阿拉丁小分子抑制剂、激动剂、拮抗剂--G蛋白偶联受体信号通路(上)

来源: 上海阿拉丁生化科技股份有限公司   2020-7-10   访问量:386评论(0)

box-sizing: border-box;">M129297Mirtazapine≥98%85650-52-8100mg,1g5-HTSB742457SB742457≥97%607742-69-85mg,25mg5-HT69.63B129690BRL-15572≥99%193611-72-25mg,10mg,50mg 5-HT1D7.9P129785PRX-08066 Maleic acid≥99%866206-55-55mg,10mg,50mg 5-HT2B3.4 nMT124762盐酸托烷司琼≥98.0%105826-92-4250mg,1g,5g5-HT370.1±0.9 nMP129438Pizotifen Malate≥99%5189-11-7 100mg,500mg A129701Azasetron HCl≥99%123040-16-425mg,100mg5-HT30.33 nMF129636夫洛丙酮≥99%2295-58-150mg5-HT1AO129694Ondansetron≥99%99614-02-510mg,50mg,250mg 5-HT3P129744Palonosetron HCl≥99%135729-62-3100mg,500mg 5-HT3V129763VUF 10166≥99%155584-74-010mg,50mg,250mg5-HT3A0.04 nM5-HT3AB22 nMN159830奈法唑酮盐酸盐98.00%82752-99-6200mg,1gC101491盐酸赛庚啶98%41354-29-41g,5g,25g5-HT20.6 nMO129679Ondansetron Hydrochloride Dihydrate≥98% (HPLC)103639-04-91g,5g5-HT3 receptor 6.16 nMA135530Alosetron Hydrochloride≥98% (HPLC)122852-69-11g,5g5-HT3 receptor S132232Sarpogrelate Hydrochloride≥98%135159-51-25mg,25mg,100mg5-HT2A8.525-HT2C7.435-HT2B6.57R166990Ramosetron hydrochloride98% (HPLC)132907-72-310mg,50mg,100mg,250mg 5-HT3 receptor 0.091 nMP111270葛根素98%3681-99-01g,5g,25g,100g 5-HT2CP111269葛根素分析标准品,≥98%3681-99-020mg5-HT2CC134704Cyclobenzaprine hydrochloride98%6202-23-91g,5g,25g5-HT2 receptor G127257Granisetron-109889-09-025mg,50mg,100mg,250mg 5HT-3L129692LY310762≥95%192927-92-710mg,50mg5-HT1D249 nMP125293Palonosetron-135729-61-210mg,100mg5-HT3 receptor 0.17 nMM1245745-甲氧基色胺97%608-07-1250mg,1g,5g,25g5-HT15-HT25-HT45-HT6S129681Sumatriptan Succinate≥98% (HPLC)103628-48-450mg,100mg,250mg,1g P129662Prucalopride≥99%179474-81-810mg,50mg5-HT4A2.5 nM5-HT4B8 nMA124880 Aripiprazole≥99%129722-12-91g,5g5-HT1A4.2 nMN129630 Naratriptan hydrochloride≥98%143388-64-110mg,25mg,50mg,100mg 5-HT R129638Rizatriptan Benzoate≥98%(HPLC)145202-66-010mg,50mg,250mg,1g,5g 5-HT1Z129649Zolmitriptan≥98%(HPLC)139264-17-8200mg,250mg,1g,5g,25g 5-HTM129673Mosapride Citrate≥98%112885-42-410mg,50mg,250mg,1g,5g,25g 5-HT4E129729Eletriptan HBr≥98%177834-92-310mg,50mg,250mg,1g,5g5-HT1B0.92 nM5-HT1D3.14 nMA129703Almotriptan Malate≥99%181183-52-81g5-HT1B5-HT1DT168187Tegaserod maleate98% (HPLC)189188-57-610mg,50mg5-HT4 receptor B129734BRL-54443≥98%57477-39-110mg,50mg,100mg5-HT1E8.75-HT1F9.25B178171 brexpiprazole97%913611-97-91gD2L0.3 nM5-HT1A0.12 nM5-HT2A0.47 nMα1B受体0.17 nMα2C受体0.59 nMM179481Mosapride95%112885-41-31g,5g5HT4S111161血清胺盐酸盐AR153-98-01g,5g,25g5-HTV124992Vilazodone≥98%163521-12-810mg,50mgF167802Flibanserin98% (HPLC)167933-07-55mg,25mg5-HT1A1 nM5-HT2A49 nMF167802Vortioxetine≥98%508233-74-710mg,50mg,250mg,1g P129402Azacyclonol≥99%115-46-850mg

