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(下)

来源: 上海阿拉丁生化科技股份有限公司   2020-7-10   访问量:411评论(0)

style="vertical-align: top; padding: 0px; box-sizing: border-box;"> P129443Pramipexole 2HCl Monohydrate≥98%(HPLC)191217-81-950mg,250mg,1gD2S受体3.9 nM D2L受体2.2 nM D3受体0.5 nM D4受体5.1 nM P129434Pramipexole≥99%104632-26-010mg,50mgD2S受体3.9 nM D2L受体2.2 nM D3受体0.5 nM D4受体5.1 nM D103111盐酸多巴胺98%62-31-75g,25g,100g,500g,2.5kg多巴胺受体 P129456Pergolide mesylate≥99%66104-23-22.5mg B178171brexpiprazole97%913611-97-91gD2L0.3 nM5-HT1A0.12 nM5-HT2A0.47 nMα1B受体0.17 nMα2C受体0.59 nMP160771吡贝地尔>98.0%(GC)(T)3605-01-4200mg,1gP129442PD128907 HCl≥98%112960-16-45mg,25mg,100mg多巴胺D3受体 0.64 nMR126364Rotigotine≥98%99755-59-610mg,50mg多巴胺受体P165634Pramipexole dihydrochloride>98% (HPLC)104632-25-910mg,50mgD2S受体3.9 nMD2L受体2.2 nMD3受体0.5 nMD4受体5.1 nMM132847MPTP盐酸盐≥98%23007-85-425mg,100mgO101521章胺盐酸盐98%770-05-81g,5g

*阿片受体

项目号产品名称规格CAS包装靶点IC50Ki
R126180Racecadotril≥98%81110-73-8250mg,1g,5g,25g阿片受体4.5 μM
N129470Naloxone HCl≥99%357-08-450mg,250mg,1g
J125889JTC-801≥99%244218-51-75mg,10mg,50mgORL194 nM
N129461Naltrexone HCl≥99%16676-29-250mg,250mg,1g阿片受体8 nM
A124975Alvimopan≥98%156053-89-325mg,100mgμ阿片受体0.77 nM
δ阿片受体4.4 nM
κ阿片受体40 nM
L129465Loperamide HCl≥98%34552-83-55g,25gμ阿片受体3.3 nM
δ阿片受体48 nM
A127848ADL5859 HCl≥98%850173-95-41mg,5mg,10mg,50mgδ阿片受体0.8 nM
M109803苦参碱98%519-02-8100mg,1g,5g,25gκ阿片受体
M109802苦参碱分析标准品,≥98%519-02-820mgκ阿片受体
T129468Trimebutine≥98%39133-31-8250mg,5g,25g,100gμ阿片受体
δ阿片受体
κ阿片受体
M129400Meptazinol HCl≥99%59263-76-210mg,50mg,250mg阿片受体

*大麻素受体

项目号产品名称规格CAS包装靶点IC50KiEC50
O135157橄榄醇95%500-66-31g,5g
R125003Rimonabant≥98%168273-06-110mg,50mg,500mghCB113.6 nM
A129844AM251≥98%183232-66-85mg,25mg,100mgCB1 700 nM
C129834CP-945598 HCl≥98%686347-12-610mg,50mgCB10.7 nM
A129838AM1241≥98%444912-48-55mg,10mg,25mg,50mgCB23.4 nM
B126713BML-190≥99%2854-32-210mg,50mgCB2435 nM
G129840GW842166X≥98%666260-75-95mg,25mg,100mgCB263 nM
O129837Org 27569≥98%868273-06-710mg,50mgCB1

*内皮素受体

项目号产品名称规格CAS包装靶点IC50
Z125040Zibotentan (ZD4054)≥98%186497-07-45mg,25mg,100mgET-A21 nM
B129849Bosentan Hydrate≥99%157212-55-050mg,250mg,1g,5gET-A4.7 nM
ET-B95 nM
M125524Macitentan≥97%441798-33-05mg,25mg,100mg,1gET-A0.5 nM
ET-B391 nM
A126631Ambrisentan≥99%177036-94-15mg,10mg,20mg,100mg,250mg,1gET-A18 nM

