1. Cytoskeleton
  2. Gap Junction Protein

Larazotide acetate 

Cat. No.: HY-106268A Purity: 99.53%
Handling Instructions

Larazotide acetate is a synthetic peptide that functions as a tight junction regulator and reverses leaky junctions to their normally closed state.

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

Larazotide acetate Chemical Structure

Larazotide acetate Chemical Structure

CAS No. : 881851-50-9

Size Price Stock Quantity
10 mM * 1 mL in Water USD 138 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
25 mg USD 320 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Larazotide acetate is a synthetic peptide that functions as a tight junction regulator and reverses leaky junctions to their normally closed state.

IC50 & Target

Paracellular permeability[1]

In Vitro

Larazotide acetate inhibits the redistribution and rearrangement of zonula occludens-1 (ZO-1) and actin caused by AT-1002 and gliadin fragments in Caco-2 and IEC6 cells. Larazotide acetate inhibits the AT-1002-induced TEER reduction and TJ opening in Caco-2 cells. Larazotide acetate inhibits the translocation of a gliadin 13-mer peptide, which has been implicated in celiac disease, across Caco-2 cell monolayers. Further, apically applied Larazotide acetate inhibits the increase in TJ permeability elicited by basolaterally applied cytokines[1].

In Vivo

When tested in vivo in gliadin-sensitized HLA-HCD4/DQ8 double transgenic mice, larazotide acetate inhibits gliadin-induced macrophage accumulation in the intestine and preserved normal tight junction structure[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

H2O : ≥ 20 mg/mL (25.45 mM)

DMSO : 3.2 mg/mL (4.07 mM; Need ultrasonic and warming)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2724 mL 6.3622 mL 12.7244 mL
5 mM 0.2545 mL 1.2724 mL 2.5449 mL
10 mM 0.1272 mL 0.6362 mL 1.2724 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Caco-2 cells are seeded onto 12-well plate and grown for 21–28 days until fully differentiated. The apical and basolateral compartments of Caco-2 cell monolayers are pre-incubated in Hank’s Balanced Salt Solution (HBSS) at 37°C for 30 min. Treatment solutions containing 7.5 mM LY with or without AT-1002 (7 mM) and different concentrations of larazotide acetate (5, 10, 12.5, 15 mM) in HBSS are added to the apical compartment of each monolayer and incubated at 37°C, 50 rpm for 180 min. At the end of the incubation, samples are removed from the basolateral compartment and analyzed in a fluorescence plate reader at excitation and emission wavelengths of 485 nm and 535 nm, respectively. The increase in LY passage is calculated for each treatment and is expressed relative to that of untreated controls[1].

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

Animal Administration
[1]

Mice[1]

Cohorts of HLA-HCD4/DQ8 mice (n=10 each) are sensitized (i.p.) with 500 μg of gliadin dissolved in 0.02 mM acetic acid in 50 μg of Complete Freund’sAdjuvant; thereafter, mice are gavaged with gliadin (2 mg/mouse), +/− treatment, 2×/week for 7 weeks. Group 1 receives larazotide acetate (250 μg/mouse) and gliadin, Group 2 receives AT-1002 (250 μg/mouse) and gliadin, and Group 3 is gavaged with gliadin only. A group of non-sensitized controls (CFA, i.p. only) is gavaged with rice. Twenty-four hours after the last gavage, small intestinal tissue is mounted in Ussing chambers for the measurement of electrical parameters (Isc, conductance) and macromolecule transport (horseradish peroxidase [HRP] flux). Tissue is processed for macrophage counts by immunohistochemistry using F4/80 antibody specific for a macrophage-restricted cell surface glycoprotein[1].

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

References
Molecular Weight

785.89

Formula

C₃₄H₅₉N₉O₁₂

CAS No.

881851-50-9

SMILES

O=C([[email protected]](C(C)C)NC([[email protected]](CC(C)C)NC([[email protected]](C(C)C)NC(CNC(CN)=O)=O)=O)=O)N[[email protected]@H](CCC(N)=O)C(N1[[email protected]@H](CCC1)C(NCC(O)=O)=O)=O.CC(O)=O

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.53%

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Product Name:
Larazotide acetate
Cat. No.:
HY-106268A
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Larazotide acetate

Cat. No.: HY-106268A