₀ of 4-5 µM. Achieved maximum inhibition of ~30% for fluid and Na⁺ reabsorption, and ~10% for Cl^- reabsorption. Produced a significantly greater reduction in Na⁺ reabsorption than in Cl^- reabsorption at 10 or 30 µM. Showed no effect on fluid, Na⁺, or K⁺ reabsorption in loop of Henle segments at 10 µM and 30 µM. Did not alter the tubuloglomerular feedback response, including stop-flow pressure magnitude, curve slope, or operating point shift, at 30 µM.

Animal Model:	Wistar (male, mean body weight 285 g, bilateral renal artery occlusion for 40 minutes)
Dosage:	20 mg/kg
Administration:	i.v.; over 30 minutes; single dose (pre-occlusion or post-reperfusion)
Result:	Increased creatinine clearance to 0.90 mL/min/kg (pre-occlusion treatment) and 0.83 mL/min/kg (post-reperfusion treatment) on day 1 post-ischemia, compared to 0.30 mL/min/kg in controls. Reduced fractional sodium excretion from 8.17% in controls to 1.42% (pre-occlusion treatment) and 1.88% (post-reperfusion treatment) on day 1. Reduced urinary sodium excretion to 0.31 mmol/kg (pre-occlusion treatment) and 0.31 mmol/kg (post-reperfusion treatment) on day 1, compared to 0.98 mmol/kg in controls. Lowered plasma creatinine elevation on days 1, 2, and 3 post-infusion compared to controls. Lowered plasma potassium concentration on days 2 and 3 compared to controls. Reduced fractional potassium excretion on day 1 compared to controls. Pronounced reduction of tubular necrosis, dilatation, protein casts, and cellular infiltration in kidneys harvested on day 7. Achieved 100% survival rate over 7 days, compared to 75% survival rate in controls.

分子式

C₁₇H₂₄Cl₂N₆O₂

分子量

415.32

CAS号

215183-03-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

纯度： 99%

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