Tenapanor

Cas No.:	1234423-95-0
Chemical Name:	Tenapanor
Synonyms:	Tenapanor;AZD 1722;AZD-1722;RDX5791;RDX-5791;17-[[[3-[(4S)-6,8-Dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]-N-[2-[2-[2-[[[3-[(4S)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]ethoxy]ethoxy]ethyl]-8-oxo-12,15-dioxa-2,7,9-triazaheptadecanamide;AZD1722;Tenapanor free base;WYD79216A6;RDX 5791;Tenapanor [USAN:INN];Ibsrela;Tenapanor (USAN/INN);GTPL8449;BDBM381823;BCP24892;B
SMILES:	ClC1=C([H])C(=C([H])C2=C1C([H])([H])N(C([H])([H])[H])C([H])([H])[C@@]2([H])C1C([H])=C([H])C([H])=C(C=1[H])S(N([H])C([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])N([H])C(N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(N([H])C([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])N([H])S(C1=C([H])C([H])=C([H])C(=C1[H])[C@@]1([H])C2C([H])=C(C([H])=C(C=2C([H])([H])N(C([H])([H])[H])C1([H])[H])Cl)Cl)(=O)=O)=O)=O)(=O)=O)Cl
Formula:	C50H66Cl4N8O10S2
M.Wt:	1145.0486
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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 μM.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.