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GPCR/G-Protein

GPCR/G-Protein

GPCR/G-Protein inhibitors are compounds that target G-protein coupled receptors (GPCRs) and associated G-proteins, which play critical roles in transmitting signals from the outside to the inside of cells. These inhibitors are essential for studying the signaling pathways mediated by GPCRs, which are involved in numerous physiological processes, including sensory perception, immune response, and neurotransmission. GPCR inhibitors are also important in drug development, as many therapeutic agents target these receptors. At CymitQuimica, we offer a wide range of high-quality GPCR/G-Protein inhibitors to support your research in pharmacology, cell biology, and related fields.

Subcategories of "GPCR/G-Protein"

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Found 5745 products of "GPCR/G-Protein"

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  • Nedocromil sodium

    CAS:
    Nedocromil sodium is a pharmacologic stabilizer of mast cells, has been shown to normalize cytokine levels and attenuate cardiac remodeling.
    Formula:C19H17NNaO7
    Purity:98%
    Color and Shape:Solid
    Molecular weight:394.335
  • DMPX

    CAS:
    DMPX (3,7-Dimethyl-1-propargylxanthine) is a caffeine-like compound capable of crossing the blood-brain barrier. It serves as an A2-selective adenosine receptor (AR) antagonist, effectively and selectively blocking the hypothermia and behavioral inhibition induced by A2 adenosine receptor agonists, such as NECA. DMPX is utilized in research on diseases like Parkinson's disease.
    Formula:C10H10N4O2
    Color and Shape:Solid
    Molecular weight:218.212
  • Sigma-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>
    Formula:C32H34N6
    Color and Shape:Solid
    Molecular weight:502.65
  • BI 703704

    CAS:
    <p>BI 703704, a soluble guanylate cyclase (sGC) activator, inhibits the progression of diabetic nephropathy in the ZSF1 rat [1].</p>
    Formula:C32H37N3O4S
    Purity:98%
    Color and Shape:Solid
    Molecular weight:559.72
  • GHSR-1a agonist-1

    CAS:
    <p>GHSR-1a agonist-1 (Compound 4b) is an orally active agonist of the human growth hormone secretagogue receptor 1a (GHSR-1a) with an EC50 of 0.49 nM. It effectively stimulates the release of endogenous growth hormone by activating GHSR-1a. Doses as low as 0.1 mg/kg (administered orally) can increase body weight and length in 4-week-old rats. GHSR-1a agonist-1 is applicable in research on pediatric growth and developmental delays.</p>
    Formula:C30H37N5O4
    Color and Shape:Solid
    Molecular weight:531.646
  • ASN-1377642

    CAS:
    <p>ASN-1377642 is an NK1 receptor antagonist with a Ki value of 251 nM. It demonstrates antitumor activity in breast cancer cells with high expression of NK1R-Tr.</p>
    Formula:C21H16ClN5OS
    Color and Shape:Solid
    Molecular weight:421.90
  • Befiradol hydrochloride

    CAS:
    <p>Befiradol HCl (NLX-112) is a selective 5-HT1A receptor agonist with anxiolytic effects and prevents ATXN3 aggregation.</p>
    Formula:C20H23Cl2F2N3O
    Purity:99.1%
    Color and Shape:Solid
    Molecular weight:430.32
  • Iralukast (CGP 45715A)

    CAS:
    Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.
    Formula:C38H37F3O8S
    Color and Shape:Solid
    Molecular weight:710.76
  • A2A receptor antagonist 2


    <p>A2A receptor antagonist 2 is a highly selective and potent antagonist of the adenosine A2Areceptor (IC50: 8.3 nM).</p>
    Formula:C25H28FN7O3
    Color and Shape:Solid
    Molecular weight:493.53
  • CCR1 antagonist 11 hydrochloride


    Oral CCR1 antagonist A1B1 targets h/m/rCCR1 (IC50: 0.03/0.58/0.32 μM), potential for treating inflammatory diseases.
    Color and Shape:Solid
  • Neladenoson

    CAS:
    Neladenoson is an effective and selective agonist of the Adenosine A1 Receptor (A1R). EGFR-IN-162 shows potential for research in heart failure.
    Formula:C29H24ClN5O2S2
    Color and Shape:Solid
    Molecular weight:574.12
  • Terguride

    CAS:
    Terguride: treats hyperprolactinemia, blocks 5-HT2A/B, activates dopamine receptors, studied for PAH.
    Formula:C20H28N4O
    Color and Shape:Solid
    Molecular weight:340.46
  • 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
    Color and Shape:Solid
    Molecular weight:321.41
  • 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>
    Formula:C19H28N2O
    Color and Shape:Solid
    Molecular weight:300.44
  • YM-31636 free base

