GPCR/Proteína-G
Os inibidores de GPCR/proteínas G são compostos que têm como alvo os receptores acoplados a proteínas G (GPCRs) e as proteínas G associadas, que desempenham papéis críticos na transmissão de sinais do exterior para o interior das células. Esses inibidores são essenciais para estudar as vias de sinalização mediadas por GPCRs, que estão envolvidas em numerosos processos fisiológicos, incluindo percepção sensorial, resposta imunológica e neurotransmissão. Os inibidores de GPCR também são importantes no desenvolvimento de medicamentos, pois muitos agentes terapêuticos têm como alvo esses receptores. Na CymitQuimica, oferecemos uma ampla gama de inibidores de GPCR/proteínas G de alta qualidade para apoiar sua pesquisa em farmacologia, biologia celular e áreas afins.
Subcategorias de "GPCR/Proteína-G"
- Receptor 5-HT(942 produtos)
- Receptor de adenosina(242 produtos)
- Receptor adrenérgico(2.948 produtos)
- Receptor de Bombesina(30 produtos)
- Receptor de Bradicinina(59 produtos)
- CXCR(149 produtos)
- CaSR(32 produtos)
- Receptor de Canabinóides(195 produtos)
- Receptor de Dopamina(409 produtos)
- Receptor Endotelina(75 produtos)
- Receptor GNRH(73 produtos)
- GPCR19(31 produtos)
- GRK(32 produtos)
- GTPase(21 produtos)
- Receptor Glucagon(166 produtos)
- Hedgehog/Smoothened(45 produtos)
- Receptor de Histamina(359 produtos)
- Receptor LPA(21 produtos)
- Receptor de Melatonina(24 produtos)
- Receptor OX(40 produtos)
- Receptor opioide(298 produtos)
- PAFR(11 produtos)
- PKA(49 produtos)
- Receptor S1P(17 produtos)
- SGLT(30 produtos)
- Receptor Sigma(46 produtos)
Exibir 18 mais subcategorias
Foram encontrados 5373 produtos de "GPCR/Proteína-G"
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Merigolix
CAS:<p>Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist .</p>Fórmula:C36H35F7N4O6Cor e Forma:SolidPeso molecular:752.68MK-0812
CAS:<p>MK-0812 is a dual antagonist of the CCR2 and CCR5 receptors that can alleviate adipose inflammation in ob/ob mice.</p>Fórmula:C24H34F3N3O3Pureza:98%Cor e Forma:SolidPeso molecular:469.54LY210073
CAS:<p>LY210073 is an antagonist of the Leukotriene B4 (LTB4) receptor (IC50: 6.2 nM).</p>Fórmula:C30H28O8Pureza:98%Cor e Forma:SolidPeso molecular:516.54MRGPRX2 modulator-1
CAS:<p>MRGPRX2 modulator-1 (example 17), a modulator of the mas-related G-protein receptor X2 (MRGPRX2), is employed in studies focused on inflammation, pain, and autoimmune disorders [1].</p>Fórmula:C20H19F6N5OCor e Forma:SolidPeso molecular:459.39LPA2 antagonist 5
CAS:<p>LPA2 antagonist 5 (EX1) functions as an antagonist of LPA2, with an IC50 value of 4.05 nM.</p>Fórmula:C17H17F3N2O5Cor e Forma:SolidPeso molecular:386.323Methacycline
CAS:<p>Methacycline, a tetracycline antibiotic, inhibits bacterial protein synthesis and effectively suppresses epithelial-mesenchymal transition (EMT). It blocks EMT in vitro and inhibits fibrogenesis in vivo without directly affecting the TGF-β1Smad signaling pathway. As an antimicrobial agent, Methacycline holds potential for research in pulmonary fibrosis.</p>Fórmula:C22H22N2O8Cor e Forma:SolidPeso molecular:442.42PD 140376
CAS:<p>PD 140376: Selective CCK-B/gastrin receptor antagonist radioligand for guinea pig stomach & brain.</p>Fórmula:C33H40N4O5Pureza:98%Cor e Forma:SolidPeso molecular:572.69GRK6-IN-5
