SR144528 - CAS:192703-06-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	SR144528
英文名称:	SR144528
别名:	角鲨烯-D6 (1S-endo)-5-(4-Chloro-3-methylphenyl)-1-((4-methylphenyl)methyl)-N-(1,3,3-trimethylbicyclo(2.2.1)hept-2-yl)-1H-pyrazole-3-carboxamide
CAS No:	192703-06-3	分子式:	C₂₉H₃₄ClN₃O	分子量:	476.05
CAS No:	192703-06-3
分子式:	C₂₉H₃₄ClN₃O
分子量:	476.05

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

S10851 SR144528 ≥98% (psaitong)

相关产品

包装规格：

100mg in glass bottle

溶解性：

溶于DMSO（50mg/mL 超声）

产品描述：

基本信息

产品编号：	S10851
产品名称：	SR144528
CAS:	192703-06-3	储存条件	粉末	-20℃	四年

分子式：	C29H34ClN3O		溶于液体	-80℃	6个月
分子量：	476.05			-20℃	1个月
化学名：	1H-pyrazole-3-carboxamide,5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜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	2.1006mL	10.5031mL	21.0062mL
5mM	0.4201mL	2.1006mL	4.2012mL
10mM	0.2101mL	1.0503mL	2.1006mL

生物活性

产品描述	一个有效且选择性的 CB2 受体拮抗剂，其 Ki 值为 0.6nM。
靶点	Ki:0.6nM (CB2 receptor)
体外研究	SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6nM.SR144528 alone is able to stimulate in a concentration-dependent manner (EC50=26±6nM,two experiments) the forskolin-sensitive adenylyl cyclase activity in CHOCB2 cells with a maximum effect at 1μM (4-fold stimulation) whereas at this concentration it has no significant effect on CHO-CB1 cells (15% inhibition).Raw 264.7 macrophages supplemented with SR144528 display reduced caspase-3 activity.SR144528 inhibits microsomal acyl-coenzymeA:cholesterol acyltransferase (ACAT) activity in a concentration-dependent manner with an IC50 value of 3.6±1.1μM.At 10μM,SR144528 inhibits ACAT activities ~68%.
体内研究	No effect on the binding of [3H]-CP 55,940 to its specific sites in the brain is observed after either oral (up to 10mg/kg) or i.c.v.(10μg/animal) administration of SR144528 in mice.The occupancy by SR144528 of the spleen cannabinoid receptor is time-dependent and significant for at least 18 hours after oral administration at 3mg/kg.SR144528 does not induce any significant effect on gastrointestinal (GI) motility when given alone.SR144528 does not block but enhances delayedgastric emptying.

推荐实验方法(仅供参考)

激酶实验：

MAP kinase activity is measured. Briefly, cells grown to 80% confluence are maintained in culture medium containing 0.5% foetal calf serum for 24 hour prior to the application of ligands.CHO CB1 or -CB2 cells previously washed with PBS are incubated at 37℃ in the absence (basal activity) or in the presence of SR144528 (10-9 to 3×10-6 M) for 20 min.Cells are then washed at 4℃ with 0.5mL of buffer A [50mM Tris-HCl,pH 7.5,150mM NaCl,1mM ethyleneglycol-bis-(β-aminoethyl ether) N,N,N′,N-tetraacetic acid,1mM Na3PO4] and lysed for 15 min in buffer A supplemented with 1% triton X-100,10μg/mL aprotinin,10μg/mL,leupeptin,1mM dithiothreitol and 1mM phenylmethylsulfonyl fluoride.The solubilized cell extracts are then clarified by centrifugation at 14,000×g for 15 min at 4℃. Aliquots (15μL) are removed and stored at -80℃ until use.Phosphorylation assays are carried out at 30℃ for 30 min (linear assay conditions) with γ [33P]ATP by using the p42/p44 MAP kinase enzyme system.The radioactivity incorporated is determined by liquid scintillation counting.

细胞实验:

cAMP accumulations are carried out in CHO-CB1 or -CB2 cells.Cells are washed with phosphate-buffered saline (PBS) and incubated for 15 min at 37℃ in 1mL of PBS in the absence or in the presence of SR144528 (3×10-9 to 10-5M).Forskolin (3μM final concentration) is added and cells are incubated for another 20 min at 37℃.The reaction is terminated by rapid aspiration of the assay medium and addition of 1.5mL of ice-cold 50mM Tris-HCl,pH 8,4mM ethylenediaminetetraacetic acid.Dishes are placed on ice for 5 min and then the extracts are transferred to a glass tube.Extracts are boiled and centrifuged for 10 min at 3500g to eliminate cell debris.Aliquots from supernatant are dried and the cAMP concentration is determined by radioimmunoassay by using the scintillant proximity assay system.The basal activity is determined in the absence of forskolin.

动物实验:
Male Wistar rats (240 to 300g) are used in this study.One week after the animals arrived at the laboratory,three different sets of experiments are carried out.In the third set of experiments,SR144528 (1mg/kg i.p.) is administered in rats.The effect of SR144528 is also analyzed in vehicle-treated rats.SR144528 volume is adjusted to a maximum of 4 to 5mL/kg.

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