    CAS:
    <p>YM-31636 (free base) is an orally active, potent, and selective agonist of the 5-HT3 receptor with a pKi value of 9.67. This compound induces contraction in isolated guinea pig distal colon and provokes tachycardia in isolated guinea pig right atrium, demonstrating a relative intrinsic activity of about 0.23. YM-31636 (free base) holds potential for research in constipation management.</p>
    Formula:C14H11N3S
    Color and Shape:Solid
    Molecular weight:253.32
  • SCH-900822

    CAS:
    SCH-900822 is a potent and selective glucagon receptor antagonist.
    Formula:C34H43Cl2N7O2
    Color and Shape:Solid
    Molecular weight:652.66
  • ADORA2A/PDE4D-IN-1

    CAS:
    <p>ADORA2A/PDE4D-IN-1 (Compound 9) is a dual inhibitor of the adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). This compound is applicable for research in bronchial asthma.</p>
    Formula:C14H11N5
    Color and Shape:Solid
    Molecular weight:249.271
  • 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
    Color and Shape:Solid
    Molecular weight:291.84
  • Rivenprost

    CAS:
    Rivenprost, selective EP4 agonist (Ki: 0.7 nM), promotes bone growth, osteoblast differentiation, and aids wound healing.
    Formula:C24H34O6S
    Color and Shape:Solid
    Molecular weight:450.59
  • 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>
    Formula:C34H33Cl2N3O6S
    Color and Shape:Solid
    Molecular weight:682.61
  • TGR5 Receptor Agonist 3

    CAS:
    TGR5 Receptor Agonist 3 is a GPBAR1 agonist with EC50 of 16.4 nM (hTGR5) & 209 nM (mTGR5), ensures gallbladder safety and reduces filling.
    Formula:C29H27N3O6
    Color and Shape:Solid
    Molecular weight:513.54
  • Butopamine hydrochloride

    CAS:
    Butopamine hydrochloride is an orally active inotropic compound that is more effective at increasing heart rate compared to Dobutamine.
    Formula:C18H24ClNO3
    Color and Shape:Solid
    Molecular weight:337.84
  • BRL-37344

    CAS:
    <p>BRL-37344 is a selective β3-adrenergic receptor agonist. It significantly reduces the body weight of obese mice.</p>
    Formula:C19H22ClNO4
    Color and Shape:Solid
    Molecular weight:363.84
  • (±)-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>
    Formula:C18H29NO2
    Color and Shape:Solid
    Molecular weight:291.43
  • BI-685509

    CAS:
    BI-685509: potent, oral sGC activator, boosts cGMP, enhances NO pathways, for CKD/DKD research.
    Formula:C34H38N4O5
    Color and Shape:Solid
    Molecular weight:582.69
  • S1PR1 agonist 2

    CAS:
    S1PR1 agonist 2 is potent for autoimmune research (from WO2021175225A1).
    Formula:C25H25N5O4
    Color and Shape:Solid
    Molecular weight:459.50
  • RBM10-8

    CAS:
    RBM10-8 irreversibly inhibits human sphingosine-1- phosphate lyase (hS1PL) while behaving also as an enzyme substrate.
    Formula:C17H36NO5P
    Color and Shape:Solid
    Molecular weight:365.45
  • K-8794

    CAS:
    <p>K-8794 is an orally active and selective endothelin receptor ETB antagonist that can be utilized in cardiovascular disease research.</p>
    Formula:C36H38N6O6S
    Color and Shape:Solid
    Molecular weight:682.789
  • LY 215840

    CAS:
    5-HT2/5-HT7 receptor antagonist
    Formula:C24H33N3O2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:395.54
  • SGLT1/2-IN-8

    CAS:
    <p>SGLT1/2-IN-8 (compound 8) is a potent and orally active dual inhibitor of SGLT1/2, exhibiting IC50 values of 4 nM and 1 nM, respectively. It shows antihyperglycemic properties, making it suitable for related research.</p>
    Formula:C22H26O6
    Color and Shape:Solid
    Molecular weight:386.438
  • Toladryl

    CAS:
    <p>Toladryl is a derivative of Diphenhydramine that can cross the blood-brain barrier and exhibits oral activity, with antihistamine and anticholinergic properties. Its anticholinergic effects are approximately a tenth of those seen with Diphenhydramine, yet it offers 2-4 times the protection against lethal doses of histamine in guinea pigs. The side effects of Toladryl are fewer and milder compared to Diphenhydramine; however, at higher doses, it may cause symptoms such as insomnia, agitation, and disorientation related to the central nervous system. Toladryl is utilized in the research of allergic diseases.</p>
    Formula:C18H23NO
    Color and Shape:Solid
    Molecular weight:269.38
  • LAS195319

    CAS:
    LAS195319 is a potent and selective inhaled PI3Kδ Inhibitor (IC50 = 0.5 nM) for the Treatment of Respiratory Diseases.
    Formula:C29H26N10O3S
    Color and Shape:Solid
    Molecular weight:594.65
  • Beloxepin

