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首页 >  新闻动态 >  阿拉丁小分子抑制剂、激动剂、拮抗剂---神经信号通路

阿拉丁小分子抑制剂、激动剂、拮抗剂---神经信号通路

发布时间:2020-10-13

阿拉丁小分子抑制剂、激动剂、拮抗剂---神经信号通路(上)

神经信号

      神经信号参与中枢神经系统的结构、功能、遗传和生理的调节。神经元合成/导入神经递质,并将其储存在突触前囊泡中。突触前神经元释放的小泡,进而传递神经冲动。常见的神经递质有γ氨基丁酸(GABA)、谷氨酸、血清素、多巴胺等。在神经信号通路中,这些神经递质的功能障碍可能多种神经系统疾病,如慢性疼痛、神经退行性疾病、失眠、精神障碍(精神分裂症、双相情感障碍、抑郁症和成瘾)等。

神经信号通路转导过程

      当受到来自环境或其他神经元的信号刺激时,神经递质受体通过G蛋白偶联信号通路和G蛋白非依赖机制激活下游细胞内信号通路:包括cAMP/PKA, PI3K/AKT, 磷脂酶A2(PLA2), 磷脂酶C(PLC)信号通路等。例如,多巴胺受体通过cAMP激活PKA等信号分子,通过CREB和其他转录因子的作用调控基因表达。其他神经递质如NMDAR或AMPAR与控制Ca2+和Na+流量的离子通道有关,这样就能在突触后神经元中传递动作电位。

神经信号通路图

产品列表

   *Aβ

项目号产品名称规格CAS包装细胞靶点IC50EC50
D126677DAPT≥98%208255-80-55mg,10mg,25mg,50mgHEK 293细胞γ-secretase20 nM
R127403RO4929097≥99%847925-91-15mg,10mg,50mg无细胞γ secretase4 nM
Aβ40
14 nM
Notch
5 nM
M126008MK-0752≥99%471905-41-65mg,10mg,50mg
γ-secretase5 nM
B126453Avagacestat (BMS-708163)≥99%1146699-66-25mg,10mg,50mg
Aβ400.3 nM
Aβ420.27 nM
L128069LY2811376≥99%1194044-20-65mg,10mg,50mg
BACE1
239 nM-249 nM

300 nM
H1088132-羟丙基-β-环糊精97%128446-35-55g,25g,100g,250g
amyloid-β aggregation

 

*5-HT受体

项目号产品名称规格CAS包装细胞靶点IC50KiED50pKi
F131623Fluoxetine HCl≥98%(HPLC)56296-78-71g,5g,25g
5-HT



V129637Venlafaxine hydrochloride≥98% (HPLC)99300-78-41g,5g,25g,100g
5-HT



D129639Dapoxetine hydrochloride≥98% (HPLC)129938-20-1250mg,1g,5g
5-HT



I125279Iloperidone≥98%133454-47-450mg,250mg,1g,5g
5-HT



V129787Vortioxetine (Lu AA21004) HBr≥98%960203-27-45mg,25mg,100mg
5-HT1A15 nM


5-HT1B33 nM


5-HT3A3.7 nM


5-HT719 nM


SERT1.6 nM


F129671Fluvoxamine maleate≥98%61718-82-9250mg,1g,5g,25g,100g
5-HT



S129789Sertraline HCl≥98% (HPLC)79559-97-01g,5g
5-HT
13 nM

L129555Lamotrigine≥98%84057-84-11g,5g人类血小板5-HT240 μM


大鼠脑突触体5-HT474 μM


C129687Clomipramine HCl≥99%17321-77-61g,5g,25g
SERT0.14 nM


NET54 nM


DAT3 nM


E122736草酸右旋西酞普兰98%219861-08-250mg,250mg,1g,5g
5-HT
0.89 nM

D123291盐酸度洛西汀≥98.0%(HPLC)136434-34-91g,5g,25g
5-HT
4.6 nM

M129386Milnacipran hydrochloride≥99%101152-94-710mg,50mg,250mg,500mg,1g,5g,25g
NET77 nM