*肾上腺素受体

项目号产品名称规格CAS包装靶点IC50KipKiKdEC50ED50pEC50
D129796甲磺酸多沙唑嗪≥99%77883-43-350mg,100mg,250mg,1g,5g,25g,100gα-1肾上腺素能受体
I129899Ivabradine HCl≥98%148849-67-6250mg,1g,5g肾上腺素受体2.9 μM
C129903Cisatracurium Besylate≥98%96946-42-81g肾上腺素受体
A124739Asenapine maleate≥98% (HPLC)85650-56-210mg,50mg,250mg,1g5-HT2C10.46
5-HT2A10.15
5-HT79.94
5-HT2B9.75
5-HT69.6
C141489卡拉洛尔98%57775-29-8250mg,1g
C120231 卡拉洛尔分析标准品57775-29-810mg
A129804Alfuzosin hydrochloride≥98%81403-68-150mg,100mg,250mg,1gα1受体
S126595Silodosin≥99%160970-54-75mg,25mg,100mg,250mg,1g
N129836Nebivolol hydrochloride≥97%152520-56-410mg,20mg,100mg,1g,5gβ1-肾上腺素受体0.8 nM
B129688BMY 7378 dihydrochloride≥98%21102-95-410mg,50mg,100mgα2C肾上腺素受体 6.54
α1D肾上腺素受体 8.2
5-HT1A受体 8.3
P160142Prazosin Hydrochloride≥98.0%19237-84-450mg,250mg,1gα肾上腺素受体
P123277甲磺酸酚妥拉明≥98.0%(TLC)65-28-1100mg,500mg,5gα-肾上腺素受体0.1 μM
M111945酒石酸美托洛尔98%56392-17-75gβ-肾上腺素能受体42 ng/mL
M111944酒石酸美托洛尔分析标准品56392-17-71gβ-肾上腺素能受体42 ng/mL
T129895Terazosin hydrochloride Dihydrate≥98%70024-40-7100mg,5g,25gα-肾上腺素能受体
M129850Maprotiline HCl≥99%(HPLC)10347-81-61g,5g,25g肾上腺素受体
C123267Carvedilol≥98%(HPLC)72956-09-31g,5g,25gα1肾上腺素受体
β1肾上腺素受体
N129805Naftopidil≥98.0%57149-07-25g,25g,500gα1-肾上腺素能受体 58.3 nM
P129843Phenoxybenzamine HCl≥98%63-92-31g,5g,25gα受体拮抗剂550 nM
A129820Acebutolol HCl≥99%34381-68-5250mgβ-肾上腺素能受体
B129336Buflomedil HCl≥98%35543-24-91g,5g,25g,100g,500gα-肾上腺素受体
C134671cis-(Z)-Flupentixol Dihydrochloride≥98% (HPLC)51529-01-2250mgα肾上腺素能受体
A132124阿普洛尔 盐酸盐≥99%13707-88-550mg,250mgβ-肾上腺素能受体
M171294Moxisylyte hydrochloride>99% (TLC)964-52-325gα-肾上腺素受体
A151072Atipamezole Hydrochloride98%104075-48-125mg,100mg,250mg,1gα2肾上腺素能受体
A132977Atipamezole≥98% (HPLC)104054-27-55mg,25mg,100mg,1gα2肾上腺素能受体
P160771吡贝地尔>98.0%(GC)(T)3605-01-4200mg,1gα2C肾上腺素受体 7.2
α2A肾上腺素受体 7.1
D2肾上腺素受体 6.9
T102080盐酸坦索罗辛98%106463-17-6100mg,500mg,1gα1A肾上腺素受体
T136685Terazosin Hydrochloride >98.0%(HPLC)63074-08-850mg,250mg,1gα-AR
D193380盐酸贝凡洛尔98%42864-78-8250mg,1g,5gβ肾上腺素受体
B129900Betaxolol≥98%63659-18-710mg,50mg,250mgβ1肾上腺素能受体
A124776阿替洛尔≥98%,powder29122-68-71g,5g,25g,100gβ1肾上腺素受体 0.25 μM
β2肾上腺素受体 1 μM
Y111137盐酸育亨宾99%65-19-01g,5g,25gα2肾上腺素受体
Y111138盐酸育亨宾分析标准品,≥99%65-19-020mgα2肾上腺素受体
Y140628盐酸育亨宾97%65-19-01g,5g,25gα2肾上腺素受体
L133648Labetalol HCl98%32780-64-650mg,250mg,1gα1肾上腺素受体
β肾上腺素受体
M126688Mirabegron≥99%223673-61-85mg,10mg,50mg,250mg,1gβ3肾上腺素受体 22.4 nM
