| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
BD1047 dihydrobromide (BD-1047) is a selective functional antagonist of sigma receptors (σ receptors) with antipsychotic activity and may be used for schizophrenia. BD 1047 is demonstrated to attenuate the dystonia produced by the high affinity σ receptor ligands di-o-tolylguanidine and Haloperidol. BD 1047 is described to have similar activity at the σ-1 receptor to BD 1063 (sc-203838) and to show higher affinity at σ-2 than BD 1063. BD 1047 is demonstrated to antagonize the effects of Trazodone on neurotransmitter release. BD 1047 did not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. Likewise, it did not modify the hyperactivity induced by NMDA receptor antagonists, phencyclidine, memantine or dizocilpine. On the other hand, BD 1047 attenuated apomorphine-induced climbing in mice and phencyclidine-induced head twitches in rats, like rimcazole and panamesine did. Summing up, BD 1047 shows a moderate activity in models used in this study suggesting that its usefulness as an antipsychtic drug is doubtful. However, more detailed studies are required for definitive confirmation of this conclusion.
| ln Vitro |
Cutamesine lowers the rate of cell death brought on by light exposure in mouse photoreceptor-derived 661w cells when BD-1047 (dihydrobromide) is administered[2]. Cutamesine lowers the elevated level of caspase 3/7 activity and mitochondrial damage, but BD-1047 (dihydrobromide) attenuates this effect[2].
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| ln Vivo |
At a dose of 10 mg/kg, BD-1047 (dihydrobromide) (1–10 mg/kg; ip) reduces the climbing behavior in mice induced by apomorphine (APO)[1]. ?The antidepressant-like effect caused by co-administration of pramipexole and sertraline (but not pramipexole and fluoxetine) is countered by BD-1047 (dihydrobromide)[3]. ?Dihydrobromide, or BD-1047, reverses the potentiation of Sig-1 R agonists in NMDA-induced pain behavior and pNR1 immunoreactivity, as well as the increasing expression of pNR1[4].
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| Animal Protocol |
Animal/Disease Models: Male Albino Swiss mice (50 days old, 25–28 g)[1]
Doses: 1 mg/kg, 3 mg/kg, 10 mg/kg Route of Administration: intraperitoneal (ip)injection Experimental Results: diminished the APO-induced climbing at the dose of 10 mg/kg in mice. |
| References |
[1]. Skuza G, et al. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 2006 Sep-Oct;58(5):626-635.
[2]. Shimazawa M, et al. Effect of a sigma-1 receptor agonist, cutamesine dihydrochloride (SA4503), on photoreceptor cell death against light-induced damage. Exp Eye Res. 2015 Mar;132:64-72. [3]. Rogóz Z, et al. Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep. 2006 Jul-Aug;58(4):493-500. |
| Molecular Formula |
C13H20CL2N2.2HBR
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| Molecular Weight |
437.04
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| CAS # |
138356-21-5
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| Related CAS # |
138356-20-4;138356-21-5 (HBr);
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| SMILES |
Br[H].Br[H].ClC1=C(C([H])=C([H])C(=C1[H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])Cl
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 33.33 mg/mL (76.26 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2881 mL | 11.4406 mL | 22.8812 mL | |
| 5 mM | 0.4576 mL | 2.2881 mL | 4.5762 mL | |
| 10 mM | 0.2288 mL | 1.1441 mL | 2.2881 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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