SERT220 nM


A129730盐酸阿米替林≥98%549-18-81g,5g,25g,100g
5-羟色胺受体3.45 nM


去甲肾上腺素受体13.3 nM


5-HT47.31 nM


5-HT2235 nM


sigma 1受体287 nM


L174987Levomilnacipran hydrochloride97%175131-60-9100mg,250mg,1g





D1542623-(3,4-二羟基苯基)-2-甲基-L-丙氨酸倍半水合物>98.0%(HPLC)(T)555-30-65g,25g,100g
DOPA decarboxylase

21.8 mg/kg
C122737氢溴酸西酞98%59729-32-71g,5g
serotonin reuptake1.8 nM


V129637Venlafaxine hydrochloride≥98% (HPLC)93413-69-51g,5g,25g,100g
SNRI



D136408盐酸去甲咪嗪≥98%58-28-61g,5g,25g





T129695曲唑酮 盐酸盐98%25332-39-21g
5-HT



P137447Protriptyline Hydrochloride≥98%1225-55-425mg,100mg





A129721Atomoxetine HCl≥98%82248-59-750mg,250mg,1g
Norepinephrine (NE) transporter
5 nM

C126883氯氮平≥98%(GC)5786-21-0100mg,1g,5g,25g,100g
5-HT110 nM


O126519Olanzapine≥99%132539-06-11g,5g
5-HT2



D2 receptor



K129651Ketanserin≥97%74050-98-950mg,250mg,1g
5-HT2A
2.5 nM

5-HT2C (Rat)
50 nM

5-HT2C (Human)
100 nM

L129669Latrepirdine≥96%97657-92-65mg,10mg,50mg
GluR



Histamine receptor 



5-HT



A129730盐酸阿米替林≥98%50-48-61g,5g,25g,100g





A124691阿戈美拉汀≥98%(HPLC)138112-76-25mg,25mg,50mg,250mg,1g,5g,25g
5-HT2C 



A124739Asenapine maleate≥98% (HPLC)85650-56-210mg,50mg,250mg,1g





R127644Risperidone≥98%106266-06-2500mg,5g,25g,100g
5-HT2A
0.17 nM

α2c-adrenergic receptor 
1.3 nM

D2 receptor
3.57 nM

D3 receptor
3.6 nM

D2L Receptor
4.16 nM

E129717Ziprasidone HCl≥98%122883-93-6250mg,1g
5-HT receptor



Dopamine receptor



W129689WAY-100635 Maleate≥99%1092679-51-05mg,25mg,100mg
5-HT0.95 nM


B129706Blonanserin≥98% (HPLC)132810-10-725mg,100mg
5-HT2
3.98 nM

dopamine D2 receptor
14.8 nM

S125056SB269970 HCl-261901-57-910mg
5-HT7



S129658SB269970 HCl≥99%261901-57-910mg,50mg
5-HT7



G120176盐酸格拉司琼98%107007-99-810mg,50mg,1g,5g
5-HT3



M129297Mirtazapine≥98%85650-52-8100mg,1g
5-HT



S127746SB742457≥97%607742-69-85mg,25mg
5-HT6



B129690BRL-15572≥99%193611-72-25mg,10mg,50mg
5-HT1D


7.9
5-HT1A


7.7
5-HT2B


7.4
5-HT2A


6.6
5-HT7


6.3
P129785PRX-08066 Maleic acid≥99%866206-55-55mg,10mg,50mg
5-HT2B3.4 nM


T124762盐酸托烷司琼≥98.0%105826-92-4250mg,1g,5g
5-HT3



P129438Pizotifen Malate≥99%5189-11-7100mg,500mg





A129701Azasetron HCl≥99%123040-16-425mg,100mg
5-HT30.33 nM


F129636夫洛丙酮≥99%2295-58-150mg
5-HT1A



O129694Ondansetron≥99%99614-02-510mg,50mg,250mg
5-HT3



P129744Palonosetron HCl≥99%135729-62-3100mg,500mg
5-HT3



V129763VUF 10166≥99%155584-74-010mg,50mg,250mg
5-HT3A
0.04 nM

5-HT3AB
22 nM

N159830奈法唑酮盐酸盐99%82752-99-6200mg,1g





C101491盐酸赛庚啶98%41354-29-41g,5g,25g
5-HT20.6 nM


SETD7/91 μM


O129679Ondansetron Hydrochloride Dihydrate≥98% (HPLC)103639-04-91g,5g
5-HT3 receptor 
6.16 nM

