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Proteina G/GPCR

Proteina G/GPCR

Gli inibitori dei GPCR/proteine G sono composti che bersagliano i recettori accoppiati alle proteine G (GPCR) e le proteine G associate, che svolgono ruoli critici nella trasmissione dei segnali dall'esterno all'interno delle cellule. Questi inibitori sono essenziali per studiare le vie di segnalazione mediate dai GPCR, coinvolte in numerosi processi fisiologici, tra cui la percezione sensoriale, la risposta immunitaria e la neurotrasmissione. Gli inibitori dei GPCR sono anche importanti nello sviluppo di farmaci, poiché molti agenti terapeutici prendono di mira questi recettori. Presso CymitQuimica, offriamo una vasta gamma di inibitori dei GPCR/proteine G di alta qualità per supportare le tue ricerche in farmacologia, biologia cellulare e campi correlati.

Sottocategorie di "Proteina G/GPCR"

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Trovati 5838 prodotti di "Proteina G/GPCR"

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  • 5-HT7R antagonist 1


    5-HT7R antagonist 1 is a G protein-biased antagonist with Ki of 6.5 nM for 5-HT 7R.
    Formula:C14H18Cl2N4
    Colore e forma:Solid
    Peso molecolare:313.23
  • Nipradolol

    CAS:
    Nipradolol blocks alpha-1-adrenergic receptors, lowers IOP in rabbits, and reduces NA-induced muscle contraction and dog artery vasodilation.
    Formula:C15H22N2O6
    Colore e forma:Solid
    Peso molecolare:326.35
  • MK-3207

    CAS:
    MK-3207 is a potent, oral CGRP receptor antagonist with high selectivity for human and monkey receptors, inhibiting blood flow in vivo.
    Formula:C31H29F2N5O3
    Colore e forma:Solid
    Peso molecolare:557.59
  • WIN 66306

    CAS:
    WIN 66306: Cyclic heptapeptide, blocks NK1/NK2 receptors, inhibits substance P-triggered contractions in guinea pig ileum.
    Formula:C41H52N8O9
    Colore e forma:Solid
    Peso molecolare:800.9
  • CP-199330

    CAS:
    CP-199330: non-toxic alternative to Zafirlukast & Pranlukast, blocks cysteyl LT1 receptors.
    Formula:C28H24ClF3N2O6S
    Colore e forma:Solid
    Peso molecolare:609.01
  • Cannabigerovarin

    CAS:
    Cannabigerovarin (CBGV) is a compound categorized as a phytocannabinoid.
    Formula:C19H28O2
    Peso molecolare:288.42
  • LPA2 antagonist 5

    CAS:
    LPA2 antagonist 5 (EX1) functions as an antagonist of LPA2, with an IC50 value of 4.05 nM.
    Formula:C17H17F3N2O5
    Colore e forma:Solid
    Peso molecolare:386.323
  • GPBAR1-IN-3

    CAS:
    GPBAR1-IN-3 (Compound 14) is both a selective agonist for GPBAR1, with an EC50 value of 0.17 μM, and an antagonist for CysLT1R [1].
    Formula:C21H23NO2
    Colore e forma:Solid
    Peso molecolare:321.41
  • AL 8810

    CAS:
    AL-8810 is an 11β-fluoro analog of PGF 2α with selective antagonist effects at the PGF 2α receptor (FP receptor) [1].
    Formula:C24H31FO4
    Colore e forma:Solid
    Peso molecolare:402.5
  • LAS195319

    CAS:
    LAS195319 is a potent and selective inhaled PI3Kδ Inhibitor (IC50 = 0.5 nM) for the Treatment of Respiratory Diseases.
    Formula:C29H26N10O3S
    Colore e forma:Solid
    Peso molecolare:594.65
  • LY 292728

    CAS:
    LY 292728 is a highly potent antagonist of leukotriene B4 receptor.
    Formula:C34H29FO9
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:600.59
  • ZK118182 isopropyl ester

    CAS:
    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).
    Formula:C23H37ClO5
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:428.99
  • Burapitant

    CAS:
    <p>Burapitant (SSR 240600) is a novel non-peptide tachykinin neurokinin 1 (NK) receptor antagonist with anti-coke oven and antidepressant activity.</p>
    Formula:C31H35Cl2F6N3O3
    Purezza:>99.99% - >99.99%
    Colore e forma:Solid
    Peso molecolare:682.52
  • (Rac)-Nebivolol

    CAS:
    (Rac)-Nebivolol, a racemic β1-adrenergic blocker (IC50=0.8 nM), has vasodilatory properties and mitigates ethanol-induced cardiac harm.
    Formula:C22H25F2NO4
    Colore e forma:Solid
    Peso molecolare:405.43
  • JKC 302

    CAS:
    JKC 302 is an ET-A receptor antagonist that partially inhibits the contraction of tracheal rings in asthmatic rats induced by ET-1.
    Formula:C30H42N6O6
    Colore e forma:Solid
    Peso molecolare:582.69
  • D4R antagonis-2