    CAS:
    Beloxepin is an oral dual selective inhibitor of serotonin and norepinephrine uptake.
    Formula:C19H21NO2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:295.38
  • Tofogliflozin

    CAS:
    Tofogliflozin specifically inhibits SGLT2; IC50s are 2.9 nM (human), 14.9 nM (rat), 6.4 nM (mouse).
    Formula:C22H26O6
    Purity:98%
    Color and Shape:Solid
    Molecular weight:386.44
  • 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
    Color and Shape:Solid
    Molecular weight:732.74
  • GPR183 inverse agonist-1

    CAS:
    GPR183 inverse agonist-1 (Compound 78) is an inverse agonist of GPR183. It inhibits GPR183-mediated Gi activation and β-arrestin2 recruitment while blocking PBMC migration. This compound is utilized in research concerning inflammation, autoimmune, and cancer-related diseases.
    Formula:C20H20BrN5O2
    Color and Shape:Solid
    Molecular weight:442.31
  • PF-4693627

    CAS:
    PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM).
    Formula:C26H29Cl2N3O3
    Purity:98%
    Color and Shape:Solid
    Molecular weight:502.43
  • SB 224289

    CAS:
    SB 224289: selective 5-HT1B antagonist, pKi 8.2, 60x selectivity, effective orally.
    Formula:C32H32N4O3
    Purity:98%
    Color and Shape:Solid
    Molecular weight:520.62
  • LY210073

    CAS:
    <p>LY210073 is an antagonist of the Leukotriene B4 (LTB4) receptor (IC50: 6.2 nM).</p>
    Formula:C30H28O8
    Purity:98%
    Color and Shape:Solid
    Molecular weight:516.54
  • Lp(a)-IN-8

    CAS:
    LPA2 antagonist 3 (compound 15) serves as an Lp(a) antagonist. Lp(a) is a pathogenic risk factor for atherosclerotic cardiovascular disease (ASCVD).
    Formula:C21H40Cl2N4O5
    Color and Shape:Solid
    Molecular weight:499.472
  • SB-423557

    CAS:
    SB-423557 is an orally active antagonist of calcium-sensing receptor (CaR) with IC50 of 520 nM
    Formula:C28H36N2O4
    Purity:98%
    Color and Shape:Solid
    Molecular weight:464.60
  • N-methyl Leukotriene C4

    CAS:
    N-methyl LTC4 is a stable synthetic analog of LTC4 and a selective CysLT2 agonist, useful in studying leukotriene pharmacology.
    Formula:C31H49N3O9S
    Color and Shape:Solid
    Molecular weight:639.8
  • NCATS-SM4420

    CAS:
    <p>NCATS-SM4420 (Compound A35) is an orally effective ligand for the thyroid-stimulating hormone receptor (TSHR) that inhibits the proliferation of MDA-T32 and MDA-T85 cells both in vitro and in vivo, with IC50 values of 0.71 μM and 0.38 μM, respectively. Additionally, it suppresses the metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds potential for research in the field of thyroid cancer.</p>
    Formula:C31H27N3O5
    Color and Shape:Solid
    Molecular weight:521.56
  • Pareptide monohydrochloride

    CAS:
    Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).
    Formula:C14H27ClN4O3
    Purity:98%
    Color and Shape:Solid
    Molecular weight:334.84
  • Merigolix

    CAS:
    Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist .
    Formula:C36H35F7N4O6
    Color and Shape:Solid
    Molecular weight:752.68
  • Zaladenant

    CAS:
    <p>Zaladenant is an adenosine receptor antagonist with antitumor properties.</p>
    Formula:C19H15F3N6O
    Color and Shape:Solid
    Molecular weight:400.357
  • RU 52583

    CAS:
    RU 52583 is an alpha 2-adrenergic receptor antagonist.
    Formula:C18H20N2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:264.36
  • Enprostil

    CAS:
    Enprostil: synthetic PGE2 analog, reduces gastric acid, protects mucosa, lowers post-meal gastrin, treats ulcers effectively and safely.
    Formula:C23H28O6
    Purity:98%
    Color and Shape:Solid
    Molecular weight:400.46
  • Org-6906

    CAS:
    DCB-3503, a tylophorine analog, may treat cancer and suppress immunity by blocking protein synthesis and modulating HSC70's ATPase activity.
    Formula:C13H16ClN
    Purity:98%
    Color and Shape:Solid
    Molecular weight:221.73
  • LTD4 antagonist 1

    CAS:
    LTD4 antagonist 1 is a potent and orally active antagonist of leukotriene D4 (LTD4; Ki: 0.57 nM).
    Formula:C31H32F3N3O5S
    Purity:98%
    Color and Shape:Solid
    Molecular weight:615.66