BD-1063 dihydrochloride
Based on 3 publication(s) in Google Scholar
BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.
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- Pureté: 98.0%
- CAS No.: 206996-13-6
- Formule: C13H20Cl4N2
- Masse moléculaire:346.12
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
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Publications Citing Use of MedChemExpress (MCE) BD-1063 dihydrochloride
MoreVoir tous les produits spécifiques à Isoform Sigma Receptor
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Activité biologique
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Sigma 1 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | EC50 |
>100 μM
Compound: BD, BD1063
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Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
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[PMID: 23415062] |
| MCF7 | EC50 |
70 μM
Compound: BD, BD1063
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Antiproliferative activity against human MCF7 cells transfected with human sigma1 receptor after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells transfected with human sigma1 receptor after 48 hrs by MTT assay
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[PMID: 23415062] |
BD-1063 dihydrochloride (10-100 μM; 30 min) inhibits sustained calcium entry evoked by histamine, VEGF, or H2O2 in human saphenous vein endothelial cells, acting independently of the Sigma-1 receptor, with effective concentrations of 10, 50, and 100 μM[2].
BD-1063 dihydrochloride (100 μM; 30 min) inhibits calcium influx through TRPC5 channels overexpressed in HEK 293 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BD-1063 (4-16 mg/kg; subcutaneous injection) dihydrochloride completely reverses carrageenan (HY-125474)-induced inflammatory mechanical hyperalgesia and thermal hyperalgesia in wild-type CD-1 mice via a σ1 receptor-mediated mechanism, with ED50 values of 4 mg/kg and 6 mg/kg, respectively, and does not affect nociceptive pain in non-inflamed mice[3].
BD-1063 (25-75 μg/paw; intraplantar injection) dihydrochloride fully reverses carrageenan (HY-125474)-induced mechanical hyperalgesia and thermal hyperalgesia in wild-type CD-1 mice via a σ1 receptor-mediated mechanism, without producing systemic effects[3].
BD-1063 (4.4-11 mg/kg; subcutaneous injection) dihydrochloride reduces ethanol self-administration behavior in male Wistar rats with ethanol dependence during acute withdrawal in a dose-dependent manner, and the 11 mg/kg dose produces significant inhibitory effects in all test subjects[4].
BD-1063 (3-11 mg/kg; subcutaneous injection) dihydrochloride reduces ethanol self-administration in genetically selected male Sardinian alcohol-preferring rats in a dose-dependent manner, with significant inhibitory effects observed at doses of 4.4 mg/kg and higher[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 206996-13-6
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Appearance Solid
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Masse moléculaire 346.12
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Formule C13H20Cl4N2
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Color White to off-white
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SMILES
CN1CCN(CCC2=CC=C(Cl)C(Cl)=C2)CC1.Cl.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Arch Toxicol
2024 Oct;98(10):3323-3336. PMID: 38896176 -
Neurobiol Dis
Sigma-1 receptor maintains ATAD3A as a monomer to inhibit mitochondrial fragmentation at the mitochondria-associated membrane in amyotrophic lateral sclerosis. [Abstract]2023 Apr:179:106031. PMID: 36736924 -
J Virol
SARS-CoV-2 NSP6 reduces autophagosome size and affects viral replication via sigma-1 receptor. [Abstract]2024 Nov 19;98(11):e0075424. PMID: 39445785
Solvant et solubilité
H2O : 100 mg/mL (288.92 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (288.92 mM); Clear solution; Need ultrasonic
Protocole
Rats: BD1063 is solubilized in isotonic saline and injected subcutaneously (s.c. 1 ml/kg), 15 min before testing. Rats are pretreated with BD1063 (0, 4.4, 7 and 11 mg/kg of body weight, free base weights, s.c.) using a within-subject Latin square design. sP rats: Rats are pretreated with BD1063 (0, 3, 4.4, 7 and 11 mg/kg of body weight, free base basis, s.c.) using a within-subject Latin square design[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Espinosa-Juárez JV, et al. Sigma-1 receptor antagonist (BD-1063) potentiates the antinociceptive effect of quercetin in neuropathic pain induced by chronic constriction injury. Drug Dev Res. 2021;82(2):267-277. [Content Brief]
[2]. Amer MS, et al. Inhibition of endothelial cell Ca²⁺ entry and transient receptor potential channels by Sigma-1 receptor ligands. Br J Pharmacol. 2013;168(6):1445-1455. [Content Brief]
[3]. Tejada MA, et al. Sigma-1 receptor inhibition reverses acute inflammatory hyperalgesia in mice: role of peripheral sigma-1 receptors. Psychopharmacology (Berl). 2014;231(19):3855-3869. [Content Brief]
[4]. Sabino V, et al. The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking. Neuropsychopharmacology. 2009;34(6):1482-1493. [Content Brief]
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.8892 mL | 14.4459 mL | 28.8917 mL | 72.2293 mL |
| 5 mM | 0.5778 mL | 2.8892 mL | 5.7783 mL | 14.4459 mL | |
| 10 mM | 0.2889 mL | 1.4446 mL | 2.8892 mL | 7.2229 mL | |
| 15 mM | 0.1926 mL | 0.9631 mL | 1.9261 mL | 4.8153 mL | |
| 20 mM | 0.1445 mL | 0.7223 mL | 1.4446 mL | 3.6115 mL | |
| 25 mM | 0.1156 mL | 0.5778 mL | 1.1557 mL | 2.8892 mL | |
| 30 mM | 0.0963 mL | 0.4815 mL | 0.9631 mL | 2.4076 mL | |
| 40 mM | 0.0722 mL | 0.3611 mL | 0.7223 mL | 1.8057 mL | |
| 50 mM | 0.0578 mL | 0.2889 mL | 0.5778 mL | 1.4446 mL | |
| 60 mM | 0.0482 mL | 0.2408 mL | 0.4815 mL | 1.2038 mL | |
| 80 mM | 0.0361 mL | 0.1806 mL | 0.3611 mL | 0.9029 mL | |
| 100 mM | 0.0289 mL | 0.1445 mL | 0.2889 mL | 0.7223 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
BD-1063 dihydrochloride Related Classifications
HY-18101A Related Classifications
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