A135530Alosetron Hydrochloride≥98% (HPLC)122852-69-11g,5g
5-HT3 receptor 



S132232Sarpogrelate Hydrochloride≥98%135159-51-25mg,25mg,100mg
5-HT2A


8.52
5-HT2B


6.57
5-HT2C


7.43
R166990Ramosetron hydrochloride98% (HPLC)132907-72-310mg,50mg,100mg,250mg
5-HT3 receptor
0.091 nM

P111269葛根素分析标准品,≥98%3681-99-020mg
5-HT2C



P111270葛根素98%3681-99-01g,5g,25g,100g
5-HT2C



T124762盐酸托烷司琼≥98.0%89565-68-4250mg,1g,5g
5-HT3 receptor 
5.3 nM

α7 nAChR
6.9 nM

C134704Cyclobenzaprine hydrochloride98%6202-23-91g,5g,25g
5-HT2 receptor



G127257Granisetron-109889-09-025mg,50mg,100mg,250mg
5HT-3



L129692LY310762≥95%192927-92-710mg,50mg
5-HT1D
249 nM

P125293Palonosetron-135729-61-210mg,100mg
5-HT3 receptor
0.17 nM

M1245745-甲氧基色胺97%608-07-1250mg,1g,5g,25g
5-HT1



5-HT2



5-HT4



5-HT6



5-HT7



T162853Tianeptine sodium salt hydrate>98.0%(HPLC)30123-17-2200mg,1g,5g
5-HT



S129681Sumatriptan Succinate≥98% (HPLC)103628-48-450mg,100mg,250mg,1g
5-HT



P129662Prucalopride≥99%179474-81-810mg,50mg
5-HT4A
2.5 nM

5-HT4B
8 nM

A124880Aripiprazole≥99%129722-12-91g,5g
5-HT1A
4.2 nM

N129630Naratriptan hydrochloride≥98%143388-64-110mg,25mg,50mg,100mg
5-HT



R129638Rizatriptan Benzoate≥98%(HPLC)145202-66-010mg,50mg,250mg,1g,5g
5-HT1



Z129649Zolmitriptan≥98%(HPLC)139264-17-8200mg,250mg,
5-HT



M129673Mosapride Citrate≥98%112885-42-410mg,50mg,250mg,1g,5g,25g
5-HT4 



E129729Eletriptan HBr≥98%177834-92-310mg,50mg,250mg,1g,5g
SSRI 



5-HT1A 



A129703Almotriptan Malate≥99%181183-52-81g
5-HT1B



5-HT1D



T168187Tegaserod maleate98% (HPLC)189188-57-610mg,50mg
5-HT4 receptor



B129734BRL-54443≥98%57477-39-110mg,50mg,100mg
5-HT1A


7.2
5-HT1B 


6.9
5-HT1D


7.2
5-HT1E


8.7
5-HT1F


9.25
B178171brexpiprazole97%913611-97-91g
5-HT1A
0.12 nM

D2L
0.3 nM

5-HT1A
0.12 nM

5-HT2A
0.47 nM

α1B受体
0.17 nM

α2C受体
0.59 nM

M179481Mosapride95%112885-41-31g,5g
5HT4



S111161血清胺盐酸盐AR153-98-01g,5g,25g
5-HT



V124992Vilazodone≥98%163521-12-810mg,50mg





F167802Flibanserin98% (HPLC)167933-07-55mg,25mg
5-HT1A
1 nM

5-HT2A
49 nM

D4 receptor
4-24 nM

V125545Vortioxetine≥98%508233-74-710mg,50mg,250mg,1g





P129402Azacyclonol≥99%115-46-850mg





 

*COX

项目号产品名称规格CAS包装细胞靶点IC50EC50Ki
C129279Celecoxib≥99%169590-42-5100mg,1g,5g,25g,100gSf9细胞COX-240 nM

