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Linerixibat (Synonyms: GSK2330672)

Cat. No.: HY-16643 Purity: 99.88%
Handling Instructions

Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment.

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

Linerixibat Chemical Structure

Linerixibat 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 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Linerixibat 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.

    Linerixibat purchased from MCE. Usage Cited in: Nat Commun. 2020 Jul 17;11(1):3612.

    TFEB protein in total liver lysates and nuclear fractions. GSK2330672 (GSK) treatment significantly increases hepatic TFEB nuclear abundance without altering total hepatic TFEB mRNA or protein in mice.
    • Biological Activity

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    • Customer Review

    Description

    Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment[1][2][3].

    IC50 & Target

    IC50: 42 nM (Apical sodium-dependent bile acid transporter (ASBT))[1]

    In Vitro

    The zwitterionic, nonhygroscopic, crystalline salt form of Linerixibat (Compound 56) shows good aqueous solubility at pH 7.4 (>7 mg/mL), excellent thermal stability, and did not generate reactive or humanspecific metabolite, characteristics[1].

    In Vivo

    Linerixibat (GSK2330672; 0.05-10 mg/kg; oral gavage; twice daily; for 14 days; male ZDF rat) treatment lowers glucose in an animal model of type 2 diabetes[1].

    Animal Model: Male Zucker Diabetic Fatty (ZDF) rat[1]
    Dosage: 0.05 mg/kg, 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg
    Administration: Oral gavage; twice daily; for 14 days
    Result: Led to a 1.30-1.64% reduction in hemoglobin A1c (HbA1c), a greater than 50% reduction in nonfasted plasma glucose to below 200 mg/dL, and statistically significant higher plasma insulin.
    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 : 50 mg/mL (91.46 mM; Need ultrasonic)

    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.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (4.57 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.88%

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    Keywords:

    LinerixibatGSK2330672GSK 2330672GSK-2330672OthersASBTtype-2diabeteslipid-loweringnonabsorbablePrimaryBiliaryCholangitisPBCaqueoussolubilityInhibitorinhibitorinhibit

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    Product Name:
    Linerixibat
    Cat. No.:
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