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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- Purity : 98.0%
- CAS No.: 206996-13-6
- 화학식: C13H20Cl4N2
- 분자량:346.12
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보관:
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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BD-1063 dihydrochloride
MoreAll Sigma Receptor Isoforms
More
Biological Activity
제품 설명
IC50 & Target
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Sigma 1 Receptor |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
In Vivo
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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분자량 346.12
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
용액&용해도
In Vitro:
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)
In Vivo:
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
Protocol
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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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