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Iinerixibat (Synonyms: GSK2330672)

Cat. No.: HY-16643 Purity: 99.55%
Handling Instructions

Iinerixibat (GSK2330672) is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) which lowers glucose in an animal model of type 2 diabetes and shows excellent developability properties for evaluating the potential therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.

For research use only. We do not sell to patients.

Iinerixibat Chemical Structure

Iinerixibat Chemical Structure

CAS No. : 1345982-69-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 325 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 270 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Iinerixibat purchased from MCE. Usage Cited in: Gene Expr. 2018 Aug 22;18(3):187-196.

    Hepatic cysteine sulfinic acid decarboxylase (CSAD) protein are significantly increased in mice treated with GSK672.
    • Biological Activity

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    • References

    • Customer Review

    Description

    Iinerixibat (GSK2330672) is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) which lowers glucose in an animal model of type 2 diabetes and shows excellent developability properties for evaluating the potential therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.

    IC50 & Target

    IC50: 42±3 nM (hASBT) [1]

    In Vitro

    Iinerixibat (GSK2330672) is a highly potent, nonabsorbable ASBT inhibitor with excellent aqueous solubility, selectivity, and developability properties for evaluation in safety studies and ultimately humans. Iinerixibat will be a valuable clinical tool for exploring the therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.[1]

    In Vivo

    Iinerixibat (GSK2330672) results in potent inhibition of ASBT and very low oral absorption in the rat. Iinerixibat shows potent mouse and rat ASBT activity and was stable in GI stability assays. Iinerixibat is stable in the rodent GI tract and potently induced fecal bile acid excretion in mice, leading us to select these three compounds for mechanistic and efficacy studies in vivo in lean rats and Zucker Diabetic Fatty (ZDF) rats, respectively.[1]

    Clinical Trial
    Molecular Weight

    546.68

    Formula

    C₂₈H₃₈N₂O₇S

    CAS No.

    1345982-69-5

    SMILES

    O=C(O)CC(NCC1=C(OC)C=C(C2=C1)[[email protected]@H](C3=CC=CC=C3)N[[email protected]](CC)(CCCC)CS2(=O)=O)CC(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 21.5 mg/mL (39.33 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8292 mL 9.1461 mL 18.2922 mL
    5 mM 0.3658 mL 1.8292 mL 3.6584 mL
    10 mM 0.1829 mL 0.9146 mL 1.8292 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      GSK2330672 is prepared in 1% methylcellulose[3].

    References

    Purity: 99.55%

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    Product name:
    Iinerixibat
    Cat. No.:
    HY-16643
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