2. Membrane Transporter/Ion Channel
  3. Apical Sodium-Dependent Bile Acid Transporter
  4. Linerixibat

Linerixibat  (Synonyms: GSK2330672)

Cat. No.: HY-16643 Purity: 99.98%
COA 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 325 In-stock
Solution
10 mM * 1 mL in DMSO USD 325 In-stock
Solid
1 mg USD 100 In-stock
5 mg USD 270 In-stock
10 mg USD 450 In-stock
25 mg USD 900 In-stock
50 mg USD 1440 In-stock
100 mg USD 2160 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 12 publication(s) in Google Scholar

Linerixibat Related Antibodies

Top Publications Citing Use of Products

    Linerixibat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Jul 17;11(1):3612.  [Abstract]

    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.

    Linerixibat purchased from MedChemExpress. Usage Cited in: Gene Expr. 2018 Aug 22;18(3):187-196.  [Abstract]

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

    • Biological Activity

    • Purity & Documentation

    • References

    • 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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Linerixibat Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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

    Appearance

    Solid

    Formula

    C28H38N2O7S
    CAS No.
    SMILES

    O=C(O)CC(NCC1=C(OC)C=C(C2=C1)[C@@H](C3=CC=CC=C3)N[C@](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 2 years
    -20°C 1 year
    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 available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.98%

    COA (258 KB) LCMS (100 KB)

    Handling Instructions (2659 KB)
    References
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    Linerixibat Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Linerixibat1345982-69-5GSK2330672GSK 2330672GSK-2330672Apical Sodium-Dependent Bile Acid TransporterASBTIleal Bile Acid TransporterIBATSLC10A2type-2diabeteslipid-loweringnonabsorbablePrimaryBiliaryCholangitisPBCaqueoussolubilityInhibitorinhibitorinhibit

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