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"

Purity (%)

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5-HT2A/5-HT2C inverse agonist 1
CAS:
- 2718990-76-0
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.
Formula:C₂₄H₃₅N₅O₂
Color and Shape:Solid
Molecular weight:425.57
Ref: TM-T200089
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Mafoprazine
CAS:
- 80428-29-1
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.
Formula:C₂₂H₂₈FN₃O₃
Color and Shape:Solid
Molecular weight:401.47
Ref: TM-T200689
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MK-3207 Hydrochloride
CAS:
- 957116-20-0
MK-3207 Hydrochloride (MK-3207 HCl) is a potent CGRP receptor antagonist with IC50 and Kiof 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. Phase 2.
Formula:C₃₁H₃₀ClF₂N₅O₃
Purity:98.19%
Color and Shape:Solid
Molecular weight:594.05
Ref: TM-T6590
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16(S)-Iloprost
CAS:
- 74843-14-4
Iloprost, a potent prostacyclin analog, binds to human IP & EP1 receptors with high affinity; inhibits platelet aggregation effectively.
Formula:C₂₂H₃₂O₄
Color and Shape:Solid
Molecular weight:360.49
Ref: TM-T36212
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Ersentilide
CAS:
- 125279-79-0
Ersentilide, a benzamide derivative, functions as both a β1-adrenergic receptor antagonist and an Ikr blocker. It has demonstrated efficacy in animal models of cardiac arrhythmias.
Formula:C₂₁H₂₆N₄O₅S
Color and Shape:Solid
Molecular weight:446.52
Ref: TM-T201538
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MRS2279
CAS:
- 367909-40-8
Selective, high affinity competitive antagonist of the P2Y1 receptor
Formula:C₁₃H₁₈ClN₅O₈P₂
Purity:98%
Color and Shape:Solid
Molecular weight:469.71
Ref: TM-T23021
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SphK2-IN-2
SphK2-IN-2 (21g) is a potent and selective inhibitor of SphK2 (IC50: 0.23 μM).
Formula:C₂₁H₂₅ClN₁₀O
Color and Shape:Solid
Molecular weight:468.94
Ref: TM-T63017
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CCR3 antagonist 2
CAS:
- 606128-24-9
CCR3 antagonist2 (example 66) is a CCR3 antagonist useful for researching inflammatory or allergic diseases, particularly those affecting the respiratory tract, such as inflammatory or obstructive airway conditions.
Formula:C₂₁H₂₈ClN₅O₃
Color and Shape:Solid
Molecular weight:433.93
Ref: TM-T212174
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CGRP antagonist 7
CAS:
- 2173508-07-9
CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki value of 0.029 nM. It effectively inhibits CGRP receptor-mediated cyclic adenosine monophosphate (cAMP) production, with an IC50 value of 1.5 nM. This compound is useful in migraine research.
Formula:C₃₀H₃₂FN₅O₃
Color and Shape:Solid
Molecular weight:529.61
Ref: TM-T211975
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25B-NBOH hydrochloride
CAS:
- 1539266-16-4
25B-NBOH hydrochloride is a phenethylamine that exhibits high affinity for serotonin (5-HT) receptors 5-HT2A and 5-HT2C, with pKi values of 8.3 and 9.4, respectively.
Formula:C₁₇H₂₁BrClNO₃
Color and Shape:Solid
Molecular weight:402.711
Ref: TM-T204858
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MRGPRX2 modulator-3
CAS:
- 2765728-26-3
MRGPRX2 modulator-3 (Compound 4-400) is a quinoline derivative and an MRGPRX2 regulator. It is utilized in the investigation of MRGPRX2-related conditions, including allergies, itching, pain, inflammation, and autoimmune diseases.
Formula:C₂₁H₂₁ClF₃N₅O
Color and Shape:Solid
Molecular weight:451.87
Ref: TM-T211385
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LY 245769
CAS:
- 127345-02-2
LY 245769 is an inhibitor of leukotriene E4 (LTE4).
Formula:C₂₅H₃₃F₃N₈OS
Purity:98%
Color and Shape:Solid
Molecular weight:550.64
Ref: TM-T27904
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PAR4 antagonist 3
CAS:
- 3057206-40-0
PAR4 antagonist3 (Compound 36) is a selective antagonist of protease-activated receptor 4 (PAR4). It exhibits antiplatelet activity with an IC50 of 26.1 nM and enhances metabolic stability in human liver microsomes, with a half-life (T1/2) of 97.6 minutes.
Formula:C₂₂H₁₆FN₃O₅S
Molecular weight:453.44
Ref: TM-T209701
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5-HT6R/MAO-B modulator 1
5-HT6R/MAO-B modulator 1 blocks 5-HT6R and permanently inhibits MAO-B, protects glial cells, and reverses memory loss.
Formula:C₃₃H₃₈N₄O₃S
Color and Shape:Solid
Molecular weight:570.74
Ref: TM-T64036
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UK-432097
CAS:
- 380221-63-6
UK 432097 is an adenosine A2A agonist.
