Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rauwolscine hydrochloride (Isoyohimbine hydrochloride) 是一种高选择性的 α2 adrenergic 受体拮抗剂,Ki=12 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
50 mg | ¥ 415 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 456 | 现货 |
产品描述 | Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5]. |
靶点活性 | α2-adrenoceptor:12 nM (Ki) |
体外活性 | [3H]Rauwolscine binding to the α2 adrenergic receptor is reversible, stcreospccific, and saturable. [3H]Rauwolscine specifically labels both the high and low-affinity states of the α2 adrenergic receptor in brain membranes[1]. [3H]Rauwolscine also behaves as a 5-HT1A receptor agonist, indicating that rauwolscine (as well as yohimbine) has agonistic properties at the level of 5-HT autoreceptors[2]. When using [3H]5-HT as a radioligand, rauwolscine is determined to have a relatively high affinity for the human receptor (Ki: 14.3/35.8 nM, for human and rat)[3]. Saturation studies show that the affinity of [3H]Rauwolscine is similar in mouse, rabbit, rat, dog (2.33-3.03 nM) except man where it is significantly higher (0.98 nM) [4]. |
激酶实验 | Fresh bovine frontal cortex is incubated in triplicate with [3H]Rauwolscine (82 Ci/mM, diluted). Incubation is terminated by filtration under reduced pressure over filters, which are then rinsed with ice-cold Tris-HCl buffer, dried overnight and added to disposable glass mini vials containing 3.0 mL of a 95% Econofluor/5% Protocol solution. Samples are counted by liquid scintillation spectrometry with an efficiency of 32%. (-)- [3H]Epinephrine binding to bovine cortex membranes is conducted at 25°C[1]. |
别名 | Corynanthidine hydrochloride, 盐酸育亨宾碱, 萝芙素盐酸盐, α-Yohimbine hydrochloride, Isoyohimbine hydrochloride |
分子量 | 390.9 |
分子式 | C21H27ClN2O3 |
CAS No. | 6211-32-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 13.75 mg/mL (35.18 mM), Heating is recommended.
H2O: 5 mM, Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 2.5582 mL | 12.791 mL | 25.582 mL | 63.955 mL |
5 mM | 0.5116 mL | 2.5582 mL | 5.1164 mL | 12.791 mL | |
DMSO | 10 mM | 0.2558 mL | 1.2791 mL | 2.5582 mL | 6.3955 mL |
20 mM | 0.1279 mL | 0.6395 mL | 1.2791 mL | 3.1977 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Rauwolscine hydrochloride 6211-32-1 GPCR/G Protein Neuroscience Adrenergic Receptor a-Yohimbine Hydrochloride α-Yohimbine Isoyohimbine Hydrochloride Corynanthidine Rauwolscine Inhibitor α-Yohimbine Hydrochloride Rauwolscine Hydrochloride Beta Receptor Corynanthidine Hydrochloride inhibit alpha-Yohimbine Hydrochloride Corynanthidine hydrochloride Isoyohimbine 盐酸育亨宾碱 萝芙素盐酸盐 α-Yohimbine hydrochloride Isoyohimbine hydrochloride inhibitor