*S1P受体

项目号产品名称规格CAS包装细胞靶点IC50KiEC50
S129855SKI II≥98%312636-16-15mg,25mg,100mg SphK0.5 μM
P125702PF-543-1415562-82-15mg,10mg,50mg SphK13.6 nM
A127517ABC294640≥99% 915385-81-85mg,10mg,50mg SphK260 μM
F126599Fingolimod HCl≥98%162359-56-0100mg,200mg,250mg,1gK562 、NK细胞S1P0.33 nM
P177659Ponesimod97%854107-55-4100mgS1P15.7 nM

*Hedgehog/Smoothened

项目号产品名称规格CAS包装细胞靶点IC50KiKd
V127477Vismodegib (GDC-0449)98%879085-55-910mg,50mg,100mg,250mg,500mg,1g无细胞hedgehog3 nM
L125247LY2940680≥99%1258861-20-95mg,10mg,50mg Smo
J169510JK18498% (HPLC)315703-52-75mg,25mg哺乳动物细胞Gli30 nM
J135916Jervine>97.0%(HPLC)469-59-010mg,25mg,50mg,100mg,250mg Hedgehog500-700 nM
C125994Cyclopamine≥99%4449-51-85mg,10mg,50mgTM3Hh12细胞Smo46 nM
L127562NVP-LDE225≥99%956697-53-310mg,50mg,100mg无细胞Smo (小鼠)1.3 nM
无细胞Smo (人) 2.5 nM
P126554PF-5274857≥99%1373615-35-05mg,10mg,50mg Smo5.8 nM4.6 nM
S129830SANT-1≥98%304909-07-75mg,25mg,100mg Smo1.2 nM
B126389BMS-833923≥99%1059734-66-510mg,50mgSmo
P126030Purmorphamine≥98%483367-10-85mg,25mg,100mgHEK293T细胞Smo~1.5 μM

*SGLT

项目号产品名称规格CAS包装细胞靶点IC50EC50
D126800 Dapagliflozin≥99%461432-26-810mg,50mg,250mg,1gCHO细胞hSGLT21.1 nM
C126191Canagliflozin≥98%842133-18-010mg,50mg,250mg,1g无细胞SGLT22.2 nM
E127439Empagliflozin (BI 10773)≥99%864070-44-05mg,25mg,100mg,500mg,1g SGLT23.1 nM
L127607LX-4211≥98%1018899-04-15mg,10mg,50mgSGLT136 nM
SGLT21.8 nM
I177384 Ipragliflozin97%761423-87-410mg,25mg,50mg,100mg,1g hSGLT27.4 nM
P127748根皮素≥98%60-82-2250mg,1g,5gSGLT1
SGLT2
P139206根皮苷≥98%60-81-1250mg,1g
P127306PF-04971729≥98%1210344-57-25mg,10mg,50mg hSGLT20.877 nM

*SGLT

项目号产品名称规格CAS包装细胞靶点Ki
K126742Ki16425≥98%355025-24-02mg,5mg,25mgRH7777细胞系LPA10.34 μM
LPA26.5 μM
LPA30.93 μM
K129869Ki16198≥99%355025-13-75mg,10mg,50mgLPA10.34 μM
LPA30.93 μM

*OX受体

项目号产品名称规格CAS包装
A129661Alverine Citrate≥99%5560-59-85g,25g
S117970五味子酯甲分析标准品,>98%58546-56-820mg,100mg

*CGRP受体

项目号产品名称规格CAS包装靶点Ki
B125641BMS-927711-1289023-67-110mg,25mg,100mgCGRP0.027 nM

*MT受体

项目号产品名称规格CAS包装靶点KipKi
R125051Ramelteon≥99%196597-26-910mg,50mg,100mgMT114 pM
MT2112 pM
小鸡前脑MT23.1 pM
M118674褪黑素98%73-31-4250mg,1g,5g,25g,100gMT
T176929Tasimelteon97%609799-22-6100mgMT19.45
MT29.8