X113957盐酸甲苯噻嗪分析标准品23076-35-9100mgα2肾上腺素能受体
X113956盐酸甲苯噻嗪98%23076-35-91g,5g,25g,100gα2肾上腺素能受体
D194797盐酸阿可乐定(曾用名:盐酸安普乐定)97%73218-79-825mg,100mg,250mg,1g,5gα2-肾上腺素能受体
I157518茚达特罗马来酸盐>98.0%(HPLC)753498-25-820mg,25mg,50mg,100mg,1gβ1肾上腺素受体 7.36
β2肾上腺素受体 5.48
I129810盐酸异丙肾上腺素≥99%51-30-95g,25g,100gβ肾上腺素受体
F129812Formoterol Hemifumarate≥99%43229-80-710mg,50mgβ2肾上腺素受体
E129809酒石酸肾上腺素≥98%51-42-31g,5g,25gα肾上腺素能受体
β肾上腺素受体
C102161盐酸可乐定98%4205-91-8250mg,1g,5g,100gα2肾上腺素能受体 0.02±0.01 mg/kg
D129407Droxidopa≥98%23651-95-850mg,250mg
D129818Dexmedetomidine≥98%113775-47-650mg,250mgα2肾上腺素能受体
P106007盐酸去氧肾上腺素99%61-76-75g,10g,25g,50g,100gα1肾上腺素能受体
G156852氯苄氨胍醋酸盐>98.0%(HPLC)23256-50-0200mg,1g,5gα2a-肾上腺素能受体 8.25
α2b-肾上腺素能受体 7.01
α2c-肾上腺素能受体 <5
N113459Naphazoline hydrochloride99%550-99-25g,25g,100g,500g
R124692利托君盐酸盐≥98%23239-51-2250mg,1g,5gβ-2肾上腺素能受体
D129813Dexmedetomidine HCl≥98%145108-58-35mg,10mg,50mg,100mgα-2肾上腺素受体
M129911Medetomidine HCl≥99%86347-15-110mg,25mg,50mg,100mgα2-肾上腺素受体 1.08 nM
T101308替扎尼定98%64461-82-15g,25gα2-肾上腺素受体
D129815Detomidine HCl≥98%90038-01-050mg,250mg,1g
S129883Scopine≥98%498-45-325mg,100mg,200mg,500mgα1-肾上腺素能受体
N107258重酒石酸去甲肾上腺素一水合物≥98%(HPLC),USP108341-18-0250mg,1g,5g,25gα-肾上腺素能受体
X139232赛拉嗪≥98.0%(HPLC)7361-61-71g,5g,10g,25gα2-肾上腺素受体
T128967特布他林半硫酸盐98%23031-32-51g,5g,25gβ2-肾上腺素能受体53 nM
T128967特布他林半硫酸盐分析标准品23031-32-5100mgβ2-肾上腺素能受体53 nM
I157589异丙肾上腺素硫酸盐二水合物>98.0%(HPLC)(N)299-95-61g,5g,25gβ-肾上腺素能受体
X129373Xylometazoline HCl≥98.0%(HPLC)1218-35-51g,5g,25g,100gα2B肾上腺素受体 4 μM
A114817双甲脒分析标准品,99%33089-61-1250mgα2肾上腺素受体
A114818双甲脒97%33089-61-11g,5gα2肾上腺素受体
G133358Guanfacine hydrochloride≥98%(HPLC)29110-48-310mg,50mg,100mg,250mgα2A-肾上腺素受体
I134069异舒普林 盐酸盐分析标准品579-56-61g,5gβ-肾上腺素能受体
I125935Indacaterol≥99%312753-06-350mg,250mgβ1-肾上腺素能受体 7.36
β2-肾上腺素能受体 5.48
B134443Bambuterol Hydrochloride≥98% (HPLC)81732-46-91g,5gβ-肾上腺素能受体
D134211DL-去甲肾上腺素 盐酸盐97%55-27-61g,5g,25g
S107339辛弗林分析标准品,≥98%94-07-520mg
S107340辛弗林98%94-07-55g,25g
N109573L-去甲肾上腺素98%51-41-2250mg,1gα1肾上腺素受体 56 nM
α2A肾上腺素受体 330 nM
β1肾上腺素受体 740 nM
B136672Brimonidine>98.0%(HPLC)59803-98-4250mg,1g,5g
D137302双氢**胺甲磺酸盐>95.0%(HPLC)6190-39-2100mg,250mg,1g
D135863Dihydro Ergotamine Mesylate药典级6190-39-2250mg
A129906Adrenalone HCl Hydrate≥98%62-13-51g,5g,25g,100gα-1肾上腺素受体
D129628醋酸去氧皮质酮≥99%56-47-3250mg,1g,5g

