Tenapanor (AZD1722) hydrochloride 是一种有效且具有口服活性的钠/氢交换异构体 3 (NHE3) 抑制剂。
| Cas No. | 1234365-97-9 |
| 别名 | TENAPANORHCL(2盐),AZD1722 hydrochloride; RDX5791 hydrochloride |
| Canonical SMILES | O=S(NCCOCCOCCNC(NCCCCNC(NCCOCCOCCNS(=O)(C1=CC=CC([C@@]2(CN(C)CC3=C(Cl)C=C(C=C23)Cl)[H])=C1)=O)=O)=O)(C4=CC([C@@]5([H])C6=CC(Cl)=CC(Cl)=C6CN(C5)C)=CC=C4)=O.Cl.Cl |
| 分子式 | C50H66Cl4N8O10S2•2HCl |
| 分子量 | 1218 |
| 溶解度 | DMSO: soluble,Water: soluble |
| 储存条件 | -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Tenapanor is an orally bioavailable inhibitor of sodium-hydrogen exchanger 3 (NHE-3; IC50= 10 nM for the recombinant rat protein).1Tenapanor (10 µM) inhibits intestinal fluid absorption in mouse jejunum, but not distal colon, in a closed intestine loop assay.2It also lowers both the sodium and phosphate urinary-to-dietary ratio in a dose-dependent manner in rats.1Tenapanor (5 mg/kg) reverses decreases in stool pellet numbers and water content induced by loperamide and prevents loperamide-induced constipation in mice.2Formulations containing tenapanor have been used in the treatment of irritable bowel syndrome with constipation. 1.LabontÉ, E.D., Carreras, C.W., Leadbetter, M.R., et al.Gastrointestinal inhibition of sodium-hydrogen exchanger 3 reduces phosphorus absorption and protects against vascular calcification in CKDJ. Am. Soc. Nephrol.26(5)1138-1149(2015)
2.Haggie, P.M., Cil, O., Lee, S., et al.SLC26A3 inhibitor identified in small molecule screen blocks colonic fluid absorption and reduces constipationJCI Insight3(14)e121370(2018) |