*PAFR

项目号产品名称规格CAS包装靶点IC50
G101969银杏内酯B分析标准品,≥99%15291-77-710mg,50mgPAFR3.6 μM

*PKA

项目号产品名称规格CAS包装细胞靶点IC50Ki
A126845A-674563≥98%552325-73-25mg,25mg,100mgPKA16 nM
Akt11 nM
H129712H 89 2HCl≥99%130964-39-510mg,50mg无细胞PKA48 nM
D155111Daphnetin>90.0%(HPLC)486-35-150mg,250mg,1gEGFR7.67 μM
PKA9.33 μM
PKC25.01 μM
D124575N6,2′-O-二丁酰基腺苷3′,5′-环磷酸 钠盐≥97% (HPLC)16980-89-525mg,100mg,250mg,1g PKA

*腺苷受体

项目号产品名称规格CAS包装靶点IC50Ki
L1250775-Iodotubercidin≥98%24386-93-45mg,25mg腺苷激酶26 nM
I125338Istradefylline≥99%155270-99-85mg,25mg,100mgA2AR2.2 nM
H1570707-(2-羟丙基)茶碱>98.0%(HPLC)(N)603-00-91g,5g,25gA1腺苷
S167655SCH 5826198% (HPLC)160098-96-45mg,10mg,25mg,50mg,100mgbovine A2a2.0 nM
rat A2a2.3 nM
R126916Reversine≥97%(HPLC)656820-32-55mg,10mg,50mg,100mg,250mg人A3腺苷受体0.66 μM
aurora A12 nM
aurora B13 nM
aurora C20 nM
T111224茶碱乙酸98%652-37-925g,100g,500g
A108807腺嘌呤核苷分析标准品58-61-720mg
A108806腺嘌呤核苷用于细胞培养,>99.5%(HPLC)58-61-75g,25g
A108808腺嘌呤核苷超纯级,99.5%58-61-71g,5g,25g,100g
A108809腺嘌呤核苷BC,99%58-61-725g,100g

*CaSR

项目号产品名称规格CAS包装靶点IC50EC50
C129866Cinacalcet HCl≥99%364782-34-310mg,50mg,250mg,1g,5gCaSR2.8 μM
N125903NPS-2143≥98%284035-33-25mg,25mg,100mgCa(2+)受体43 nM

*CXCR

项目号产品名称规格CAS包装细胞靶点IC50
T103998单宁酸AR1401-55-410g,25g,100g,250g,500gCXCL12
CXCR4
R126706Reparixin≥98%266359-83-55mg,25mg,100mgCXCR1
CXCR2
CXCL8
P129846Plerixafor 8HCl (AMD3100 8HCl)≥99%155148-31-55mg,10mg,50mgCXCR444 nM
CXCL125.7 nM
P128026Plerixafor≥98%110078-46-110mg,50mg,250mg无细胞CXCR444 nM
CXCL125.7 nM
D178502danirixin97%954126-98-8100mgCXCL812.5 nM

*血管升压素受体

项目号产品名称规格CAS包装靶点IC50
C129921Conivaptan HCl≥99%168626-94-610mg,50mg,250mg加压素受体1
加压素受体2
T129870Tolvaptan≥98%150683-30-010mg,50mg,250mg,1g加压素受体21.28μM
M129872Mozavaptan≥99%137975-06-510mg,50mg加压素受体11.2 μM
加压素受体214 nM

*cAMP

项目号产品名称规格CAS包装靶点IC50EC50
B101323硫双二氯酚97%97-18-725g,100g,500gsAC4.0 μM
F127328Forskolin≥98%66575-29-910mg,50mg,100mg,500mg,1gAC
P118976PACAP(6-38), human, ovine, rat98%137061-48-41mg,5mg,25mgPAC11.1 nM
PAC1s1.7 nM
PAC1vs121 nM

*TAAR

项目号产品名称规格CAS包装靶点Ki
T101154色胺98%61-54-15g,25g,100g,500ghTAAR11.08 μM
T105543酪胺98%51-67-21g,5g,25g,100g,500ghTAAR134 nM

*前列腺素受体

项目号产品名称规格CAS包装
B129831Bimatoprost≥99%155206-00-110mg,50mg,100mg,500mg
P129960Prostaglandin E1≥98%(HPLC)745-65-35mg,25mg,100mg
D133402Dinoprostone98%363-24-61mg,10mg,25mg
D136300Dinoprost≥99%38562-01-51mg,5mg,25mg,100mg
E129511 Ethamsylate≥98%2624-44-41g,5g,25g,100g
,
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(下)

