奥卡哌酮 - CAS:129029-23-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	奥卡哌酮
英文名称:	Ocaperidone
别名:	3-[2-[4-(6-氟苯并[d]异恶唑-3-基)哌啶-1-基]乙基]-2,9-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮 R79598
CAS No:	129029-23-8	分子式:	C₂₄H₂₅FN₄O₂	分子量:	420.48
CAS No:	129029-23-8
分子式:	C₂₄H₂₅FN₄O₂
分子量:	420.48
MDL:	MFCD00866668

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

O10238 奥卡哌酮 ≥98% (psaitong)

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包装规格：

100mg in glass bottle

溶解性：

溶于DMSO（16.67mg/mL 超声）

产品描述：

基本信息

产品编号：	O10238
产品名称：	Ocaperidone
CAS:	129029-23-8	储存条件	粉末	-20℃	四年

分子式：	C24H25FN4O2		溶于液体	-80℃	6个月
分子量	420.48			-20℃	1个月
化学名：	3-(2-(4-(6-Fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-2,9-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
Solubility (25°C)：
体外:	DMSO	15mg/mL (35.67mM; Need ultrasonic)
	Ethanol
	Water
体内(现配现用):	请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80 →45% saline Solubility: ≥ 1.67 mg/mL (3.97mM); Clear solution
	此⽅案可获得 ≥ 1.67 mg/mL (3.97mM，饱和度未知) 的澄清溶液。以 1mL ⼯作液为例，取 100μL 16.699999 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50μL Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。
	请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility: 1.67 mg/mL (3.97mM); Suspended solution; Need ultrasonic
	此⽅案可获得 1.67 mg/mL (3.97mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。以 1mL ⼯作液为例，取 100μL 16.699999 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.3782mL	11.8912mL	23.7823mL
5mM	0.4756mL	2.3782mL	4.7565mL
10mM	0.2378mL	1.1891mL	2.3782mL

生物活性

产品描述	一种有效的安定剂，为 5-HT2 和多巴胺 D2 的拮抗剂，5-HT1A 的激动剂，对 5-HT2，a1-adrenergic 受体，dopamine D2，组胺 H1 和 a2-adrenergic 受体的 Ki 值分别为 0.14nM，0.46nM，0.75nM，1.6nM 和 5.4nM，对 h5-HT1A 的 pEC50 和 pKi 值分别为 7.60 和 8.08。
靶点	5-HT2 Receptor 0.14nM (Ki)	D2 Receptor 0.75nM (Ki)	5-HT1A Receptor 7.6 (pEC50, h5-HT1A)	5-HT1A Receptor 8.08 (pKi, h5-HT1A)
靶点	a1-adrenergic receptor 0.46nM (Ki)	Histamine H1 1.6nM (Ki)	a2-adrenergic receptor 5.4nM (Ki)
体外研究	Ocaperidone has high affinify at 5-HT2 and dopamine D2, with Kis of 0.14nM, 0.46nM, 0.75nM, 1.6nM and 5.4nM for 5HT2, a1 -adrenergic, dopamine D2, histamine H1 and a2-adrenergic, respectively. Ocaperidone shows 5-HT1A receptor agonist activity, with a pEC50 and pKi of 7.60 and 8.08.
体内研究	Ocaperidone shows a potent occupation of 5HT2 receptor via in vivo binding in the frontal cortex of rats with an ED50 of 0.04 mg/kg, and 0.1 4-0.1 6 mg/kg for D2 receptor in the striatum and the nucleus accumbens. Ocaperidone (R 79598) antagonizes dopamine D2 and 5-HT2, and shows a a partial generalization to buspirone with an ED50 of 0.163 mg/kg .

推荐实验方法(仅供参考)

Kinase Assay

The membranes are prepared from frozen HA7 cells. Cells are harvested in ice-cold Tris-HCl pH 7.4, homogenized and centrifuged at 40 000×g, 4°C for 10 min. The pellet is suspended in the same buffer and centrifuged again. After the second centrifugation, the pellet is suspended in an assay buffer consisting of pargyline (10μM) and CaCl2 (4mM) in Tris-HCl (50mM, pH 7.4). Membrane protein, 0.031-0.084 mg/tube, is incubated with [3H] 8-OH-DPAT (1nM final concentration) and Ocaperidone at seven concentrations, for 30 min, room temperature. The reaction is terminated by filtration through Whatman filters, and radioactivity is counted by liquid scintillation spectrometry. The experiments are performed in triplicate. Data are analyzed using the non-linear curve fitting program EBDA/LIGAND. Results expressed as pKi values are means of three determinations.

Animal Administration

Rats

Male Wistar rats (200 g) are treated subcutaneously with various dosages (0.01-10 or 2.5-40 mg/kg) of Ocaperidone dissolved in saline (injection of 1mL of drug solution/100 g of body weight) or with saline (control); 1 hr thereafter the rats receive 1 μ g/kg (5-10μCi) [3H]spiperone by intravenous injection in the tail vein. The rats are sacrificed by decapitation 1 hr after the [3 H]spiperone injection; the striatum, the nucleus accumbens, the tuberculum olfactorium, the frontal cortex, and the cerebellum are immediately dissected. The tissues are cooled on ice, weighed, and dissolved in 10mL of Instagel II, in plastic counting vials. After 48 hr the radioactivity is counted; data are expressed in dpm, using external standard counting and referring to a quenched standard curve. The counted radioactivity is converted to pg of [3H]spiperone/mg of tissue. Four to six animals are treated at each drug dosage. For each drug and brain area, the values are averaged and graphically plotted versus the logarithm of the drug dosages. On each graph, values measured in the cerebellum are plotted; labeling in the cerebellum is taken as an indication of nonspecific tissue labeling.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果