CAS:<p>GRK6-IN-5 is an inhibitor of the GRK6 polypeptide, with an IC50 of 4.48 μM. GRK6-IN-5 is utilized in research focused on hematological malignancies, inflammatory diseases, and autoimmune disorders.</p>Fórmula:C23H21N3O2Cor e Forma:SolidPeso molecular:371.432Mrgx2 antagonist-3
CAS:<p>Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of the MrgX2 receptor, with an IC50 range of 0.042-2.5 nM. It blocks downstream G protein signaling and β-arrestin recruitment, inhibiting Mrgx2 receptor-mediated calcium influx and cell degranulation. Mrgx2 antagonist-3 shows potential for research in inflammation-associated diseases and pruritus, such as chronic urticaria and allergic asthma.</p>Fórmula:C15H15F2N3OCor e Forma:SolidPeso molecular:291.30Fasitibant
CAS:<p>Fasitibant is a potent and selective nonpeptide kinin B2 receptor antagonist.</p>Fórmula:C36H49Cl2N6O6SCor e Forma:SolidPeso molecular:764.78CHF-6366
CAS:<p>CHF-6366: M3 antagonist & β2 agonist (pKi 10.4/11.4), mild Ca channel blocker, used in COPD study.</p>Fórmula:C42H48N6O8Cor e Forma:SolidPeso molecular:764.87Zafirlukast metabolite M1
CAS:<p>Zafirlukast metabolite M1 (compound 15) is an inhibitor used in the treatment of asthma and other allergic pulmonary conditions, effectively antagonizing leukotriene activity.</p>Fórmula:C25H25N3O4SCor e Forma:SolidPeso molecular:463.549GnRH-R antagonist 1
CAS:<p>Compound 21a: Oral GnRH-R antagonist, IC50=0.57 nM, potent against prostate cancer/prevents LH surges.</p>Fórmula:C31H28F5N7O6SPureza:98%Cor e Forma:SolidPeso molecular:721.65UMB24
CAS:<p>UMB24 is an effective antagonist of the σ2 receptor, exhibiting dissociation constants (Ki values) of 170 nM for the σ2 receptor and 322 nM for the σ1 receptor. This compound mitigates cocaine-induced convulsions and hyperactivity without causing mortality.</p>Fórmula:C17H21N3Cor e Forma:SolidPeso molecular:267.37PF-06372222
CAS:<p>PF-06372222: a small-molecule that modulates GCGR and antagonizes GLP-1R, affecting insulin and glucagon.</p>Fórmula:C26H28F3N5O3Pureza:98%Cor e Forma:SolidPeso molecular:515.53EP4 receptor antagonist 7
CAS:<p>EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.</p>Fórmula:C24H18F3N3O3Cor e Forma:SolidPeso molecular:453.413SR 140333
CAS:<p>SR 140333 is a NK1 receptor antagonist.</p>Fórmula:C37H45Cl3N2O2Pureza:98%Cor e Forma:SolidPeso molecular:656.12Lp(a)-IN-8
CAS:<p>LPA2 antagonist 3 (compound 15) serves as an Lp(a) antagonist. Lp(a) is a pathogenic risk factor for atherosclerotic cardiovascular disease (ASCVD).</p>Fórmula:C21H40Cl2N4O5Cor e Forma:SolidPeso molecular:499.472CCG258208
CAS:<p>GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).</p>Fórmula:C24H25FN4O4Pureza:98%Cor e Forma:SolidPeso molecular:452.48Gemilukast
CAS:<p>Gemilukast (ONO-6950) is a cysteinyl leukotriene 1 and 2 receptor inhibitor that inhibits bronchoconstriction and is used in the treatment of asthma.</p>Fórmula:C36H37F2NO5Pureza:98.27% - 99.5%Cor e Forma:SolidPeso molecular:601.68Pareptide monohydrochloride
CAS:<p>Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).</p>Fórmula:C14H27ClN4O3Pureza:98%Cor e Forma:SolidPeso molecular:334.84Tebideutorexant
CAS:<p>Tebideutorexant, an orexin-1 receptor antagonist, shows anti-panic effects in rodents and humans, providing a tool for stress response and psychiatric research.</p>Fórmula:C23H16D2F4N4O2Pureza:98.89%Cor e Forma:SolidPeso molecular:460.42LPA2 antagonist 6