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

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按靶点分类:

*多巴胺受体



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项目号产品名称规格CAS包装靶点IC50KiED50EC50
B129216Benztropine mesylate≥98%132-17-21g,5gDAT118 nM
C131611盐酸氯丙嗪≥98%(HPLC)69-09-05g,25g,100g多巴胺受体6.1 μM
钾离子通道16 μM
C129569盐酸氯丙嗪分析标准品69-09-0250mg多巴胺受体6.1 μM
钾离子通道16 μM
C125175Clemizole≥98%442-52-45mg,25mg,100mg组胺H1受体
B129446Amfebutamone (Bupropion) HCl≥98% (HPLC)31677-93-7250mg,1g,5g多巴胺受体3.4 μM
AChR6.5 μM
T162449三氟拉嗪二盐酸盐>98.0%(HPLC)(T)440-17-55g,25g,100g多巴胺D2受体1.1 nM
D129436Domperidone≥98%57808-66-950mg,250mg,1g,5g,25g,100g多巴胺D2受体
M129977Methyldopa Sesquihydrate≥98%555-30-61g,5g,25g多巴脱羧酶21.8 mg/kg
O126519Olanzapine≥99%132539-06-11g,5g多巴胺D2受体
5-HT2
Q129431Quetiapine Fumarate≥98%111974-72-21g,5g多巴胺受体
E129717Ziprasidone HCl≥98%122883-93-6250mg,1g5-HT
多巴胺受体
A129432Amisulpride≥98%71675-85-950mg,250mg,1g多巴胺受体
P120141帕利哌酮98%144598-75-410mg,50mg,250mg,1g,5g,25g多巴胺受体
H113852氟**醇98%52-86-85g,25g
C129441Chlorprothixene≥98%113-59-750mg,250mg多巴胺D1受体 18 nM
多巴胺D2受体 2.96 nM
多巴胺D3受体 4.56 nM
多巴胺D5受体 9 nM
组胺H1受体3.75 nM
5-HT29.4 nM
5-HT63 nM
5-HT75.6 nM
P108682吩噻嗪分析标准品92-84-2250mg多巴胺-2(D2)受体
P108681吩噻嗪98%92-84-2100g,500g,5kg多巴胺-2(D2)受体
D129475Droperidol≥98%548-73-250mg,250mg,1g
L129452Levosulpiride≥98%23672-07-35g,25g多巴胺D2受体
T101543延胡索乙素97%2934-97-61g,5g
T101542延胡索乙素分析标准品,>97%2934-97-6250mg
P160649Perphenazine>97.0%58-39-95g,25g多巴胺D1/D2受体
H1972336-羟基多巴胺氢溴酸盐95%636-00-050mg,250mg,1g
C171261Chlorprothixene hydrochloride98%6469-93-81g
T162447三氟丙嗪盐酸盐>98.0%(HPLC)1098-60-81g,5g
P160772Penfluridol>97.0%(HPLC)26864-56-2200mg,1g多巴胺受体1.6 μM
M132784Molindone Hydrochloride≥98.0%(HPLC)15622-65-8100mg,250mg,1g,5g,25g多巴胺D2/D5受体
R136626Rotundine≥98%483-14-7100mg,250mg,500mg多巴胺D1受体
P160775Sulpiride>98.0%(HPLC)15676-16-15g,25g,100g多巴胺D2受体
T135203丁苯那嗪98%58-46-8250mg,1g,5g
A129598Azaperone≥99%1649-18-950mg,250mg多巴胺受体
C184839Chlorpromazine95%50-53-31g,5g
M124438甲氧氯普胺98%364-62-55g,25g多巴胺受体
C171931Cariprazine hydrochloride97%1083076-69-01g多巴胺D2/D3受体
D111048左旋多巴99%59-92-725g,100g,500g多巴胺受体
D111049左旋多巴分析标准品,>99%59-92-720mg多巴胺受体
A109736盐酸金刚烷胺99%(T)665-66-75g,25g,100g,500g多巴胺受体