SB-224289 hydrochloride - CAS:180084-26-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	SB-224289 hydrochloride
英文名称:	SB-224289 hydrochloride
别名:	SB-224289A
CAS No:	180084-26-8	分子式:	C₃₂H₃₂N₄O₃?HCl	分子量:	557.08
CAS No:	180084-26-8
分子式:	C₃₂H₃₂N₄O₃?HCl
分子量:	557.08
MDL:	MFCD06407944

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

S10802 SB-224289 hydrochloride ≥95% (普西唐-psaitong)

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包装规格：

10mg in glass bottle

溶解性：

溶于DMSO（14.29 mg/mL 超声）

产品描述：

基本信息

产品编号：	S10802
产品名称：	SB-224289 hydrochloride
CAS:	180084-26-8	储存条件	粉末	-20℃	四年

分子式：	C32H33ClN4O3		溶于液体	-80℃	6个月
分子量	557.08			-20℃	1个月
化学名：	[4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl]-(1'-methylspiro[6,7-dihydro-2H-furo[2,3-f]indole-3,4'-piperidine]-5-yl)methanone;hydrochloride
Solubility (25°C)：
体外:	DMSO	14.29 mg/mL (25.65mM; Need ultrasonic)
	Ethanol
	Water	Insoluble
体内(现配现用):	1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 1.43 mg/mL (2.57mM); Clear solution
	此⽅案可获得 ≥ 1.43 mg/mL (2.57mM，饱和度未知) 的澄清溶液。以 1mL ⼯作液为例，取 100μL 14.299999 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。
	2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 1.43 mg/mL (2.57mM); Clear solution
	此⽅案可获得 ≥ 1.43 mg/mL (2.57mM，饱和度未知) 的澄清溶液。以 1mL ⼯作液为例，取 100μL 14.299999 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。
	3.请依序添加每种溶剂：10% DMSO →90% corn oil Solubility: ≥ 1.43 mg/mL (2.57mM); Clear solution
	此⽅案可获得 ≥ 1.43 mg/mL (2.57mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以 1mL ⼯作液为例，取 100μL 14.299999 mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中，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	1.7951mL	8.9754mL	17.9507mL
5mM	0.3590mL	1.7951mL	3.5901mL
10mM	0.1795mL	0.8975mL	1.7951mL

生物活性

产品描述	一种选择性的 5-HT1B receptor 拮抗剂，具有抗焦虑作用。
靶点	5-HT1B Receptor
体外研究	SB-224289 has specific toxin-blocking ability and does not inhibit Cho1p. SB-224289 (100 μM-25μM) shows consistent efficacy at producing Pap-A resistance. SB-224289 does not directly inhibit the PS synthase enzyme in this in vitro assay. Moreover, SB-224289 specifically blocks the activity of papuamides and not other membrane disruptors. SB-224289 is unable to protect wild-type cells against KF, but it is able to provide protection against TPap-A. SB-224289 has a pKi of 8 at human cloned 5-HT1B receptors and displays more than 80 fold selectivity over the closely related 5-HT1D receptor and a range of other receptors. SB-224289 is a potent antagonist with pEC50 of 7.9±0.1. SB-224289 evokes a parallel rightward shift in the 5-HT concentration response curve with pA2 of 8.4±0.2. SB-224289 (100nM and 1μM) also significantly increases [3H]- 5HT release in electrically stimulated guinea-pig brain cortex slices
体内研究	SB-224289 (SB 224289) alone or in combination with cocaine, increases anxiety-like behavior. SB 224289 significantly reduces the amount of locomotor activity in the cocaine-treated rats. SB 224289-treated animals spend a significantly longer time in the corners than those treated with vehicle. SB 224289 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F-99101-induced hypothermia in the guinea-pig. SB 224289 (4 mg/kg, p.o) reverses sumatriptan-induced inhibition of 5- HT release showing that it is also a potent terminal 5-HT autoreceptor antagonist in vivo. SB 224289 (2-16 mg/kg, p.o) does not increase 5-HT levels in the fuinea-pig frontal cortex. However, SB 224289 (4 mg/kg, p.o) causes a significantly increase in levels of 5-HT in the fuinea-pig dentate gyrus.

推荐实验方法(仅供参考)

Animal Administration

Ninety minutes before each animal is tested, it receives an ip injection of either 5 mg/kg SB 224289 in a vehicle of 10% Trappsol in sterile water or vehicle alone (total volume 1mL/kg). This dosage of this drug is effective as a pharmacological agent. The rat is put back in its home cage until just before it is to be tested.

保存条件：

-20℃ 充氮保存

UN码：

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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