Tenapanor is an orally bioavailable inhibitor of sodium-hydrogen exchanger 3 (NHE-3; IC = 10 nM for the recombinant rat protein). Tenapanor (10 µM) inhibits intestinal fluid absorption in mouse jejunum, but not distal colon, in a closed intestine loop assay. It also lowers both the sodium and phosphate urinary-to-dietary ratio in a dose-dependent manner in rats. Tenapanor (5 mg/kg) reverses decreases in stool pellet numbers and water content induced by loperamide and prevents loperamide-induced constipation in mice. Formulations containing tenapanor have been used in the treatment of irritable bowel syndrome with constipation.
Tenapanor (hydrochloride) is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor (hydrochloride) reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor (hydrochloride) has the potential for the research of hyperphosphatemia.
Tenapanor hydrochloride (0.15 mg/kg; p.o.; twice-daily for 11 consecutive days) increases the reduction in urinary phosphorus excretion in rats[2] .
Animal Model:
Rats (intestinal loop model)[1]
Dosage:
0.15, 0.5 mg/kg
Administration:
P.o.
Result:
Reduced passive paracellular phosphate absorption by reduced urinary phosphate and sodium excretion after the high-phosphate meal and increased sodium and phosphate delivery to the cecum.
Animal Model:
8 weeks, 250 g male Sprague–Dawley rats[2]
Dosage:
0.15 mg/kg in combination with sevelamer (0%, 0.75%, 1.5%, and 3% (wt/wt))
Administration:
Oral gavage; twice-daily for 11 consecutive days
Result:
Significantly augmented the reduction in urinary phosphorus excretion.
分子式
C50H66Cl4N8O10S2.2HCl
分子量
1217.97
CAS号
1234365-97-9
中文名称
盐酸替那帕诺
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
2-8°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : 100 mg/mL (82.10 mM; Need ultrasonic)
H2O : 20 mg/mL (16.42 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
0.8210 mL
4.1052 mL
8.2104 mL
5 mM
0.1642 mL
0.8210 mL
1.6421 mL
10 mM
0.0821 mL
0.4105 mL
0.8210 mL
*
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: