Tenapanor (AZD1722) hydrochloride is a first-in-class, potent, orally active sodium/hydrogen exchange isomer 3 (NHE3) inhibitor that reduces intestinal phosphate absorption primarily by decreasing passive paracellular phosphate flux. Tenapanor hydrochloride reduces intestinal absorption of phosphate by reducing passive paracellular phosphate flux. Tenapanor hydrochloride is used in studies related to chronic renal insufficiency, hyperphosphatemia, constipation, and irritable bowel syndrome.
| Molecular Weight | 1217.97 |
| Formula | C50H68Cl6N8O10S2 |
| CAS Number | 1234365-97-9 |
| Form | Solid |
| Storage | 4°C, protect from light, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Na+/H+ Exchanger (NHE) Products |
|---|
| NHE3-IN-1
NHE3-IN-1 is an inhibitor of sodium/proton exchanger 3 (NHE-3). |
| NHE3-IN-2
NHE3-IN-2 is a Na+/H+ exchanger 3 (NHE3) inhibitor. |
| Eniporide
Eniporide (EMD 96785) is a Na(+)/H(+) exchange (NHE) inhibitor. |
| Zoniporide hydrochloride hydrate
Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM). |
| Zoniporide hydrochloride
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM). |
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