Tenapanor
(Synonyms: AZD1722; RDX5791) 目录号 : GC19352
A NHE-3 inhibitor
Cas No.:1234423-95-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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.
| Cas No. | 1234423-95-0 | SDF | |
| 别名 | 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 | ||
| 分子式 | C50H66Cl4N8O10S2 | 分子量 | 1145.05 |
| 溶解度 | DMSO : 50 mg/mL (43.67 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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