BMY 14802是一种 sigma-1 受体 (σ1R) 的拮抗剂,同时也是 5-HT 1A 受体和 α-1 肾上腺素能受体的激动剂。该化合物在帕金森病 (PD) 的大鼠模型中可抑制异常不自主运动 (AIM),并下调其表达,适用于帕金森病的研究。
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产品名称 | Adrenergic Receptor ↓ ↑ | α-adrenergic receptor ↓ ↑ | β-adrenergic receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ivabradine HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Maprotiline hydrochloride | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Cisatracurium besylate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Yohimbine HCI | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BMY 7378 |
++
α1D-adrenoceptor, pKi: 5.1 α2C-adrenoceptor, pKi: 6.54 |
+
β1-adrenoceptor, pIC50: 5.1 |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Asenapine maleate |
++++
α2A-adrenergic receptor, pKi: 8.9 α2B-adrenergic receptor, pKi: 8.9 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Piribedil |
++
adrenoceptor α2C, pKi: 7.2 adrenoceptor α2A, pKi: 7.1 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Prazosin HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Silodosin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Phenoxybenzamine HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Naftopidil |
+++
α1A-adrenergic receptor, Ki: 3.7 nM α1D-adrenergic receptor, Ki: 20 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Naftopidil 2HCl |
+
α1-adrenergic receptor, IC50: 0.2 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Alfuzosin HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Terazosin HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Atipamezole | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Phentolamine methanesulfonate salt | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Doxazosin mesylate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Tolazoline HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Zenidolol hydrochloride |
++++
β2-adrenergic receptor, Ki: 0.7nM β1-adrenergic receptor, Ki: 611nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | 5-HT ↓ ↑ | 5-HT1 ↓ ↑ | 5-HT2 ↓ ↑ | 5-HT3 ↓ ↑ | 5-HT5 ↓ ↑ | 5-HT6 ↓ ↑ | 5-HT7 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Desvenlafaxine |
++
5-HT, Ki: 40.2 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Lamotrigine |
+
5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Venlafaxine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Fluvoxamine maleate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Iloperidone | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ziprasidone HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Atomoxetine HCI |
+
5-HT, Ki: 77 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Dapoxetine HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Trazodone | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Clomipramine HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mirtazapine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Escitalopram oxalate |
+++
5-HT, Ki: 0.89 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Duloxetine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Sertraline HCl |
++
5-HT, Ki: 13 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Citalopram HBr |
+++
serotonin reuptake, IC50: 1.8 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Latrepirdine 2HCl | ✔ | GluR | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Fluoxetine HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Paroxetine hydrochloride | ✔ | AChR | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
BMY 7378 |
++
5-HT1D, pIC50: 5.9 5-HT1A, pIC50: 6.4 |
+
5-HT2, pIC50: 5.5 |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Flibanserin |
+++
5-HT1A, Ki: 1 nM |
+
5-HT2A, Ki: 49 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
LY310762 |
+
5-HT1D, Ki: 249 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Cyclobenzaprine HCI | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Blonanserin |
+++
5-HT2, Ki: 3.98 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Cyproheptadine HCl |
++++
5-HT2, IC50: 0.6 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Olanzapine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Pimavanserin hemitartrate |
+++
5-HT2A, pIC50: 8.7 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ketanserin |
+++
5-HT2C (Rat), Ki: 50 nM 5-HT2C (Human), Ki: 2.5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Loxapine succinate |
++
5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Agomelatine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Clozapine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Amitriptyline |
+
5-HT2, Ki: 235 nM |
SERT | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
PRX-08066 maleate |
+++
5-HT2B, IC50: 3.4 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
RS-127445 |
++++
5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Sarpogrelate HCl |
++++
5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Tropisetron | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Palonosetron | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ramosetron HCl |
++++
5-HT3 receptor, Ki: 0.091 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ondansetron | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Granisetron | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Alosetron HCl | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ondansetron hydrochloride dihydrate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
VUF10166 |
++++
5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Azasetron hydrochloride |
++++
5-HT3, IC50: 0.33 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Asenapine maleate |
+++
5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6 |
++++
5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46 |
+++
5-HT5A, pKi: 8.84 |
++++
5-HT6, pKi: 9.6 |
++++
5-HT7, pKi: 9.94 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||
Risperidone |
++
5-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 nM |
++++
5-HT2C, Ki: 12 nM 5-HT2A, Ki: 61.9 nM |
+
5-HT5A, Ki: 206 nM |
++
5-HT7, Ki: 6.6 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
SB 271046 HCl |
+++
5-HT6, pKi: 8.92 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Intepirdine |
++++
5-HT6, pKi: 9.63 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SB-269970 HCl |
++
5-HT7, pKi: 8.3 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BRL 15572 |
++
5-HT1D, pKi: 6 5-HT1B, pKi: 6.1 |
++
5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2 |
+
5-HT6, pKi: 5.9 |
+
5-HT7, pKi: 6.3 |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 mitigates abnormal involuntary movement (AIM) in a rat model of Parkinson's disease (PD) by downregulating AIM expression[1].[2]. |
体内研究 | A single intraperitoneal dose of BMY 14802 (15 mg/kg) significantly curtails AIM and reduces dyskinesias, particularly noticeable within the first hour in the rat PD model[1].[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.87mL 0.57mL 0.29mL |
14.35mL 2.87mL 1.44mL |
28.70mL 5.74mL 2.87mL |
CAS号 | 105565-56-8 |
分子式 | C18H22F2N4O |
分子量 | 348.39 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(143.52 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |