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GPCR/Proteína-G

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"

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Foram encontrados 5352 produtos de "GPCR/Proteína-G"

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  • Rodatristat ethyl

    CAS:
    <p>Rodatristat ethyl is an oral TPH1 inhibitor reducing 5-HT levels &amp; lowering PAH at low doses.</p>
    Fórmula:C29H31ClF3N5O3
    Pureza:98%
    Cor e Forma:Solid
    Peso molecular:590.04
  • UR-AK49

    CAS:
    <p>UR-AK49 (compound 11) is an agonist for the human histamine H1 and H2 receptors. It exhibits an EC50 of 23 nM in the GTPase assay involving hH2R-Gsalpha fusion protein expressed in Sf9 insect cells. UR-AK49 is applicable in neurologically related research.</p>
    Fórmula:C16H27N5O
    Cor e Forma:Solid
    Peso molecular:305.42
  • APJ receptor agonist 8

    CAS:
    <p>APJ receptor agonist 8 is a small molecule agonist of the APJ receptor, enhancing load-independent cardiac contractility in isolated perfused rat hearts.</p>
    Fórmula:C24H27N7O5S
    Pureza:98.31% - 99.60%
    Cor e Forma:Solid
    Peso molecular:525.58
  • Remlifanserin

    CAS:
    <p>Remlifanserin is a potent inverse agonist of the serotonin receptor (5-HT2A).</p>
    Fórmula:C24H29F2N3O2
    Cor e Forma:Solid
    Peso molecular:429.50
  • O-1269

    CAS:
    <p>O-1269 acts as a partial agonist for the cannabinoid receptor 1 (CB1R), with a binding affinity (Ki) of 32 nM. Additionally, it exhibits analgesic properties.</p>
    Fórmula:C22H22Cl3N3O
    Cor e Forma:Solid
    Peso molecular:450.79
  • MF-592

    CAS:
    <p>MF-592: EP4 receptor antagonist, hEP4 IC50 3 nM, hWB IC50 78 nM, great oral PK, rat arthritis ED50 0.1 mg/kg/day, promising for development.</p>
    Fórmula:C34H33Cl2N3O6S
    Cor e Forma:Solid
    Peso molecular:682.61
  • SB 258741 hydrochloride


    <p>SB 258741 hydrochloride is a potent antagonist of the 5-HT 7 receptor, designed specifically for studying schizophrenia [1].</p>
    Fórmula:C19H31ClN2O2S
    Cor e Forma:Solid
    Peso molecular:386.98
  • Metrazoline

    CAS:
    <p>Metrazoline (o-Methyl-tracizoline) acts as a ligand for adrenergic receptors (low affinity) and imidazoline I2 receptors.</p>
    Fórmula:C14H16N2O4
    Cor e Forma:Solid
    Peso molecular:276.288
  • FDU-PB-22

    CAS:
    <p>FDU-PB-22, a novel synthetic cannabinoid, undergoes rapid metabolism in human liver microsomes (HLM) with a half-life of 12.4 minutes.</p>
    Fórmula:C26H18FNO2
    Cor e Forma:Solid
    Peso molecular:395.43
  • HU-308

    CAS:
    <p>HU-308, a synthetic cannabinoid analogue, is a highly selective agonist of the CB2 receptor. It demonstrates an affinity for the CB2 receptor that is over 440 times greater than its affinity for the CB1 receptor, which are predominantly found in immune cells. This compound plays a crucial role in modulating the immunosuppressive effects of the endocannabinoid system (ECS). Additionally, HU-308 possesses anti-inflammatory and neuroprotective properties, and it regulates the function of microglia. Its potential applications include research into neuroinflammation and retinal diseases.</p>
    Fórmula:C27H42O3
    Cor e Forma:Solid
    Peso molecular:414.62
  • CCR1 antagonist 13

    CAS:
    <p>CCR1 antagonist13 is a selective small molecule antagonist of CCR1.</p>
    Fórmula:C25H27ClFN3O4
    Cor e Forma:Solid
    Peso molecular:487.95
  • Opipramol dihydrochloride

    CAS:
    <p>Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA) primarily functioning as a sigma (σ) receptor agonist. It interacts effectively with sigma recognition sites, having a Ki value of 50 nM. Opipramol is applicable in the study of generalized anxiety disorder (GAD).</p>
    Fórmula:C23H31Cl2N3O
    Cor e Forma:Solid
    Peso molecular:436.418
  • CB2R/5-HT1AR agonist 1

    CAS:
    <p>Compound 2o, also known as CB2R/5-HT1AR agonist 1, serves as a partial orally active agonist for the CB2 receptor (EC50 = 479.6 nM) and a full agonist for the 5-HT1A receptor (EC50 = 2.7 μM). This compound demonstrates both anti-anxiety and anti-depressive effects and has favorable pharmacokinetic properties [1].</p>
    Fórmula:C24H33NO3
    Cor e Forma:Solid
    Peso molecular:383.52
  • MDA77

    CAS:
    <p>MDA77 is a CB2 agonist with an EC50 value of 5.82 nM and exhibits no activity towards CB1.</p>
    Fórmula:C21H23N3O3
    Cor e Forma:Solid
    Peso molecular:365.43
  • Befiradol hydrochloride

    CAS:
    <p>Befiradol HCl (NLX-112) is a selective 5-HT1A receptor agonist with anxiolytic effects and prevents ATXN3 aggregation.</p>
    Fórmula:C20H23Cl2F2N3O
    Pureza:99.1%
    Cor e Forma:Solid
    Peso molecular:430.32
  • 5-HT7R antagonist 3

    CAS:
    <p>Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.</p>
    Fórmula:C30H33FN4O3
    Cor e Forma:Solid
    Peso molecular:516.61
  • Dopamine 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:C23H27Cl2N3O3
    Cor e Forma:Solid
    Peso molecular:464.38
  • SAR-114137

    CAS:
    <p>SAR-114137 is a histone sphingomyelin kinase inhibitor used in the study of molluscum arteriosum and peripheral neuropathic pain.</p>
    Fórmula:C25H34N4O7S
    Pureza:99.09% - 99.91%
    Cor e Forma:Solid
    Peso molecular:534.63
  • Flucopride

    CAS:
    <p>Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments.</p>
    Fórmula:C22H33FN2O2
    Cor e Forma:Solid
    Peso molecular:376.51
  • Sulfinalol hydrochloride

    CAS:
    <p>Sulfinalol hydrochloride is an orally active β-adrenoceptor (β-adrenoceptor) antagonist that exhibits direct vasodilatory activity. It is also classified as an antihypertensive agent.</p>
    Fórmula:C20H28ClNO4S
    Cor e Forma:Solid
    Peso molecular:413.96
  • Ro-24-4736

    CAS:
    <p>Ro 24-4736 is an effective and selective platelet-activating factor antagonist.</p>
    Fórmula:C31H20ClN5OS
    Pureza:98%
    Cor e Forma:Solid
    Peso molecular:546.04
  • AChE-IN-5


    <p>AChE-IN-5: oral, crosses blood-brain barrier, targets AChE/5-HT1A/SERT, potent with 2.29 nM IC50.</p>
    Fórmula:C38H45N5O
    Cor e Forma:Solid
    Peso molecular:587.8
  • AGH-107

    CAS:
    <p>AGH-107 is a highly selective 5-HT7 receptor agonist that can cross the blood-brain barrier, featuring a Ki value of 6 nM and an EC50 value of 19 nM. Demonstrating high selectivity for central nervous system targets, AGH-107 also exhibits high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.</p>
    Fórmula:C13H12IN3
    Cor e Forma:Solid
    Peso molecular:337.16
  • Tipindole

    CAS:
    <p>Tipindole is a serotonin antagonist utilized in research related to depression.</p>
    Fórmula:C16H20N2O2S
    Cor e Forma:Solid
    Peso molecular:304.41
  • ASP-2205

    CAS:
    <p>ASP-2205, a 5-HT2C receptor agonist (human 5-HT2C receptor, EC50=0.85 nM; rat 5-HT2C receptor, EC50=2.5 nM), enhances the urethral closure reflex mediated by the genital nerve, thereby preventing urinary incontinence.</p>
    Fórmula:C19H28N2O
    Cor e Forma:Solid
    Peso molecular:300.44
  • YM-49598 iodide

    CAS:
    <p>YM-49598 iodide is a tachykinin NK-1 receptor antagonist. It inhibits drug-induced bladder contractions in rats with an IC50 of 11 μg/kg.</p>
    Fórmula:C36H45Cl2IN2O2
    Cor e Forma:Solid
    Peso molecular:735.57
  • D4R antagonist-1


    <p>Potent, selective D4R antagonist; IC50 = 6.87 µM; potential in Parkinson’s disease research.</p>
    Fórmula:C21H25F2NO2
    Cor e Forma:Solid
    Peso molecular:361.43
  • CCG258208

    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:C24H25FN4O4
    Pureza:98%
    Cor e Forma:Solid
    Peso molecular:452.48
  • Etoperidone

    CAS:
    <p>Etoperidone is an antidepressant that acts as an orally active reuptake inhibitor for serotonin (serotonin) and noradrenaline (nor-adrenaline). It demonstrates specific binding affinities (Kd) for several receptors: 36 nM at the 5-HT2 receptor, 38 nM at the α1-adrenergic receptor (α1-adrenergic receptor), 85 nM at the 5-HT1A receptor, and 570 nM at the α2-adrenergic receptor (α2-adrenergic receptor).</p>
    Fórmula:C19H28ClN5O
    Cor e Forma:Solid
    Peso molecular:377.91
  • Substituted piperidines-1

    CAS:
    <p>Substituted piperidines-1 can promote the release of growth hormone in humans and animals.</p>
    Fórmula:C29H39N7O2
    Pureza:98%
    Cor e Forma:Solid
    Peso molecular:517.67
  • UMB24

    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:C17H21N3
    Cor e Forma:Solid
    Peso molecular:267.37
  • UNC10099984A

    CAS:
    <p>UNC10099984A (Compound 6) is a functionally selective ligand for the dopamine D2 receptor, exhibiting a Ki value of 4.6 nM and an EC50 of 6.2 nM for β-arrestin. This compound is useful for research into central nervous system diseases related to the D2 receptor.</p>
    Fórmula:C24H29Cl2N3O2
    Cor e Forma:Solid
    Peso molecular:462.41
  • MrgprX2 antagonist-7


    <p>MrgprX2 antagonist-7 is an anti-allergic agent with significant anti-allergic effects and inhibits mast cell degranulation.</p>
    Fórmula:C24H22ClF3N6O3
    Cor e Forma:Solid
    Peso molecular:534.92
  • MRS4865

    CAS:
    <p>MRS4865 (compound 7a) serves as a chimeric antagonist for the P2Y14 receptor and an agonist for UDP-glucose, offering protection against neuropathic pain.</p>
    Fórmula:C39H39F3N4O7
    Cor e Forma:Solid
    Peso molecular:732.74
  • LK 11

    CAS:
    <p>LK-11, an alkaloid derivative, inhibits the passive uptake of norepinephrine (NA) by synaptic vesicles in the thalamus, similarly to cocaine.</p>
    Fórmula:C15H26N2O3
    Cor e Forma:Solid
    Peso molecular:282.38
  • AA 497 (Free Base)

    CAS:
    <p>AA 497, a beta-2 agonist, causes relaxation and suppresses Ca spike frequency.</p>
    Fórmula:C14H21NO3
    Pureza:98%
    Cor e Forma:Solid
    Peso molecular:251.32
  • (±)-Penbutolol