Formula:C₄₀H₄₇N₁₁O₆
Color and Shape:Solid
Molecular weight:777.87
Ref: TM-T29049
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Protease-Activated Receptor-1 antagonist 2
Selective, orally active PAR-1 antagonist with an IC50 of 7 nM, potential for cardiovascular disease studies.
Color and Shape:Solid
Ref: TM-T64285
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YM158 free base
CAS:
- 179102-65-9
YM158 free base is a potent and selective antagonist of TXA2 and LTD4 receptor (pA2s: about 8.81 and 8.87).
Formula:C₃₂H₃₃ClN₆O₅S₂
Purity:98%
Color and Shape:Solid
Molecular weight:681.22
Ref: TM-T10501
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PSB 36
CAS:
- 524944-72-7
A1 adenosine receptor antagonist
Formula:C₂₁H₃₀N₄O₃
Purity:98%
Color and Shape:Solid
Molecular weight:386.49
Ref: TM-T23202
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L-654284
CAS:
- 98719-20-1
L-654284 is an α2-adrenergic receptor antagonist characterized by its notable selectivity. It competes with 3H-clonidine and 3H-rauwolscine for binding in vitro, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 effectively blocks the pre-ejaculatory effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. The compound demonstrates significant selectivity for α2 over α1 adrenergic receptors, with a Ki value of 110 nM against 3H-prazosin binding. In vivo, L-654284 significantly increases the turnover of norepinephrine in the rat cerebral cortex, indicating its activity in blocking α2-adrenergic receptors within the central nervous system.
Formula:C₁₈H₂₄N₂O₄S
Color and Shape:Solid
Molecular weight:364.46
Ref: TM-T201031
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(Rac)-Nebivolol
CAS:
- 99200-09-6
(Rac)-Nebivolol, a racemic β1-adrenergic blocker (IC50=0.8 nM), has vasodilatory properties and mitigates ethanol-induced cardiac harm.
Formula:C₂₂H₂₅F₂NO₄
Color and Shape:Solid
Molecular weight:405.43
Ref: TM-T62004
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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
Color and Shape:Solid
Molecular weight:313.23
Ref: TM-T60790
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Teoprolol
CAS:
- 65184-10-3
Teoprolol is a blocker of β-adrenergic receptor.
Formula:C₂₃H₃₀N₆O₄
Purity:98%
Color and Shape:Solid
Molecular weight:454.52
Ref: TM-T13124
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(R)-MrgprX2 antagonist-3
CAS:
- 2642174-20-5
(R)-MrgprX2 antagonist-3 is an antagonist of MrgprX2. It is applicable in the study of inflammatory skin diseases. For more detailed information, please refer to compound E118 in patent document WO2021092240A1.
Formula:C₁₆H₂₀FN₃O₂S
Molecular weight:337.41
Ref: TM-T208997
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PAR-2-IN-2
CAS:
- 313986-65-1
PAR-2-IN-2 (compound P-596) is an inhibitor of protease-activated receptor 2 (PAR-2), with an IC50 of 10.79 μM for SLIGKV and an IC50 greater than 200 μM for trypsin.
Formula:C₂₅H₂₀F₃N₅O₂
Color and Shape:Solid
Molecular weight:479.454
Ref: TM-T204647
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Osanetant HCl
CAS:
- 173050-51-6
Osanetant HCl is the (R)-enantiomer; neurokinin-3 receptor antagonist
Formula:C₃₅H₄₂Cl₃N₃O₂
Color and Shape:Solid
Molecular weight:643.09
Ref: TM-T70231
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CB1/2 receptor-1
CAS:
- 1260669-31-5
CB1/2 receptor-1 (compound 5.3) serves as an agonist for CB1/2 receptors and is utilized in angiogenesis research.
Formula:C₃₃H₄₈O₂
Color and Shape:Solid
Molecular weight:476.73
Ref: TM-T200966
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LK-732
CAS:
- 673485-33-1
LK-732 is a thrombin inhibitor with antithrombotic activity. It exhibits dose-dependent inhibition in models of hypercoagulability, with an IC50 value of 1.3 mg/kg. LK-732 is used in cardiovascular and cerebrovascular research.
Formula:C₂₅H₂₉N₅O₃S
Color and Shape:Solid
Molecular weight:479.59
Ref: TM-T201818
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Macitentan (n-butyl analogue)
CAS:
- 556797-16-1
Macitentan n-butyl analogue, an oral ETA/ETB receptor blocker, may treat IPF and PAH.
Formula:C₂₀H₂₁Br₂N₅O₄S
Purity:98%
Color and Shape:Solid
Molecular weight:587.29
Ref: TM-T11935
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ZD6021
CAS:
- 255049-08-2
ZD6021 is an antagonist of neurokinin 1 receptor.
Formula:C₃₅H₃₅Cl₂N₃O₂S
Purity:98%
Color and Shape:Solid
Molecular weight:632.64
Ref: TM-T29210
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TGR5 Receptor Agonist 3
CAS:
- 2643391-08-4
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
Ref: TM-T63554
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ATL444
CAS:
- 867054-13-5
ATL444 is an adenosine receptor antagonist with affinity (Ki values) for rA1AR, rA2AAR, rA2BAR, and rA3AR of 7.0, 2.5, 61.8, and >1000 nM, respectively.
