| BD 1008 dihydrobromideδ1-receptor antagonist,potent and selective |

Sample solution is provided at 25 µL, 10mM.
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Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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Chemical structure


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| Cas No. | 138356-09-9 | SDF | Download SDF |
| Chemical Name | N-(3,4-dichlorophenethyl)-N-methyl-2-(pyrrolidin-1-yl)ethanamine dihydrobromide | ||
| Canonical SMILES | ClC1=CC(CCN(C)CCN2CCCC2)=CC=C1Cl.Br.Br | ||
| Formula | C15H22Cl2N2.2HBr | M.Wt | 463.08 |
| Solubility | Soluble in H2O | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
BD 1008 dihydrobromide is a potent and selective ligand for σ-receptor with Ki values of 2 and 8 nM for σ-1 receptor and σ-2 receptor, respectively [1].
σ-receptor is a type of opioid receptor. There are two subtypes of σ-receptor: σ-1 and σ-2 [2].
BD 1008 dihydrobromide is a potent and selective σ-receptor ligand. BD1008 showed high affinity to sites labeled by 4-[125I]PEMP with Ki value of 5.06 nM in guinea pig brain membranes. In MCF-7 breast cancer and melanoma (A375) cells, 4-[125I]PEMP inhibited the binding of BD1008 with Ki value of 11 nM in a dose-dependent way [2]. In Xenopus oocytes coexpressed N-methyl-D-aspartate (NMDA) receptor (NR) 1a with either NR2A, 2B or 2C, BD1008 inhibited NMDA-activated membrane current responses with IC50 values of 62, 18 and 120 μM for NR1a/2A, NR1a/2B and NR1a/2C respectively, which were due to direct effects on the receptor channel complex [3].
In mice, BD1008 (1 mg/kg) inhibited cocaine-induced locomotor activity with ED50 value increased from 6.50 mg/kg to 11.19 mg/kg [1].
References:[1]. McCracken KA, Bowen WD, Matsumoto RR. Novel sigma receptor ligands attenuate the locomotor stimulatory effects of cocaine. Eur J Pharmacol, 1999, 365(1): 35-38.[2]. John CS, Gulden ME, Vilner BJ, et al. Synthesis, in vitro validation and in vivo pharmacokinetics of [125I]N-[2-(4-iodophenyl)ethyl]-N-methyl-2-(1-piperidinyl) ethylamine: a high-affinity ligand for imaging sigma receptor positive tumors. Nucl Med Biol, 1996, 23(6): 761-766.[3]. Whittemore ER, Ilyin VI, Woodward RM. Antagonism of N-methyl-D-aspartate receptors by sigma site ligands: potency, subtype-selectivity and mechanisms of inhibition. J Pharmacol Exp Ther, 1997, 282(1): 326-338.
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目前大量制备单抗的方法主要有两大系统,一是动物体内生产法,这是国内外实验室所广泛采用;另一是体外培养法。
(1)动物体内生产单抗的方法
迄今为止,通常情况下均采用动物体内生产单抗的方法,鉴于绝大多数动物用杂交瘤均由BALB/c小鼠的骨髓瘤细胞与同品系的脾细胞融合而得,因此使用的动物当然首选BALB/c小鼠。本方法即将杂交瘤细胞接种于小鼠腹腔内,在小鼠腹腔内生长杂交瘤,并产生腹水,因而可得到大量的腹水单抗且抗体浓度很高。可见该法操作简便、经济,不过,腹水中常混有小鼠的各种杂蛋白(包括Ig),因此在很多情况下要提纯后才能使用,而且还有污染动物病毒的危险,故而最好用SPF级小鼠。
(2)体外培养生产单抗的方法
总体上讲,杂交瘤细胞系并不是严格的贴壁依赖细胞(anchoragedependentcell,ADC),因此既可以进行单层细胞培养,又可以进行悬浮培养。杂交瘤细胞的单层细胞培养法是各个实验室最常用的手段,即将杂交瘤细胞加入培养瓶中,以含10-15%小牛血清的培养基培养,细胞浓度以1×106-2×106/ml为佳,然后收集培养上清,其中单抗含量约10-50ug/ml。显然,这种方法制备的单抗量极为有限,无疑是不适用于单抗的大规模生产。要想在体外大量制备单抗,就必须进行杂交瘤细胞的大量(高密度)培养。单位体积内细胞数量越多,细胞存活时间越长,单抗的浓度就越高,产量就越大。
二、补体(complement,C)是存在于正常人和动物血清与组织液中的一组经活化后具有酶活性的蛋白质。早在19世纪末Bordet即证实,新鲜血液中含有一种不耐热的成分,可辅助和补充特异性抗体,介导免疫溶菌、溶血作用,故称为补体。补体是由30余种可溶性蛋白、膜结合性蛋白和补体受体组成的多分子系统,故称为补体系统(complementsystem)。根据补体系统各成分的生物学功能,可将其分为补体固有成分、补体调控成分和补体受体(CR)。

