Tenapanor (Synonyms: AZD1722; RDX5791) |
| Katalog-Nr.GC19352 |
Tenapanor (AZD1722) ist ein potenter und oral aktiver Hemmer der Natrium/Wasserstoff-Austauscher-Isoform 3 (NHE3).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1234423-95-0
Sample solution is provided at 25 µL, 10mM.
Tenapanor is an inhibitor of the Na+/H+ exchanger NHE3 with IC50 values of 5 and 10 nM against human and Rat NHE3, respectively.
Tenapanor exhibits human and rat NHE3 with IC50 values of 5 and 10 nM, respectively. Human intestinal transporters NHE1, NHE2, TGR5, ASBT, and Pit-1 and the sodium-dependent phosphate transporter NaPiIIb are not inhibited by tenapanor at concentrations up to 10 to 30 uM[1].
Tenapanor plays a prominent role in sodium handling in the gastrointestinal tract and kidney. It acts exclusively in the gastrointestinal tract to inhibit sodium uptake when administered orally to rats. Average plasma Cmax values of tenapanor in rats and humans are less than 1 ng/mL with negligible area under the curve at doses of up to 30mg/kg in rats, 10mg/kg in dogs, and 900 mg in humans. Dose-dependent reductions in urinary sodium and increases in fecal sodium and luminal fluid mass are observed upon administering single doses of tenapanor to rats. Chronic administration of tenapanor to rats fed with standard chow (0.49% NaCl) causes a sustained reduction of urinary sodium and increase in fecal sodium[1].
References:
[1]. Spencer AG, et al. Intestinal inhibition of the Na+/H+ exchanger 3 prevents cardiorenal damage in rats and inhibitsNa+ uptake in humans.
Animal experiment: | Rats: For urinary and fecal sodium assessments, 8-week-old Sprague-Dawley rats are randomized into groups before oral administration of vehicle or tenapanor (10ml/kg). After 16 to 24 hours, collected excreta are analyzed for electrolytes by ion chromatography. In normal rats, tenapanor doses ranges from 0.1 to 10 mg/kg. Higher doses within this range (1 to 10 mg/kg) are used to evaluate aldosterone levels and serum bicarbonate; lower doses (0.1 to 3 mg/kg) are used to evaluate urine electrolytes as well as other electrolytes[1]. |
References: [1]. Spencer AG, et al. Intestinal inhibition of the Na+/H+ exchanger 3 prevents cardiorenal damage in rats and inhibitsNa+ uptake in humans. | |
| Cas No. | 1234423-95-0 | SDF | |
| Überlieferungen | AZD1722; RDX5791 | ||
| Canonical SMILES | O=C(NCCOCCOCCNS(=O)(C1=CC=CC([C@@H]2CN(C)CC3=C2C=C(Cl)C=C3Cl)=C1)=O)NCCCCNC(NCCOCCOCCNS(=O)(C4=CC=CC([C@@H]5CN(C)CC6=C5C=C(Cl)C=C6Cl)=C4)=O)=O | ||
| Formula | C50H66Cl4N8O10S2 | M.Wt | 1145.05 |
| Löslichkeit | DMSO : 50 mg/mL (43.67 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.8733 mL | 4.3666 mL | 8.7332 mL |
| 5 mM | 0.1747 mL | 0.8733 mL | 1.7466 mL |
| 10 mM | 0.0873 mL | 0.4367 mL | 0.8733 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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- Purity: >98.00%
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