A NHE-3 inhibitor
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Tenapanor (hydrochloride)

Item No. 32875

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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, dihydrochloride
CAS Number
1234365-97-9
Synonyms
  • AZD 1722
Molecular Formula
C50H66Cl4N8O10S2 • 2HCl
Formula Weight
1218.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleWater: Soluble
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
InChi Code
InChI=1S/C50H66Cl4N8O10S2.2ClH/c1-61-31-43(41-27-37(51)29-47(53)45(41)33-61)35-7-5-9-39(25-35)73(65,66)59-15-19-71-23-21-69-17-13-57-49(63)55-11-3-4-12-56-50(64)58-14-18-70-22-24-72-20-16-60-74(67,68)40-10-6-8-36(26-40)44-32-62(2)34-46-42(44)28-38(52)30-48(46)54;;/h5-10,25-30,43-44,59-60H,3-4,11-24,31-34H2,1-2H3,(H2,55,57,63)(H2,56,58,64);2*1H/t43-,44-;;/m0../s1
InChi Key
VFRAXTZDILCRKY-OWRGXFNZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $81

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    10 mg

    $128

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    25 mg

    $200

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    Product Description

    Tenapanor is an orally bioavailable inhibitor of sodium-hydrogen exchanger 3 (NHE-3; IC50 = 10 nM for the recombinant rat protein).1 Tenapanor (10 µM) inhibits intestinal fluid absorption in mouse jejunum, but not distal colon, in a closed intestine loop assay.2 It also lowers both the sodium and phosphate urinary-to-dietary ratio in a dose-dependent manner in rats.1 Tenapanor (5 mg/kg) reverses decreases in stool pellet numbers and water content induced by loperamide (Item No. 14875) and prevents loperamide-induced constipation in mice.2 Formulations containing tenapanor have been used in the treatment of irritable bowel syndrome with constipation.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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 CKD. J. 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 constipation. JCI Insight 3(14), e121370 (2018).