N127367Nepafenac≥99%78281-72-8250mg,1g,5g
COX1


COX2


I129291Ibuprofen≥98%(GC)15687-27-15g,25g,100g,250g,500g
COX-113 μM

COX-2370 μM

I106885吲哚美辛99%53-86-15g,25g,100g,500g
COX10.28 μM

COX214 μM

S125148Sulindac≥98%38194-50-21g,5g,25g,100g
COX


D155733Diclofenac>98.0%15307-86-51g,5g,25g,100g
COX-1


COX-2


R126597Rofecoxib≥98%162011-90-750mg,250mg
COX-218 nM

M129228Meloxicam≥98%71125-38-75g,10g,25g,100g




D129705地塞米松磷酸钠≥99%55203-24-250mg,250mg
IL receptor


B129286Bufexamac≥98.0%(HPLC)2438-72-45g,25g
IFN-α
8.9 μM
A104180乙酰水杨酸99% 50-78-225g,100g,500g,2.5kg
COX1


COX2


A118582乙酰水杨酸用于植物细胞培养, ≥99.0% 50-78-2250g
COX1


COX2


S129974Suprofen≥99%40828-46-410mg,50mg
COX-1


COX-2


P129294Piroxicam≥98%(HPLC)36322-90-41g,5g,25g,100g
COX


E129317Etodolac≥98%41340-25-41g,5g,25g,100g
COX


K129331Ketoprofen≥98%(HPLC)22071-15-45g,25g,100g,250g,500g
COX-1


COX-2


D129332Diclofenac Sodium≥99%15307-79-65g,25g,100g,500g
COX-160 nM

COX-2200 nM

I129329Ibuprofen Lysine≥99%57469-77-920mg,100mg
COX


L129341Lornoxicam≥98% (HPLC)70374-39-9250mg,1g,5g
COX-15 nM

COX-28 nM

K194835酮咯酸98%74103-06-3250mg,1g,5g
COX-11.23 μM

COX-23.50 μM

N129290Naproxen Sodium≥98%26159-34-25g,25g,100g
COX-18.7 μM

COX-25.2 μM

L129349Lumiracoxib≥98%220991-20-850mg,250mg
COX-1

3 μM
COX-2

60 nM
P129299Pranoprofen≥99%52549-17-41g,5g
COX


Z129346Zaltoprofen≥98%74711-43-6250mg,1g,5g,25g,100g
COX-1


COX-2


A129429Acemetacin≥98%53164-05-91g,5g,25g
COX


T129337托灭酸≥98%13710-19-55g,25g,100g
COX-20.2 μM

V125795Valdecoxib≥99%181695-72-710mg,50mg,1g,5g
COX-25nM

P109420非那西汀≥98.0% (HPLC) 62-44-225g,100g,500g
COX


N159746Nimesulide>98.0%(HPLC)51803-78-21g,5g,25g
COX-226 μM

A129507Amfenac Sodium Monohydrate≥99%61618-27-750mg,250mg,1g,5g,25g
COX-1250 nM

COX-2150 nM

N129597尼氟酸>98.0%(HPLC)4394-00-71g,5g,25g,100g
COX-2


A110659安替比林CP,98%60-80-0100g,500g
COX3


A110660安替比林99%60-80-0100g,500g
COX3


A129352Ampiroxicam≥98%99464-64-950mg,250mg,1g
COX


S161049Naproxen>99.0%22204-53-15g,25g,100g,500g
COX-1


COX-2


B107666次水杨酸铋97%14882-18-9100g,500g
COX120 nM

COX220 nM

X139028(±)-磺吡酮≥96%57-96-51g,5g




C153919Carprofen>98.0%(HPLC)53716-49-71g,5g,25g,100g
canine COX230 nM

D129411Diclofenac Diethylamine≥99%78213-16-85g,25g
COX1


COX2


D133115二氟苯水杨酸≥98%22494-42-41g,5g
COX


P113217菲尼酮98.50%92-43-325g,100g,500g
COX


LOX


P113218菲尼酮97%92-43-3100g,500g