CAS:<p>LPA2 antagonist 6 (example 2) acts as an antagonist of Lp(a). It inhibits the formation of Lp(a) with an IC50 value of 2.33 nM, making it useful for cardiovascular disease research.</p>Fórmula:C26H34Cl2N2O6Cor e Forma:SolidPeso molecular:541.464(S)-Bucindolol
CAS:(S)-Bucindolol is an enantiomer of bucindolol, specifically a β1-adrenergic receptor antagonist. It is primarily utilized in research related to heart failure.Fórmula:C22H25N3O2Cor e Forma:SolidPeso molecular:363.45BI 703704
CAS:<p>BI 703704, a soluble guanylate cyclase (sGC) activator, inhibits the progression of diabetic nephropathy in the ZSF1 rat [1].</p>Fórmula:C32H37N3O4SPureza:98%Cor e Forma:SolidPeso molecular:559.72APJ receptor agonist 3
CAS:<p>APJ receptor agonist 3 is a highly effective and orally administerable agonist of the APJ receptor, demonstrating a potent EC50 value of 0.027 nM.</p>Fórmula:C26H29ClN4O5Cor e Forma:SolidPeso molecular:512.98Danavorexton
CAS:<p>Danavorexton is an orexin receptor agonist.</p>Fórmula:C21H32N2O5SCor e Forma:SolidPeso molecular:424.55NMDAR antagonist 5
CAS:<p>NMDAR antagonist 5 (Compound A17) is a multi-target antagonist that acts on NMDAR and monoamine transporters (SERT, DAT, and NET). It demonstrates strong NMDAR antagonistic efficacy (IC50= 0.3 μM) and effective activity on monoamine transporters (SERT IC50= 1.1 μM, DAT IC50= 0.7 μM, NET IC50= 2.7 μM). NMDAR antagonist 5 exhibits high safety with low toxicity (hepatic and renal toxicity IC50> 100 μM; cardiac toxicity IC50= 24.5 μM). It has antidepressant properties and is useful for depression research.</p>Fórmula:C17H21N3Cor e Forma:SolidPeso molecular:267.369Nocloprost
CAS:<p>Nocloprost (SH 475) is a prostaglandin E2 (PGE2) analog, an EP1 and EP3 receptor agonist with local gastric protection and ulcer healing effects.</p>Fórmula:C22H37ClO4Cor e Forma:SolidPeso molecular:400.98Sigma-1 receptor antagonist 6
CAS:<p>Sigma-1 receptor antagonist 6 (Compound 12), a σ1R antagonist, demonstrates significant antiallodynic effects by targeting the Sigma-1 receptor (σ1R). This compound is effective in animal models for neuropathic pain, particularly for reducing mechanical allodynia caused by paclitaxel.</p>Fórmula:C32H34N6Cor e Forma:SolidPeso molecular:502.65S1P1 agonist 4
CAS:<p>S1P1 agonist 4 exhibits enhanced potency with an EC 50 value of less than 0.05 mg/kg and a predicted human half-life (t1/2) of approximately 5 days, indicating</p>Fórmula:C24H31NO3Cor e Forma:SolidPeso molecular:381.51LY 245769
CAS:<p>LY 245769 is an inhibitor of leukotriene E4 (LTE4).</p>Fórmula:C25H33F3N8OSPureza:98%Cor e Forma:SolidPeso molecular:550.64D4R antagonist-1
<p>Potent, selective D4R antagonist; IC50 = 6.87 µM; potential in Parkinson’s disease research.</p>Fórmula:C21H25F2NO2Cor e Forma:SolidPeso molecular:361.43AL 8810
CAS:<p>AL-8810 is an 11β-fluoro analog of PGF 2α with selective antagonist effects at the PGF 2α receptor (FP receptor) [1].</p>Fórmula:C24H31FO4Cor e Forma:SolidPeso molecular:402.5UK-432097
CAS:<p>UK 432097 is an adenosine A2A agonist.</p>Fórmula:C40H47N11O6Cor e Forma:SolidPeso molecular:777.87TAAR1 agonist 2
CAS:<p>TAAR1 agonist 2 (compound 30), a full agonist at trace amine-associated receptor 1 (TAAR1) (pEC50=7.5), also displays agonistic properties at H1 receptors and activates various muscarinic acetylcholine receptors, including the M2 receptor (pEC50=5). This compound is utilized in researching neuropsychiatric diseases.</p>Fórmula:C9H11NOCor e Forma:SolidPeso molecular:149.19ZK118182 isopropyl ester
