2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. AT 1001

AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease.

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AT 1001

AT 1001 Chemical Structure

CAS No. : 1314801-63-2

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AT 1001 Related Antibodies

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Description

AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease[1][2][3].
In Vitro

AT 1001 (3-300 nM) potently, non-competitively inhibits epibatidine-induced calcium flux in α3β4-transfected HEK cells with an IC50 of 35.2 nM, with no inherent agonist activity[1].
AT 1001 (10 nM; 500 ms) potently and reversibly inhibits epibatidine-induced inward currents in α3β4-transfected HEK cells, reducing current amplitude by 66% at 10 nM[1].
AT 1001 (10 μM; 10 min) partially inhibits nicotine-induced [3H]dopamine release from rat NAc synaptosomes, producing 40% inhibition at 10 μM[1].
AT 1001 exhibits high selectivity for α3β4 nAChRs over most tested receptors and ion channels, with only weak affinity for a small subset of off-targets, including sigma1 receptors (Ki = 84 nM)[1].
AT 1001 inhibits gliadin-induced intestinal epithelial cell cytoskeletal and tight junction dysfunction, and blocks gliadin- and ZOT analogue-induced paracellular permeability in in vitro intestinal epithelial cell monolayers and diseased human duodenal epithelia[2].
AT 1001 (1722 nM; 120 s) acts as a partial agonist at rat α3β4 nAChRs expressed in HEK cells, with an EC50 of 1722 nM and 38.1% of nicotine's maximum stimulatory activity[3].
AT 1001 (10000 nM; 120 s) shows weak partial agonist activity at rat α4β2 nAChRs expressed in HEK cells, with less than 25% of nicotine's maximum stimulatory activity at 10000 nM and an EC50 exceeding 10000 nM[3].
AT 1001 (91 nM; 15 min) acts as a functional antagonist at rat α3β4 nAChRs expressed in HEK cells, inhibiting epibatidine-induced calcium mobilization with an IC50 of 91 nM[3].
AT 1001 (276 nM; 15 min) acts as a functional antagonist at rat α4β2 nAChRs expressed in HEK cells, inhibiting epibatidine-induced membrane potential changes with an IC50 of 276 nM, which is threefold higher than its IC50 at α3β4 nAChRs[3].

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

AT 1001 Related Antibodies
In Vivo

AT 1001 (0.75-3 mg/kg; s.c.; single administration) dose-dependently blocks nicotine self-administration behavior in male Sprague-Dawley rats, reducing this behavior by 90.5% at the subcutaneous dose of 3 mg/kg without affecting food-maintained responding behavior[1].
Oral administration of AT 1001 blocks intestinal permeability and humoral autoimmune expression, thereby alleviating the progression of type 1 diabetes in BB/wor DP rats[2].
AT 1001 (0.3-30 μg/kg; intravenous injection; single administration) shows no reinforcing effect in rats with a history of nicotine exposure. Its lever-pressing counts and breakpoint are comparable to those of the normal saline control group, and significantly lower than those of the nicotine group[3].
AT 1001 (0.75-3.0 mg/kg; s.c.; single administration) attenuates nicotine-seeking behavior reinstatement induced by pre-injection of nicotine and Varenicline (HY-10019), and the 3.0 mg/kg dose also reduces lever-pressing behavior at the extinction level[3].
AT 1001 (0.75-1.5 mg/kg; s.c.; single administration) selectively blocks nicotine self-administration behavior in a co-administration paradigm without altering alcohol lever-pressing behavior[3].

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

Animal Model: Sprague-Dawley (male, age ≥81 days, maintained at ~85% free-feeding body weight during food training, 90-95% free-feeding body weight during nicotine self-administration)[1]
Dosage: 0.75 mg/kg; 1.5 mg/kg; 3 mg/kg
Administration: s.c.; 10 min before 1-hour test session
Result: Significantly reduced nicotine rewards earned compared with vehicle at 0.75 mg/kg.
Produced a greater significant reduction in nicotine rewards earned compared with vehicle at 1.5 mg/kg.
Reduced nicotine rewards by 90.5% at 3 mg/kg.
Did not produce significant reductions in lever-pressing responses for food rewards at any tested dose.
Returned nicotine responding to baseline levels within 24 hours after administration of the 3 mg/kg dose.
Animal Model: Sprague-Dawley (male, 200-225 g, trained to self-administer nicotine via fixed ratio-3 and progressive ratio schedules)[3]
Dosage: 0.3 μg/kg; 3.0 μg/kg; 30 μg/kg
Administration: i.v.; 4 days of FR-3 sessions followed by 1 day of PR session weekly
Result: Induced lever-pressing levels significantly lower than nicotine (baseline nicotine response rate: 26.9 responses in 2 h) and comparable to saline controls.
Exhibited break points similar to saline and significantly lower than nicotine break points.
Animal Model: Sprague-Dawley (male, 200-225 g, trained to self-administer nicotine then extinguished from nicotine-seeking behavior)[3]
Dosage: 0.75 mg/kg; 1.5 mg/kg; 3 mg/kg
Administration: s.c.; single injection 10 min before reinstatement session or priming injection
Result: Significantly reduced nicotine-associated lever pressing.
Attenuated nicotine priming-induced reinstatement dose-dependently.
Significantly attenuated varenicline priming-induced reinstatement at all doses.
Animal Model: Sprague-Dawley (male, 200-225 g, trained to co-administer nicotine and alcohol via operant conditioning)[3]
Dosage: 0.75 mg/kg; 1.5 mg/kg
Administration: s.c.; single injection 10 min before test session
Result: Decreased nicotine-associated lever pressing dose-dependently.
Did not alter alcohol-associated lever pressing at any tested dose.
Molecular Weight

309.24

Formula

C15H21BrN2
CAS No.
Appearance

Solid

Color

Brown to dark brown

SMILES

BrC(C=CC=C1)=C1N[C@H]2C[C@@H]3N(C)[C@@H](CCC3)C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (161.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2337 mL 16.1687 mL 32.3373 mL
5 mM 0.6467 mL 3.2337 mL 6.4675 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.94%

SDS (393 KB)

COA (250 KB) HNMR (132 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2337 mL 16.1687 mL 32.3373 mL 80.8434 mL
5 mM 0.6467 mL 3.2337 mL 6.4675 mL 16.1687 mL
10 mM 0.3234 mL 1.6169 mL 3.2337 mL 8.0843 mL
15 mM 0.2156 mL 1.0779 mL 2.1558 mL 5.3896 mL
20 mM 0.1617 mL 0.8084 mL 1.6169 mL 4.0422 mL
25 mM 0.1293 mL 0.6467 mL 1.2935 mL 3.2337 mL
30 mM 0.1078 mL 0.5390 mL 1.0779 mL 2.6948 mL
40 mM 0.0808 mL 0.4042 mL 0.8084 mL 2.0211 mL
50 mM 0.0647 mL 0.3234 mL 0.6467 mL 1.6169 mL
60 mM 0.0539 mL 0.2695 mL 0.5390 mL 1.3474 mL
80 mM 0.0404 mL 0.2021 mL 0.4042 mL 1.0105 mL
100 mM 0.0323 mL 0.1617 mL 0.3234 mL 0.8084 mL
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AT 1001 Related Classifications

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  • 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.

Keywords:

AT 10011314801-63-2AT1001AT-1001nAChRNicotinic acetylcholine receptorsα3β4 nAChRBB/wor DP ratsα4β2 nAChRsigma1 receptorsnicotine addictionHEK cellsSprague-Dawley ratsType 1 DiabetesVibrio choleraecoeliac diseaseInhibitorinhibitorinhibit

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