    Potent D4R antagonist-2: selective, IC50=6.52 μM, good in vitro PK and brain penetration, potential for Parkinson's research.
    Formula:C21H23ClF2N2O2
    Colore e forma:Solid
    Peso molecolare:408.87
  • Danavorexton

    CAS:
    Danavorexton is an orexin receptor agonist.
    Formula:C21H32N2O5S
    Colore e forma:Solid
    Peso molecolare:424.55
  • Monlunabant

    CAS:
    Monlunabant ((S)-MRI-1891), a solid dispersion compound, functions as an inhibitor of the cannabinoid CB1 receptor [1].
    Formula:C26H22ClF3N6O3S
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:591.00
  • PSB-KK1415

    CAS:
    PSB-KK1415 is a selective agonist for the human orphan G protein-coupled receptor GPR18, with an EC50 of 19.1 nM.
    Formula:C24H23ClN6O2
    Peso molecolare:462.93
  • H1R ligand-1

    CAS:
    <p>H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). It can serve as a scaffold for synthesizing a series of derivatives to investigate H1R binding kinetics.</p>
    Formula:C19H23NO
    Colore e forma:Solid
    Peso molecolare:281.392
  • 5-HT1A antagonist 1


    <p>Compound 6f is a potent, selective 5-HT1A receptor blocker (Ki: 35 nM), useful in CNS disorder research.</p>
    Formula:C23H29ClN6O2
    Colore e forma:Solid
    Peso molecolare:456.97
  • PD 140376

    CAS:
    PD 140376: Selective CCK-B/gastrin receptor antagonist radioligand for guinea pig stomach & brain.
    Formula:C33H40N4O5
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:572.69
  • L-796778 acetate

    CAS:
    L-796778 acetate is a selective sst3 receptor agonist. In CHO-K1 cells expressing hsst3 receptors, it acts as a partial agonist that inhibits Forskolin-induced cAMP production, with an IC50 value of 18 nM. Additionally, L-796778 acetate exhibits anticonvulsant properties.
    Formula:C31H44N6O9
    Colore e forma:Solid
    Peso molecolare:644.716
  • ONO-8809

    CAS:
    ONO-8809: Thromboxane A2 antagonist, reduces airway hyperresponse, macrophage accumulation, and MMP-9 in SHRSP brains.
    Formula:C30H46BrNO4S
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:596.66
  • 9-Methyl-β-carboline

    CAS:
    9-Methyl-β-carboline is a cognitive enhancer with neuroprotective, neurorestorative, and anti-inflammatory properties. Its behavioral effects may be linked to hippocampal dopamine levels and the stimulation of dendritic and synaptic proliferation.
    Formula:C12H10N2
    Colore e forma:Solid
    Peso molecolare:182.221
  • CHF-6366

    CAS:
    <p>CHF-6366: M3 antagonist &amp; β2 agonist (pKi 10.4/11.4), mild Ca channel blocker, used in COPD study.</p>
    Formula:C42H48N6O8
    Colore e forma:Solid
    Peso molecolare:764.87
  • OX2R agonist 1

    CAS:
    OX2R agonist 1 is an OX2R activator with an EC50 of less than 100 nM. It is utilized in research related to narcolepsy and cataplexy.
    Formula:C21H28F2N2O5S
    Peso molecolare:458.52
  • MRS4865

    CAS:
    MRS4865 (compound 7a) serves as a chimeric antagonist for the P2Y14 receptor and an agonist for UDP-glucose, offering protection against neuropathic pain.
    Formula:C39H39F3N4O7
    Colore e forma:Solid
    Peso molecolare:732.74
  • 25C-NBF hydrochloride

    CAS:
    25C-NBF hydrochloride is an agonist of 5-HT receptors, specifically activating 5-HT2A and 5-HT2C receptors, with an EC50 of approximately 0.3 μM.
    Formula:C17H20Cl2FNO2
    Peso molecolare:360.251
  • AChE-IN-5


    AChE-IN-5: oral, crosses blood-brain barrier, targets AChE/5-HT1A/SERT, potent with 2.29 nM IC50.
    Formula:C38H45N5O
    Colore e forma:Solid
    Peso molecolare:587.8
  • SphK2-IN-2


    SphK2-IN-2 (21g) is a potent and selective inhibitor of SphK2 (IC50: 0.23 μM).
    Formula:C21H25ClN10O
    Colore e forma:Solid
    Peso molecolare:468.94
  • Taranabant

    CAS:
    <p>Taranabant: potent CB1 receptor inverse agonist; inhibits agonists with 0.13 nM Ki in vitro.</p>
    Formula:C27H25ClF3N3O2
    Purezza:99.06% - 99.06%
    Colore e forma:Solid
    Peso molecolare:515.96
  • Terguride

    CAS:
    Terguride: treats hyperprolactinemia, blocks 5-HT2A/B, activates dopamine receptors, studied for PAH.
    Formula:C20H28N4O
    Colore e forma:Solid
    Peso molecolare:340.46
  • DA-302168S