COX


LOX


M157895甲芬那酸>98.0%61-68-725g,100g,500g
COX-1


COX-2


E126660Etoricoxib≥98.0%202409-33-410mg,50mg,250mg,1g,5g
COX-2


S161351D-α-生育酚>97.0%(GC)59-02-9 25g,100g,500g




O129611Oxaprozin≥98%21256-18-85g,25g,100g
COX-1


COX-2


R107337吴茱萸次碱分析标准品,≥98%84-26-410mg,20mg
COX2


R107338吴茱萸次碱98%84-26-450mg,250mg,1g
COX2


S104922D(-)-水杨苷99%138-52-35g,25g,100g
COX1 


S104923D(-)-水杨苷分析标准品,≥99%138-52-320mg
COX1 


S118533水杨酸用于植物细胞培养,≥99 %69-72-7500g




S104158水杨酸AR,99.5%69-72-7250g,1kg,2.5kg




S104162水杨酸ACS,≥99.0%69-72-7250g,1kg




X139169黄腐酚≥97.0%(HPLC)6754-58-15mg,25mg,100mg




F121952Flunixin meglumine98%42461-84-7250mg,1g,5g,25g




 

*γ-secretase

项目号产品名称规格CAS包装细胞靶点IC50
D126677DAPT≥98%208255-80-55mg,10mg,25mg,50mgHEK 293细胞γ secretase(Aβ)20 nM
R127403RO4929097≥99%847925-91-15mg,10mg,50mg无细胞γ secretase4 nM
Aβ4014 nM
Notch5 nM
S125519Semagacestat (LY450139)≥98%425386-60-35mg,10mg,50mg人神经胶质瘤细胞Aβ4210.9 nM
Aβ4012.1 nM
Aβ3812.0 nM
Notch14.1 nM
M126008MK-0752≥99%471905-41-65mg,10mg,50mg
Aβ405 nM
B126453Avagacestat (BMS-708163)≥99%1146699-66-25mg,10mg,50mg
Aβ400.3 nM
Aβ420.27 nM
Y129283YO-01027≥97%209984-56-52mg,5mg,25mg无细胞APPL2.6 nM
Notch2.9 nM
L125846LY-411575≥98%209984-57-65mg,25mg,100mgHEK293细胞APP0.078 nM
NΔE0.082 nM
Notch0.39 nM
P127448PF-3084014≥98%1290543-63-35mg,10mg,25mg,50mg,100mg无细胞γ-secretase 6.2 nM

 

*GluR

项目号产品名称规格CAS包装细胞靶点IC50KiEC50
X113958黄尿酸96%59-00-71g,5g
mGlu2


R129533Riluzole≥98%1744-22-51g,5g,25g,100g
mGlu3 


L129669Latrepirdine≥96%97657-92-65mg,10mg,50mg
histamine receptors


GluR


5-HT receptors


C126237CTEP (RO4956371)≥99%871362-31-15mg,10mg,50mg
mGlu52.2 nM

M127959MPEP≥98%96206-92-7 10mg,50mg,250mg
mGluR536 nM

L127760LY404039≥99%635318-11-55mg,25mg,50mg
mGlu2/mGlu3
149 nM
mGlu2/mGlu3
92 nM
G103978L-谷氨酸99%56-86-0100g,250g,500g,2.5kg




G103979L-谷氨酸超纯级,≥99.5% (NT)56-86-0100g,500g,2.5kg




G107510L-谷氨酸非动物源,EP,JP,USP ;用于细胞培养,98.5 to 101.0%56-86-0100g,500g




A129508ADX-47273≥99%851881-60-25mg,10mg,50mg
mGlu5

0.17 μM
V129515VU 0357121≥98%433967-28-310mg,50mg,250mg
mGluR5

30 nM
S161191L-O-磷酸丝氨酸>98.0%(T)407-41-01g,5g,25g
mGluR


V129525VU 0364770≥98%61350-00-310mg,50mg,250mg
mGlu4

1.1 μM
V129527VU 0361737≥98%(HPLC)1161205-04-410mg,50mg,250mg人类受体mGluR4

240 nM
大鼠受体mGluR4

110 nM
D107632D-谷氨酰胺98%5959-95-51g,5g,25g,100g





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