| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BD-1063 (10–100 μM; 30 min) inhibited sustained calcium influx in human saphenous vein endothelial cells induced by histamine, VEGF, or H2O2, with effects independent of Sigma-1 receptors, at effective concentrations of 10, 50, and 100 μM [2]. BD-1063 (100 μM; 30 min) inhibited calcium influx mediated by TRPC5 channels overexpressed in HEK 293 cells [2].
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| ln Vivo |
BD-1063 (5.6-56.2 mg/kg; subcutaneous injection) produced dose-dependent anti-ectopic pain and anti-hyperalgesia effects in a rat CCI neuropathic pain model, with an ED50 value of 28.8 mg/kg for anti-hyperalgesia and 18.2 mg/kg for anti-ectopic pain; it also had a synergistic effect with quercetin hydrate [1]. BD-1063 (4-16 mg/kg; subcutaneous injection) completely reversed carrageenan-induced inflammatory mechanoalgesia and thermal hyperalgesia in wild-type CD-1 mice through a σ1 receptor-mediated mechanism, with ED50 values of 4 mg/kg and 6 mg/kg, respectively, and had no effect on nociceptive pain in non-inflammatory mice [3]. BD-1063 (25-75 μg/paw; plantar injection) completely reversed carrageenan-induced mechanical 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) reduced ethanol self-administration behavior in male Wistar rats during acute withdrawal in a dose-dependent manner, with a significant inhibitory effect observed at 11 mg/kg in all subjects [4]. BD-1063 (3-11 mg/kg; subcutaneous injection) reduced ethanol self-administration behavior in genetically selected male Sardinian alcoholics rats in a dose-dependent manner, with significant inhibitory effects observed at doses of 4.4 mg/kg and above [4].
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| Animal Protocol |
Animal/Disease Models:CD-1 mice (female, wild-type, 25-30 g, carrageenan-induced inflammatory hyperalgesia model) [3]
Doses: 4 mg/kg; 8 mg/kg; 16 mg/kg Route of Administration: Subcutaneous injection; single dose Experimental Results: Dose-dependent reversal of inflammatory mechanical and thermal hyperalgesia resulted in a response latency approaching that of the non-inflammatory control mice. The ED50 for reversing mechanical hyperalgesia was 4 mg/kg. The ED50 for reversing thermal hyperalgesia was 6 mg/kg. There was no significant difference in maximum analgesic effect (Emax) between the two sensory modalities and 100% recovery. At doses that completely reversed hyperalgesia (8 mg/kg for mechanical hyperalgesia and 16 mg/kg for thermal hyperalgesia), the response latency of non-inflammatory mice was not altered. Subcutaneous injection of the σ1 receptor agonist PRE-084 can completely eliminate its anti-hyperalgesic effect in a dose-dependent manner. Animal/Disease Models:Wistar rats (male, weighing 300 g at the start of the study, induced with alcohol dependence by intermittent 14-hour daily ethanol vapor exposure for 6 weeks) [4] Doses: 4.4 mg/kg; 7 mg/kg; 11 mg/kg Route of Administration: Subcutaneous injection; single dose (15 minutes before the test) Experimental Results: Ethanol self-administration decreased in a dose-dependent manner. Compared with the solvent group, the 7 mg/kg and 11 mg/kg dose groups had significantly lower ethanol intake and lever presses. Ethanol self-administration was reduced by 49% in low-response-dependent rats and by 34% in high-response-dependent rats. Self-administration via drinking water was not changed. |
| References |
|
| Molecular Formula |
C13H18CL2N2
|
|---|---|
| Molecular Weight |
273.20
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| CAS # |
150208-28-9
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
ClC1=CC=C(C=C1Cl)CCN2CCN(C)CC2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6603 mL | 18.3016 mL | 36.6032 mL | |
| 5 mM | 0.7321 mL | 3.6603 mL | 7.3206 mL | |
| 10 mM | 0.3660 mL | 1.8302 mL | 3.6603 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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