    CAS:
    <p>DA-302168S is an orally active, selective GLP-1R agonist with an EC50 value of 1.32 nM. It promotes insulin secretion and has a hypoglycemic effect. Additionally, DA-302168S reduces food intake. It primarily activates GLP-1R in humans and monkeys, with minimal effect on GLP-1R in rats, mice, and dogs. DA-302168S can be used for research in type 2 diabetes and obesity.</p>
    Formula:C33H24ClF2N3O5
    Colore e forma:Solid
    Peso molecolare:616.011
  • Aplaviroc

    CAS:
    Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist. With IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
    Formula:C33H43N3O6
    Purezza:97.98% - 98.26%
    Colore e forma:Solid
    Peso molecolare:577.71
  • LJ-4517


    LJ-4517 is an effective A2AAR antagonist (Ki=18.3 nM). LJ-4517 can effectively replace the binding of [3H] ZM241385 at WT A2AAR.
    Formula:C19H21N5O3S
    Colore e forma:Solid
    Peso molecolare:399.47
  • D1R antagonist 1

    CAS:
    Compound 12a (D1R antagonist 1) is a D1R antagonist that participates in both G-protein-coupled and β-arrestin-mediated signaling pathways [1].
    Formula:C22H26BrNO4
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:448.35
  • MF-592

    CAS:
    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.
    Formula:C34H33Cl2N3O6S
    Colore e forma:Solid
    Peso molecolare:682.61
  • Tiprenolol hydrochloride

    CAS:
    Tiprenolol hydrochloride is a β-adrenoceptor (β-adrenoceptor) antagonist. This compound is effective in eliminating ventricular arrhythmias in dogs caused by intravenous administration of adrenaline, following inhalation of halothane.
    Formula:C13H22ClNO2S
    Colore e forma:Solid
    Peso molecolare:291.84
  • Sulfinalol hydrochloride

    CAS:
    Sulfinalol hydrochloride is an orally active β-adrenoceptor (β-adrenoceptor) antagonist that exhibits direct vasodilatory activity. It is also classified as an antihypertensive agent.
    Formula:C20H28ClNO4S
    Colore e forma:Solid
    Peso molecolare:413.96
  • UNC10099984A

    CAS:
    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.
    Formula:C24H29Cl2N3O2
    Colore e forma:Solid
    Peso molecolare:462.41
  • Thielavin B

    CAS:
    Thielavin B, from Thielavia terricola, inhibits prostaglandin E2 synthesis and reduces rat oedema.
    Formula:C31H34O10
    Colore e forma:Solid
    Peso molecolare:566.6
  • Tofogliflozin

    CAS:
    Tofogliflozin specifically inhibits SGLT2; IC50s are 2.9 nM (human), 14.9 nM (rat), 6.4 nM (mouse).
    Formula:C22H26O6
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:386.44
  • Tipindole

    CAS:
    Tipindole is a serotonin antagonist utilized in research related to depression.
    Formula:C16H20N2O2S
    Colore e forma:Solid
    Peso molecolare:304.41
  • DSP-1053 benzenesulfonate

    CAS:
    DSP-1053: Benzylpiperidine-based, potent SERT inhibitor (Ki=1.02nM), partial 5-HT1A receptor agonist (Ki=5.05nM), antidepressant.
    Formula:C32H38BrNO7S
    Colore e forma:Solid
    Peso molecolare:660.62
  • Nolpitantium besilate

    CAS:
    Nolpitantium besilate is a neurokinin-1 receptor antagonist.
    Formula:C43H50Cl2N2O5S
    Colore e forma:Solid
    Peso molecolare:777.84
  • Udifitimod

    CAS:
    Udifitimod (BMS-986166) is a potent, selective, and orally active modulator of the S1P1R receptor, showing potential for research in autoimmune diseases.
    Formula:C25H33NO2
    Colore e forma:Solid
    Peso molecolare:379.54
  • Remlifanserin

    CAS:
    Remlifanserin is a potent inverse agonist of the serotonin receptor (5-HT2A).
    Formula:C24H29F2N3O2
    Colore e forma:Solid
    Peso molecolare:429.50
  • RXFP1 receptor agonist-9

    CAS:
    RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC50 value of 2.5 μM and a Ymax of 65%. This compound exhibits significant microsomal stability, desirable pharmacokinetic properties, and pharmacodynamic activity. RXFP1 receptor agonist-9 is useful in the study of heart failure.
    Formula:C37H34F5N3O7
    Colore e forma:Solid
    Peso molecolare:727.67
  • LAB687

    CAS:
    LAB687 (Compound 2a) is an inhibitor of microsomal triglyceride transfer protein (MTP) with an IC50 of 0.9 nM for inhibiting the secretion of apolipoprotein B (apoB) in HepG2 cells. Additionally, LAB687 acts as a Smoothened (Smo) antagonist, exhibiting IC50 values of 2.48 μM and 3.42 μM for mouse and human Smo receptors, respectively. This compound is effective in reducing triglyceride and low-density lipoprotein cholesterol (LDL-C) levels and in inhibiting the Hedgehog signaling pathway.
    Formula:C26H23F3N2O3
    Colore e forma:Solid
    Peso molecolare:468.47