    CAS:
    <p>(±)-Penbutolol ((Rac)-Penbutolol) is the racemic form of Penbutolol. It acts as an orally active β-adrenergic receptor antagonist. (±)-Penbutolol mitigates the tachycardia induced by exercise, reduces the increase in peak expiratory flow rate (PEFR) caused by physical activity, and decreases plasma renin activity (PRA) at rest. The peak plasma concentration of this compound is achieved one hour after oral administration, with a half-life of 4.5 hours, and it is metabolized into active metabolites in the body. This compound is utilized in research related to cardiovascular diseases.</p>
    Fórmula:C18H29NO2
    Cor e Forma:Solid
    Peso molecular:291.43
  • RS 61756-007

    CAS:
    <p>RS 61756-007 is a selective thromboxane receptor (TP) agonist.</p>
    Fórmula:C23H28O5
    Pureza:98%
    Cor e Forma:Solid
    Peso molecular:384.47
  • Pareptide monohydrochloride

    CAS:
    <p>Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).</p>
    Fórmula:C14H27ClN4O3
    Pureza:98%
    Cor e Forma:Solid
    Peso molecular:334.84
  • SGL5213

    CAS:
    <p>SGL5213 is a potent oral SGLT1 inhibitor (IC50: 29 nM) with potential for treating type 2 diabetes.</p>
    Fórmula:C37H55N3O8
    Pureza:98%
    Cor e Forma:Solid
    Peso molecular:669.85
  • PF-07258669

    CAS:
    <p>PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite.</p>
    Fórmula:C25H27FN6O2
    Pureza:99.9%
    Cor e Forma:Solid
    Peso molecular:462.52
  • Treprostinil diethanolamine

    CAS:
    <p>Treprostinil diethanolamine (UT-15C) is a potent agonist of EP2, DP1 and IP, with values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1,</p>
    Fórmula:C27H45NO7
    Pureza:99.86%
    Cor e Forma:Solid
    Peso molecular:495.65
  • BMS-986141

    CAS:
    <p>BMS-986141(UDM-003183) is a selective and potent protease-activated receptor-4 (PAR-4) antagonist with oral activity and an IC50 value of 0.4 nM.BMS-98614</p>
    Fórmula:C27H23N5O5S2
    Pureza:98.43% - 99.26%
    Cor e Forma:Solid
    Peso molecular:561.63
  • SB-224289 hydrochloride

    CAS:
    <p>SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.</p>
    Fórmula:C32H33ClN4O3
    Pureza:97.82% - 98.99%
    Cor e Forma:Solid
    Peso molecular:557.08
  • Vofopitant dihydrochloride

    CAS:
    <p>Vofopitant dihydrochloride (GR 205171A) is a tachykinin NK1 receptor antagonist and a potential compound for the treatment of pathologic vomiting.</p>
    Fórmula:C21H25Cl2F3N6O
    Pureza:98.99%
    Cor e Forma:Solid
    Peso molecular:505.36
  • Dersimelagon

    CAS:
    <p>Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist.Cost-effective and quality-assured.</p>
    Fórmula:C36H45F4N3O5
    Pureza:97.35% - 98.23%
    Cor e Forma:Solid
    Peso molecular:675.75
  • SB-423562

    CAS:
    <p>SB-423562 is a calcium-sensing receptor (CaSR) antagonist and can be used in studies about osteoporosis.</p>
    Fórmula:C26H32N2O4
    Pureza:99.22%
    Cor e Forma:Solid
    Peso molecular:436.54
  • LSN3318839

    CAS:
    <p>LSN3318839 is a potent and orally available glucagon-like peptide-1 receptor (GLP-1R) modulator.LSN3318839 enhances GLP-1R G-protein-coupled signaling and can</p>
    Fórmula:C26H23Cl2N3O2
    Pureza:99.21%
    Cor e Forma:Solid
    Peso molecular:480.39
  • Vofopitant

    CAS:
    <p>Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).</p>
    Fórmula:C21H23F3N6O
    Pureza:97.86%
    Cor e Forma:Solid
    Peso molecular:432.44
  • AZD-5672

    CAS:
    <p>AZD-5672 is an antagonist of CCR5 with an IC50 of 0.32 nM.</p>
    Fórmula:C32H38F2N2O5S2
    Pureza:98.1%
    Cor e Forma:Solid
    Peso molecular:632.78