A peptide antagonist of α3β4 subunit-containing nAChRs
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Larazotide (acetate)

Item No. 43008

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
glycylglycyl-L-valyl-L-leucyl-L-valyl-L-glutaminyl-L-prolyl-glycine, monoacetate salt
CAS Number
881851-50-9
Synonyms
  • AT-1001
  • Gly-Gly-Val-Leu-Val-Gln-Pro-Gly
Molecular Formula
C32H55N9O10 • C2H4O2
Formula Weight
785.9
Purity
≥98%
Formulation
A solid
Peptide Sequence
GGVLVQPG
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/mlPBS pH 7.2: Sparingly Soluble: 1-10 mg/ml
SMILES
CC(O)=O.NCC(NCC(N[C@@H](C(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](C(C)C)C(N[C@@H](CCC(N)=O)C(N1[C@@H](CCC1)C(NCC(O)=O)=O)=O)=O)=O)=O)=O)=O
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)46;1-2(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
InChi Key
NYGCNONRVCGHAT-UFIKZEAMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $110

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    10 mg

    $180

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    50 mg

    $413

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    Product Description

    Larazotide is a peptide antagonist of α3β4 subunit-containing nicotinic acetylcholine receptors (nAChRs).1 It selectively inhibits epibatidine-induced calcium mobilization in HEK293 cells expressing human α3β4 subunit-containing nAChRs over HEK293 cells expressing α4β2 subunit-containing nAChRs (IC50s = 91 and 276 nM, respectively). Larazotide (100 µM) decreases inflammatory cytokine-induced tight junction dysfunction in isolated rat intestinal epithelial cells.2 In vivo, larazotide (0.3, 3, and 30 µg/kg) inhibits nicotine self-administration and varenicline-induced reinstatement of nicotine-seeking behavior in rats. It also increases intestinal epithelial cell bridging and decreases intestinal damage without reducing liver damage in a rat model of thioacetamide-induced acute liver failure.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cippitelli, A., Wu, J., Gaiolini, K.A., et al. AT-1001: A high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br. J. Pharmacol. 172(7), 1834-1845 (2015).

    2. Khaleghi, S., Ju, J.M., Lamba, A., et al. The potential utility of tight junction regulation in celiac disease: focus on larazotide acetate. Therap. Adv. Gastroenterol. 9(1), 37-49 (2016).

    3. Caliskan, A.R., Gul, M., Yilmaz, I., et al. Effects of larazotide acetate, a tight junction regulator, on the liver and intestinal damage in acute liver failure in rats. Hum. Exp. Toxicol. 40 (12 suppl), S693-S701 (2021).