AM-0902 - CAS:1883711-97-4 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	AM-0902
英文名称:	AM-0902
别名:	1-((3-(4-氯苯乙基)-1,2,4-恶二唑-5-基)甲基)-7-甲基-1H-嘌呤-6(7H)-酮 1-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl-6H-Purin-6-one
CAS No:	1883711-97-4	分子式:	C₁₇H₁₅ClN₆O₂	分子量:	370.79
CAS No:	1883711-97-4
分子式:	C₁₇H₁₅ClN₆O₂
分子量:	370.79

点击下载产品说明书(PDF)

A12351 AM-0902 ≥98% (psaitong)

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包装规格：

5mg 10mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO(2mg/mL)

产品描述：

基本信息

产品编号：	A12351
产品名称：	AM-0902
CAS:	1883711-97-4	储存条件	粉末	-20℃	四年

分子式：	C17H15ClN6O2		溶于液体	-80℃	6个月
分子量：	370.79			-20℃	1个月
化学名：	1-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl-6H-Purin-6-one
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	2.6969mL	13.4847mL	26.9694mL
5mM	0.5394mL	2.6969mL	5.3939mL
10mM	0.2697mL	1.3485mL	2.6969mL

生物活性

产品描述	一种有效的选择性瞬时受体电位A1(TRPA1)
靶点	IC50:71nM (rTRPA1),131nM (hTRPA1)
体外研究	AM-0902 is a potent,selective antagonist of TRPA1 with IC50s of 71 and 131nM for rTRPA1 and hTRPA1,respectively.AM0902 is highly permeable (average Papp=44.5μcm/s in MDCK cells),an unlikely substrate for P-gp (efflux ratio=1.3 in P-gp overexpressing MDCK cells),and demonstrates good solubility (PBS pH 7.4:226μM,SIF:248μM).AM-0902 shows good selectivity over other TRP channels,as no activity is observed against human TRPV1 or TRPV4,or rat TRPV1,TRPV3,or TRPM8,at concentrations up to 10μM.AM-0902 inhibits 45Ca2+flux upon activation of rat TRPA1 with methylglyoxal with an IC50 of 0.019μM.
体内研究	AM-0902 is a potent,selective antagonist of TRPA1 in vivo.AM-0902 has moderate terminal elimination half-life (t1/2=0.6h and 2.8h for rat (0.5mg/kg,iv),rat (30mg/kg,oral)).A dose-dependent reduction of allyl isothiocyanate (AITC)-induced flinching is observed for AM-0902,with a significant reduction in flinching observed postdosing of 10 and 30mg/kg.The unbound plasma concentrations (Cu) at 1h for the 1,3,10,and 30mg/kg doses are 0.051±0.024 (n=8),0.19±0.11 (n=8),0.58±0.35 (n=8),and 2.2±0.40 (n=8)μM,covering the in vitro rat TRPA1 45Ca2+ IC50 at 0.72,2.7,8.2,and 30.3 fold,respectively.A good exposure-response relationship is observed in this target coverage model.An unbound in vivo IC50 of 0.35μM,which is in good agreement with the in vitro rat TRPA1 45Ca2+ IC50,and unbound in vivo IC90 of 1.7μM are determined.It is noteworthy that at a dose of 30mg/kg,AM-0902 engages TRPA1 at concentrations that exceed the in vivo IC90,making it a useful tool for exploration of in vivo models of acute pain.

推荐实验方法(仅供参考)

细胞实验:

MDCK cells are generated and maintained for the TRPA1 calcium flux assays.On the day of assay,culture media is removed and cells are incubated for 10 min at room temperature (RT) with 50μL of AM-0902 (compound 27) in AM-0902 dilution buffer [HBSS containing 1mM HEPES+0.1mg/mL BSA] at final concentrations (2.0nM to 40μM,1:3 ratio),followed by another 3 min incubation at RT.The reaction mixture is aspirated,and cells are washed three times with phosphate buffer saline (PBS) containing 0.1mg/mL BSA.Radioactivity is measured using a TopCount microplate scintillation counter.The activation of TRPA1 is measured by the cellular uptake of radioactive calcium.

动物实验:

Rats

Rats are dosed orally with either vehicle (2% HPMC/1% Tween-80) or AM-0902 at 1,3,10,or 30mg/kg.After 1h,one left ventral hind paw is injected with the TRPA1 agonist AITC (0.1%).AM-0902 is also given by an intravenous (IV) injection to rats (0.5mg/kg).

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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