CAS:<p>ZK118182 isopropyl ester is a PG analog with potent DP-agonist activity (EC50 = 16.5 nM) and high affinity for the DP receptor (Ki = 74 nM).</p>Fórmula:C23H37ClO5Pureza:98%Cor e Forma:SolidPeso molecular:428.99D4R antagonis-2
<p>Potent D4R antagonist-2: selective, IC50=6.52 μM, good in vitro PK and brain penetration, potential for Parkinson's research.</p>Fórmula:C21H23ClF2N2O2Cor e Forma:SolidPeso molecular:408.87Protease-Activated Receptor-1 antagonist 2
<p>Selective, orally active PAR-1 antagonist with an IC50 of 7 nM, potential for cardiovascular disease studies.</p>Cor e Forma:SolidDopamine D3 receptor antagonist-2
<p>Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor selective (Ki=2.16 nM) or multi-targeting dual ligand that shows potential effects in CNS disorders.</p>Fórmula:C23H27Cl2N3O3Cor e Forma:SolidPeso molecular:464.38SGL5213
CAS:<p>SGL5213 is a potent oral SGLT1 inhibitor (IC50: 29 nM) with potential for treating type 2 diabetes.</p>Fórmula:C37H55N3O8Pureza:98%Cor e Forma:SolidPeso molecular:669.85Ici D1542
CAS:Ici D1542: potent TXS inhibitor & TXA2 receptor antagonist, effective thromboxane blocker in vitro.Fórmula:C25H30N2O7Pureza:98%Cor e Forma:SolidPeso molecular:470.51IRL 2500
CAS:<p>IRL 2500 is an antagonist of Endothelin receptor with IC50s of 1.3 and 94 nM for Endothelin A receptor and Endothelin B receptor.</p>Fórmula:C36H35N3O4Pureza:99.36%Cor e Forma:White Crystalline SolidPeso molecular:573.68Becondogrel
CAS:<p>Becondogrel (2-Oxoclopidogrel) is a metabolite of Clopidogrel. It irreversibly inhibits the P2Y12 receptor, thereby preventing platelet aggregation and thrombosis.</p>Fórmula:C16H16ClNO3SCor e Forma:SolidPeso molecular:337.821Mafoprazine
CAS:<p>Mafoprazine, a phenylpiperazine derivative, exhibits varying affinities for neuronal receptors, primarily exerting its antipsychotic effects through blocking D2 receptors and enhancing α-adrenergic activity. It also increases the activity of dopamine metabolites.</p>Fórmula:C22H28FN3O3Cor e Forma:SolidPeso molecular:401.47Abarelix acetate
CAS:<p>Abarelix acetate: synthetic GnRHR antagonist, spikes histamine, lowers LH and testosterone temporarily, used in advanced prostate cancer.</p>Fórmula:C72H95ClN14O14·xC2H4O2Cor e Forma:SolidPeso molecular:1476.14RBM10-8
CAS:<p>RBM10-8 irreversibly inhibits human sphingosine-1- phosphate lyase (hS1PL) while behaving also as an enzyme substrate.</p>Fórmula:C17H36NO5PCor e Forma:SolidPeso molecular:365.45LY 292728
CAS:<p>LY 292728 is a highly potent antagonist of leukotriene B4 receptor.</p>Fórmula:C34H29FO9Pureza:98%Cor e Forma:SolidPeso molecular:600.59Nedemelteon
CAS:<p>Nedemelteon is an agonist of the melatonin receptor (melatonin receptor).</p>Fórmula:C15H18N2O2Cor e Forma:SolidPeso molecular:258.325-HT2A/5-HT2C inverse agonist 1
CAS:<p>5-HT2A/5-HT2C inverse agonist 1 serves as a dual and potent inverse agonist for the 5-HT2A and 5-HT2C receptors, with hERG inhibition properties that mitigate cardiovascular risks. Demonstrating significant antipsychotic efficacy in the MK-801-induced mouse model, this compound holds potential for psychosis research.</p>Fórmula:C24H35N5O2Cor e Forma:SolidPeso molecular:425.57
