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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
AT-1001, formerly known as Larazotide Acetate, is a novel and synthetic peptide acting as a tight junction regulator and reverses leaky junctions to their normally closed state. It is being studied in people with celiac disease.
ln Vitro |
On Vero cell proliferation, larazotideacetate (1-100μM; 5 days) had an effect [1]. The varicella zoster virus (VZV) can be inhibited by larazotide acetate (1-100 μM; 3 d); the EC50 values for the OKA strain and the 07-1 strain, respectively, are 44.14 and 59.06 μM [1]. In Caco-2 cells, larazotideacetate (1 and 3 mM; 72 hours) reduces the permeability of tight junctions caused by cytokines [2]. In IEC6 cells, PTG-induced ZO-1 translocation and actin cytoskeleton rearrangement are inhibited by larazotideacetate (12.5 mM; 1 h) [2].
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ln Vivo |
Larazotide acetate (250 μg; intraperitoneally injected twice weekly for 7 weeks) inhibits intestinal permeability in gluten-sensitive transgenic mice [1].
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Cell Assay |
Cytotoxicity assay [1]
Cell Types: Vero cell line Tested Concentrations: 1-100 μM Incubation Duration: 5 days Experimental Results: Inhibited Vero cell growth, CC50 value was 82.5 μM. |
Animal Protocol |
Animal/Disease Models: HLA-HCD4/DQ8 double transgenic mice [2]
Doses: 250 μg Route of Administration: intraperitoneal (ip) injection; 250 μg twice a week for 7 weeks Experimental Results: Barrier function parameters improved, macrophages in lamina propria Cell count diminished to control levels. |
References |
[1]. Di Micco S, et al. Peptide Derivatives of the Zonulin Inhibitor Larazotide (AT1001) as Potential Anti SARS-CoV-2: Molecular Modelling, Synthesis and Bioactivity Evaluation. Int J Mol Sci. 2021 Aug 30;22(17):9427.
[2]. Gopalakrishnan S, et al. Larazotide acetate regulates epithelial tight junctions in vitro and in vivo. Peptides. 2012 May;35(1):86-94. |
Molecular Formula |
C34H59N9O12
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Molecular Weight |
785.9
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CAS # |
881851-50-9
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Related CAS # |
Larazotide;258818-34-7
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SMILES |
O=C(O)CNC([C@H]1N(C([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC(CN)=O)=O)C(C)C)=O)CC(C)C)=O)C(C)C)=O)CCC(N)=O)=O)CCC1)=O.CC(O)=O
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InChi Key |
NYGCNONRVCGHAT-UFIKZEAMSA-N
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InChi Code |
InChI=1S/C32H55N9O10.C2H4O2/c1-16(2)12-20(38-30(49)26(17(3)4)39-24(44)14-35-23(43)13-33)28(47)40-27(18(5)6)31(50)37-19(9-10-22(34)42)32(51)41-11-7-8-21(41)29(48)36-15-25(45)461-2(3)4/h16-21,26-27H,7-15,33H2,1-6H3,(H2,34,42)(H,35,43)(H,36,48)(H,37,50)(H,38,49)(H,39,44)(H,40,47)(H,45,46)1H3,(H,3,4)/t19-,20-,21-,26-,27-/m0./s1
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Chemical Name |
2-[[(2S)-1-[(2S)-5-Amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carbonyl]amino]acetic acid Acetate
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Synonyms |
Larazotide Acetate AT-1001 AT 1001 AT1001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O : ~16.67 mg/mL (~21.21 mM)
DMSO : ~3.2 mg/mL (~4.07 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (127.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.2724 mL | 6.3621 mL | 12.7243 mL | |
5 mM | 0.2545 mL | 1.2724 mL | 2.5449 mL | |
10 mM | 0.1272 mL | 0.6362 mL | 1.2724 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.