S3226
Based on 1 Customer Validation
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.
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- Purity: 99.65%
- CAS No.: 215183-03-2
- 화학식: C17H24Cl2N6O2
- 분자량:415.32
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보관:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
S3226 acts as a selective inhibitor of NHE3 in transfected mouse fibroblast L cells, opossum kidney cells, and porcine renal brush-border membrane vesicles[2].
S3226 potently inhibits rat NHE3 in fibroblasts transfected with rat NHE3 with an IC50 of 0.2 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
S3226 (20 mg/kg; i.v.; over 30 minutes) improves glomerular filtration rate, renal electrolyte handling, and renal histology, and supports 100% survival in rats with ischemia-induced acute renal failure[3].
S3226 (20 mg/kg; i.v.; over 30 minutes; two doses) significantly reduces renal intracellular pH by 0.15 units during reperfusion in uninephrectomized rats with ischemia-induced acute renal failure[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Munich-Wistar-Fromter (adult male, 270-350 g, anesthetized with superficial nephrons)[2]
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Dosage:4-5 µM; 10 µM; 30 µM
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Administration:intratubular microperfusion; single application per nephron; 5-minute equilibration before measurement
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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.
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Animal Model:Wistar (male, mean body weight 285 g, bilateral renal artery occlusion for 40 minutes)[3]
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Dosage:20 mg/kg
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Administration:i.v.; over 30 minutes; single dose (pre-occlusion or post-reperfusion)
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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.
Chemical Information
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CAS No. 215183-03-2
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Appearance Solid
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분자량 415.32
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화학식 C17H24Cl2N6O2
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Color White to off-white
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SMILES
[H]Cl.[H]Cl.C/C(C(NC(N)=N)=O)=C\C(C=CC(C)=C1)=C1/C=C(C)/C(NC(N)=N)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
순도&문서
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kawagishi R, et al. Na+ / H+ exchanger-3 is involved in mouse blastocyst formation. J Exp Zool A Comp Exp Biol. 2004;301(9):767-775. [Content Brief]
[3]. Hropot M, et al. S3226, a novel NHE3 inhibitor, attenuates ischemia-induced acute renal failure in rats. Kidney Int. 2001;60(6):2283-2289. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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