*组胺受体


项目号产品名称规格CAS包装靶点IC50Ki
C115479Cetirizine dihydrochloride98%83881-52-11g,5g,25g,100g组胺受体
F129253Fexofenadine HCl≥98%153439-40-810mg,50mg,1g,5g组胺H1受体246 nM
E129640Epinastine HCl≥99%108929-04-050mg,250mg,1g,5g,25g组胺受体
O159894Olopatadine Hydrochloride>98.0%(HPLC)140462-76-6250mg,1g组胺受体559 μM
A124055安他唑啉 盐酸盐98%2508-72-71g,5g,25g,100g组胺H1受体
K124652酮替芬延胡索酸99%34580-14-8100mg,250mg,1g,5g,25g组胺H1受体
A129250Azatadine dimaleate≥98%3978-86-710mg,50mg,250mg,1g组胺受体6.5 nM
胆碱能10 nM
H107699橙皮素分析标准品,≥98%520-33-220mg组胺受体
H107700橙皮素97%520-33-21g,5g,25g,100g组胺受体
C136571CarbinoxamineMaleateSalt-3505-38-25g,10g,25g组胺-H1受体
D129627Doxylamine Succinate≥99%562-10-71g,5g,10g,25g,50g组胺H1受体
B102783盐酸倍他司汀99%5579-84-01g,5g,10g,25g,100g组胺H3受体1.9 μM
C129211Clemastine Fumarate≥98% (HPLC)14976-57-9100mg,250mg,500mg,1g组胺H1受体3 nM
L129669Latrepirdine≥96%97657-92-65mg,10mg,50mg
L129223Loratadine≥98%79794-75-5100mg,1g,5g,25gB(0)AT24 μM
B129218Bepotastine Besilate98%190786-44-810mg,50mg,100mg,250mg,1g
M129226Mianserin HCl≥98%21535-47-750mg,250mg,1g,5g组胺受体
M157977美喹他嗪>98.0%(GC)29216-28-2100mg,250mg,1g组胺H1受体
A129214Azelastine HCl≥98%(HPLC)79307-93-0100mg,250mg,1g,5g,25g组胺受体
R129213盐酸雷尼替丁≥98%(HPLC)66357-59-31g,5g,25g组胺H2-受体3.3±1.4 μM
D129201Diphenhydramine Hydrochloride≥98% (HPLC)147-24-05g,25g,100g,500g组胺H1受体
D155989Desloratadine>98.0%(HPLC)(T)100643-71-8100mg,250mg,1g,5g,25g组胺H1受体51nM
C129233马来酸氯苯那敏≥99%113-92-85g,25g,100g,500g组胺H1受体12nM
