2C-B-FLY hydrochloride
Based on 1 Customer Validation
2C-B-FLY hydrochloride is a 5-HT2A receptor agonist with a Ki of 0.01 μM. 2C-B-FLY hydrochloride exhibits potent hallucinogenic and psychostimulant activity. 2C-B-FLY hydrochloride activates the 5-HT2A receptor and triggers G protein-mediated calcium mobilization and atypical β-arrestin 2 recruitment, thereby producing corresponding behavioral and physiological effects. 2C-B-FLY hydrochloride also inhibits human monoamine oxidase A (MAO-A) with an IC50 of 19 μM. 2C-B-FLY hydrochloride can be used in research on allergic asthma.
For research use only. We do not sell to patients.
- Purity : 99.9%
- CAS No.: 178557-21-6
- Formula: C12H15BrClNO2
- Molecular Weight:320.61
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All 5-HT Receptor Isoforms
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Biological Activity
Description
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5-HT2A Receptor 0.01 μM (Ki) |
hMAO-A 19 μM (IC50) |
In Vitro
2C-B-FLY hydrochloride inhibits NET, DAT, and SERT in HEK 293 cells with IC50 values of 94, 187, and 73 μM, respectively[1].
2C-B-FLY hydrochloride binds with high affinity to rat TAAR1 (Ki = 0.03 μM) and human 5-HT2A (Ki = 0.01 μM), and exhibits lower-affinity binding to monoamine transporters and other receptors in HEK 293 membrane preparations[1].
2C-B-FLY (100 μM; 4 h) hydrochloride does not produce cytotoxicity in HEK 293[1].
2C-B-FLY hydrochloride (5-500 μM; 120 min) is metabolized by CYP2D6 in human liver microsomes (HLM) and recombinant monoamine oxidase and competitively inhibits MAO-A activity[2].
2C-B-FLY (1 pM-100 µM; 2 h) hydrochloride acts as a 5-HT2A receptor agonist in stably expressing HEK 293 T cells, inducing β-arrestin 2 recruitment with an EC50 of 8.11 nM and an Emax of 81.8% relative to the reference agonist[4].
2C-B-FLY (10 pM-10 μM; 80 s) hydrochloride is a highly potent agonist of Gαq-mediated calcium mobilization in HEK293 cells expressing human 5-HT2A receptors, with an EMAX of 99.05% and a pEC50 of -7.27[5].
2C-B-FLY hydrochloride (2-1250 μM; 20 min) inhibits human recombinant MAO-A in a cell-free system with an IC50 of 19 µM, but is inactive against human recombinant MAO-B[6].
2C-B-FLY hydrochloride (25 µM; 2 h) has no receptor-activating effect in HEK293T cells expressing the human μ opioid receptor (MOR)[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK 293 cells
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Concentration:100 μM
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Incubation Time:4 h
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Result:Did not induce cytotoxicity.
In Vivo
2C-B-Fly (0.5 mg/kg; i.n.; single administration; 15 min) hydrochloride exhibits an anti-inflammatory effect of partially reducing airway hyperresponsiveness (AHR) in the OVA (HY-W250978)-induced allergic asthma Brown Norway rat model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6-8 weeks old)[3]
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Dosage:0.1, 0.3, 1, 3, and 10 mg/kg
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Administration:i.p.; single administration; 30 min
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Result:Dose-dependently induced the characteristic head twitch response (HTR) in mice.
Demonstrated high behavioral potency, with a calculated median effective dose (ED50) of 1.79 μmol/kg (i.e., 0.57 mg/kg).
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Animal Model:Brown Norway (RijHsd-BN; male; 6-8 weeks old on arrival; 170-220 g; sensitized at 7-9 weeks old)[5]
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Dosage:0.5 mg/kg
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Administration:i.n.; single administration; 15 min
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Result:Only partially reduced methacholine-induced airway hyperresponsiveness (AHR) and normalized enhanced pause (PenH) levels.
Exhibited reduced in vivo anti-inflammatory efficacy compared to other potent, fully efficacious structural analogs.
Chemical Information
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CAS No. 178557-21-6
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Appearance Solid
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Molecular Weight 320.61
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Formula C12H15BrClNO2
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Color White to light yellow
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SMILES
BrC1=C2CCOC2=C(CCN)C3=C1OCC3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (284 KB)
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SDS (605 KB)
- English - EN (605 KB)
- Français - FR (605 KB)
- Deutsch - DE (605 KB)
- Norwegian - NO (605 KB)
- Español - ES (605 KB)
- Swedish - SV (605 KB)
- Italian - IT (605 KB)
- Korean - KR (605 KB)
- Portuguese - PT (605 KB)
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Handling Instructions (2659 KB)
References
[1]. Rickli A, et al. Pharmacological profile of novel psychoactive benzofurans. British journal of pharmacology. 2015 Jul;172(13):3412-25. [Content Brief]
[3]. Halberstadt AL, et al. Comparison of the behavioral responses induced by phenylalkylamine hallucinogens and their tetrahydrobenzodifuran ("FLY") and benzodifuran ("DragonFLY") analogs. Neuropharmacology. 2019 Jan;144:368-376. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)