BD 1008 dihydrobromide
目录号 : GC16595
An Analytical Reference Standard
Cas No.:138356-09-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 138356-09-9 | SDF | |
| 化学名 | N-(3,4-dichlorophenethyl)-N-methyl-2-(pyrrolidin-1-yl)ethanamine dihydrobromide | ||
| Canonical SMILES | ClC1=CC(CCN(C)CCN2CCCC2)=CC=C1Cl.Br.Br | ||
| 分子式 | C15H22Cl2N2.2HBr | 分子量 | 463.08 |
| 溶解度 | Water: 50mM | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1595 mL | 10.7973 mL | 21.5945 mL |
| 5 mM | 0.4319 mL | 2.1595 mL | 4.3189 mL |
| 10 mM | 0.2159 mL | 1.0797 mL | 2.1595 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。