M129292Meclizine 2HCl≥98%1104-22-9250mg,1g,5g,25g组胺H1受体
M129245Mizolastine≥98%108612-45-91g,5g组胺H1受体47 nM
C102301Cimetidine99%51481-61-95g,25g,100g组胺H2受体
L129237Lafutidine≥99%118288-08-710mg,50mg,250mg组胺H2受体
N129229Nizatidine≥98%76963-41-25g,25g组胺H2受体0.9 nM
AChE6.7 nM
H168667羟嗪 二盐酸盐98%2192-20-310mg,10g组胺H1受体19 nM
B129275Brompheniramine hydrogen maleate≥98%980-71-250mg,250mg,1g,5g,25g组胺H1受体
J129258JNJ-7777120≥98% (HPLC)459168-41-310mg,50mg组胺H4受体4.5 nM
P129261Pemirolast potassium≥99%100299-08-910mg,50mg,250mg组胺H1受体
L124802盐酸左旋西替利嗪≥98% (HPLC)130018-87-01g,5g组胺H1受体
P129451Pheniramine Maleate≥99%132-20-71g,5g
C119225*平盐酸盐分析标准品14984-68-05g,10g,25g
R129246盐酸罗沙替丁醋酸酯≥99%93793-83-0200mg,1g,5g,25g组胺H2受体3.2 μM
A151022阿伐斯汀>98.0%(HPLC)87848-99-520mg,100mg
E134559富马酸依美斯汀≥98.0%(HPLC)87233-62-350mg,250mg,1g,5g组胺H1受体
M118323美海屈林萘二磺酸盐98%6153-33-91g,5g,25g
F129242Famotidine≥99%76824-35-65g,25g组胺H2受体0.6 mM
P133927盐酸异丙嗪>98.0%(HPLC)58-33-325g,100g组胺H1受体
L129221Lidocaine≥99%137-58-65g,25g,100g组胺H1受体>32 μM
H111796组胺96%51-45-61g,5g
H110868组胺二盐酸盐98%56-92-85g,25g,100g组胺H1受体
组胺H2受体
B152161甲磺酸倍他司汀>99.0%(HPLC)54856-23-425g,100g,500g
,
阿拉丁小分子抑制剂、激动剂、拮抗剂--G蛋白偶联受体信号通路(上)

G蛋白偶联受体

G蛋白偶联受体(GPCRs)是一类与G蛋白偶联的细胞表面受体,具有7个跨膜α螺旋结构。G蛋白偶联受体(GPCRs)能接受许多细胞外信号并传递给G蛋白,进而启动细胞内不同的信号转导通路。GPCRs介导对环境刺激物、神经递质、激素、细胞因子和脂质信号分子的多种生理反应,从而在视觉、嗅觉、自主神经系统和行为等生物过程中发挥着重要作用。GPCRs还与众多疾病相关,是治疗许多疾病的重要靶点之一。异常的GPCR功能与病理状态有关,如神经、免疫和激素紊乱等。

