AT-1001 | CAS#1314801-63-2 | α3β4 nAChR partial agonist

MedKoo Cat#: 533256 | Name: AT-1001

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

Chemical Structure

AT-1001

CAS#1314801-63-2

Theoretical Analysis

MedKoo Cat#: 533256

Name: AT-1001

CAS#: 1314801-63-2

Chemical Formula: C14H19BrN2

Exact Mass: 294.0732

Molecular Weight: 295.22

Elemental Analysis: C, 56.96; H, 6.49; Br, 27.07; N, 9.49

Price and Availability

Size	Price	Availability
5mg	USD 250.00	Ready to ship
10mg	USD 450.00	Ready to ship
50mg	USD 1,350.00	2 Weeks

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Related CAS #

No Data

Synonym

AT-1001; AT 1001; AT1001;

IUPAC/Chemical Name

(1R,3r,5S)-N-(2-Bromophenyl)-8-methyl-8-azabicyclo[3.2.1]octan-3-amine

InChi Key

BUVQHAVXIBTLGL-ZSBIGDGJSA-N

InChi Code

InChI=1S/C14H19BrN2/c1-17-11-6-7-12(17)9-10(8-11)16-14-5-3-2-4-13(14)15/h2-5,10-12,16H,6-9H2,1H3/t10-,11+,12-

SMILES Code

CN1[C@@]2([H])C[C@H](NC3=CC=CC=C3Br)C[C@]1([H])CC2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 295.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Troisi J, Venutolo G, Terracciano C, Carri MD, Di Micco S, Landolfi A, Fasano A. The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases. Curr Med Chem. 2021;28(28):5788-5807. doi: 10.2174/0929867328666210104110053. PMID: 33397225. 2: Yuan M, Malagon AM, Yasuda D, Belluzzi JD, Leslie FM, Zaveri NT. The α3β4 nAChR partial agonist AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. Behav Brain Res. 2017 Aug 30;333:251-257. doi: 10.1016/j.bbr.2017.07.004. Epub 2017 Jul 8. PMID: 28693859; PMCID: PMC5557392. 3: Khroyan TV, Yasuda D, Toll L, Polgar WE, Zaveri NT. High affinity α3β4 nicotinic acetylcholine receptor ligands AT-1001 and AT-1012 attenuate cocaine- induced conditioned place preference and behavioral sensitization in mice. Biochem Pharmacol. 2015 Oct 15;97(4):531-541. doi: 10.1016/j.bcp.2015.08.083. Epub 2015 Aug 7. PMID: 26256075; PMCID: PMC4600456. 4: Tuan EW, Horti AG, Olson TT, Gao Y, Stockmeier CA, Al-Muhtasib N, Bowman Dalley C, Lewin AE, Wolfe BB, Sahibzada N, Xiao Y, Kellar KJ. AT-1001 Is a Partial Agonist with High Affinity and Selectivity at Human and Rat α3β4 Nicotinic Cholinergic Receptors. Mol Pharmacol. 2015 Oct;88(4):640-9. doi: 10.1124/mol.115.099978. Epub 2015 Jul 10. PMID: 26162864; PMCID: PMC4576681. 5: Cippitelli A, Brunori G, Gaiolini KA, Zaveri NT, Toll L. Pharmacological stress is required for the anti-alcohol effect of the α3β4* nAChR partial agonist AT-1001. Neuropharmacology. 2015 Jun;93:229-36. doi: 10.1016/j.neuropharm.2015.02.005. Epub 2015 Feb 14. PMID: 25689019; PMCID: PMC4387088. 6: Cippitelli A, Wu J, Gaiolini KA, Mercatelli D, Schoch J, Gorman M, Ramirez A, Ciccocioppo R, Khroyan TV, Yasuda D, Zaveri NT, Pascual C, Xie XS, Toll L. AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br J Pharmacol. 2015 Apr;172(7):1834-45. doi: 10.1111/bph.13034. Epub 2015 Jan 23. PMID: 25440006; PMCID: PMC4376460. 7: Zaveri NT, Bertrand S, Yasuda D, Bertrand D. Functional characterization of AT-1001, an α3β4 nicotinic acetylcholine receptor ligand, at human α3β4 and α4β2 nAChR. Nicotine Tob Res. 2015 Mar;17(3):361-7. doi: 10.1093/ntr/ntu170. Epub 2014 Sep 1. PMID: 25180076; PMCID: PMC4837995. 8: Toll L, Zaveri NT, Polgar WE, Jiang F, Khroyan TV, Zhou W, Xie XS, Stauber GB, Costello MR, Leslie FM. AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats. Neuropsychopharmacology. 2012 May;37(6):1367-76. doi: 10.1038/npp.2011.322. Epub 2012 Jan 25. PMID: 22278092; PMCID: PMC3327842. 9: Paterson BM, Lammers KM, Arrieta MC, Fasano A, Meddings JB. The safety, tolerance, pharmacokinetic and pharmacodynamic effects of single doses of AT-1001 in coeliac disease subjects: a proof of concept study. Aliment Pharmacol Ther. 2007 Sep 1;26(5):757-66. doi: 10.1111/j.1365-2036.2007.03413.x. PMID: 17697209.

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