G蛋白偶联受体信号通路转导过程

G 蛋白偶联受体可被多种不同的外界刺激激活。当配体与GPCRs结合时,激活附着在细胞内侧端的G蛋白(由α、β、γ三个亚基组成的异源三聚体)。G蛋白上原本结合的GDP被GTP取代,导致α亚基与β-γ亚基复合物解离,并触发各种不同的信号级联放大,激活下游信号通路。这些细胞内信号通路包括cAMP/PKA、钙/NFAT、磷脂酶C(PLC)、蛋白酪氨酸激酶、MAP激酶、PI3K、NO/cGMP、Rho和JAK/STAT等,从而作用于相应的靶分子,进而调控代谢过程及基因表达功能。

G蛋白偶联受体信号通路图

产品列表

按靶点分类:

*5-HT受体

项目号产品名称规格CAS包装细胞靶点IC50KipKi
F131623Fluoxetine HCl≥98%(HPLC)56296-78-71g,5g,25g5-HT0.1 pM
V129637Venlafaxine hydrochloride≥98%(HPLC)99300-78-41g,5g,25g,100g 5-HT
D129639Dapoxetine hydrochloride≥98%(HPLC)129938-20-1250mg,1g,5g5-HT
I125279Iloperidone≥98%133454-47-450mg,250mg,1g,5g 5-HT
V129787Vortioxetine (Lu AA21004) HBr≥98%960203-27-45mg,25mg,100mg5-HT1A15 nM
5-HT1B33 nM
5-HT3A3.7 nM
5-HT7受体19 nM
SERT1.6 nM
F129671Fluvoxamine maleate≥98%61718-82-9250mg,1g,5g,25g,100g 5-HT
S129789Sertraline HCl≥98% (HPLC)79559-97-01g,5g5-HT
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,25g5-HT
E122736草酸右旋西酞普兰98%219861-08-250mg,250mg,1g,5g 5-HT0.89 nM
D123291盐酸度洛西汀≥98.0%(HPLC)136434-34-91g,5g,25g5-HT
M129386Milnacipran hydrochloride≥99%101152-94-710mg,50mg,250mg,500mg,1g,5g,25gNET77 nM
SERT420 nM
A129730盐酸阿米替林≥98%549-18-81g,5g,25g,100g5-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
C122737氢溴酸西酞98%59729-32-71g,5gserotonin 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%25332-39-21g5-HT
P137447Protriptyline Hydrochloride≥98%1225-55-425mg,100mg
A129721 Atomoxetine HCl≥98%82248-59-750mg,250mg,1gNorepinephrine (NE) transporter 5 nM
5-HT77 nM
DA transporter 1451 nM
C126883氯氮平≥98%(GC)5786-21-0100mg,1g,5g,25g,100g 5-HT110 nM
O126519Olanzapine≥99%132539-06-11g,5g5-HT2
D2 receptor
K129651Ketanserin≥97%74050-98-950mg,250mg,1g5-HT2A2.5 nM
大鼠5-HT2C50 nM
5-HT2C100 nM
L129669Latrepirdine≥96%97657-92-65mg,10mg,50mg
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,100g5-HT2A0.17 nM
α2c-adrenergic receptor 1.3 nM
D2 receptor3.57 nM
D3 receptor3.6 nM
D2L Receptor 4.16 nM
E129717Ziprasidone HCl≥98%122883-93-6250mg,1g5-HT receptor
Dopamine receptor
W129689WAY-100635 Maleate≥99%1092679-51-05mg,25mg,100mg 5-HT0.95 nM
B129706Blonanserin≥98% (HPLC)132810-10-725mg,100mgdopamine D2 receptor 14.8 nM
5-HT23.98 nM
S129658SB269970 HCl≥99%261901-57-910mg,50mg5-HT78.3
S125056SB269970 HCl-261901-57-910mg5-HT78.3
G120176盐酸格拉司琼98%107007-99-810mg,50mg,1g,5g 5-HT3
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