Formula:C₁₇H₁₉N₅O
Color and Shape:Solid
Molecular weight:309.37
Ref: TM-T201669
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BRL-37344
CAS:
- 90730-96-4
BRL-37344 is a selective β3-adrenergic receptor agonist. It significantly reduces the body weight of obese mice.
Formula:C₁₉H₂₂ClNO₄
Color and Shape:Solid
Molecular weight:363.84
Ref: TM-T88348
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R-137696
CAS:
- 695185-73-0
R-137696 is an orally active 5-HT1A receptor agonist that facilitates the relaxation of the proximal stomach. It is utilized in research related to functional dyspepsia.
Formula:C₁₇H₂₃N₃O₂
Color and Shape:Solid
Molecular weight:301.38
Ref: TM-T201501
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Flucopride
CAS:
- 1639925-34-0
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.
Formula:C₂₂H₃₃FN₂O₂
Color and Shape:Solid
Molecular weight:376.51
Ref: TM-T201815
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AGH-107
CAS:
- 2172907-10-5
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.
Formula:C₁₃H₁₂IN₃
Color and Shape:Solid
Molecular weight:337.16
Ref: TM-T201735
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Tipindole
CAS:
- 7489-66-9
Tipindole is a serotonin antagonist utilized in research related to depression.
Formula:C₁₆H₂₀N₂O₂S
Color and Shape:Solid
Molecular weight:304.41
Ref: TM-T201819
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Sulfinalol hydrochloride
CAS:
- 63251-39-8
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
Color and Shape:Solid
Molecular weight:413.96
Ref: TM-T201759
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UTPγS trisodium salt
CAS:
- 1266569-94-1
P2Y2 and P2Y4 receptor agonist
Formula:C₉H₁₂N₂Na₃O₁₄P₃S
Purity:98%
Color and Shape:Solid
Molecular weight:566.15
Ref: TM-T23499
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(-)-5-HT2C agonist-3
CAS:
- 2104810-16-2
Compound (−)-19, also known as (-)-5-HT2C agonist-3, is a selective 5-HT2C agonist exhibiting a preference for Gq signaling. It demonstrates efficiency with EC50 values for 5-HT2 receptor subtypes as follows: 5-HT2C at 103 nM, 5-HT2B at 570 nM, and 5-HT2A at 72 nM. This compound is utilized in research on antipsychotics.
Formula:C₁₉H₂₃ClFNO₂
Color and Shape:Solid
Molecular weight:351.84
Ref: TM-T200458
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Quinagolide Free Base
CAS:
- 87056-78-8
Quinagolide Free Base is a non-ergot dopamine D(2)-agonist.
Formula:C₂₀H₃₃N₃O₃S
Color and Shape:Solid
Molecular weight:395.56
Ref: TM-T68483
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L-365260 hemihydrate
L-365260 hemihydrate: selective oral CCK-B/gastrin blocker, Ki=1.9/2.0 nM, competes with guinea pig receptors.
Formula:C₂₄H₂₄N₄O₃
Color and Shape:Solid
Molecular weight:407.47
Ref: TM-T62039
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SGLT inhibitor-1
CAS:
- 2247314-23-2
SGLT inhibitor-1 is a potentsodium glucose co-transporter proteins (SGLTs) dual inhibitor(hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively).
Formula:C₂₄H₂₇FO₈
Purity:98%
Color and Shape:Solid
Molecular weight:462.46
Ref: TM-T12893
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A3AR antagonist 5
CAS:
- 333436-43-4
A3AR antagonist 5 (Compound 16) acts as a selective antagonist for the human adenosine A3 receptor (human adenosine A3 receptor), with an affinity expressed as a pC value of 4.542 μM.
Formula:C₁₈H₁₆N₂O₂S
Color and Shape:Solid
Molecular weight:324.40
Ref: TM-T200493
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AL 8810
CAS:
- 246246-19-5
AL-8810 is an 11β-fluoro analog of PGF 2α with selective antagonist effects at the PGF 2α receptor (FP receptor) [1].
Formula:C₂₄H₃₁FO₄
Color and Shape:Solid
Molecular weight:402.5
Ref: TM-T21752
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SSTR5 antagonist 2 hydrochloride
SSTR5 antagonist 2 hydrochloride: potent, oral SSTR5 blocker with potential in type 2 diabetes research.
Formula:C₃₂H₃₆ClFN₂O₅
Color and Shape:Solid
Molecular weight:583.09
Ref: TM-T64119
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AAZ-A 154 hydrobromide
CAS:
- 2930845-96-6
AAZ-A 154 hydrobromide is a selective, competitive, non-hallucinogenic 5-HT2AR antagonist. It promotes neuronal growth in rodents and yields enduring beneficial behavioral effects.
Formula:C₁₄H₂₁BrN₂O
Color and Shape:Solid
Molecular weight:313.23
Ref: TM-T200446
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Tixanox sodium
CAS:
- 40691-57-4
Tixanox sodium effectively blocks histamine release in the lungs triggered by anti-IgE. It has also been demonstrated that when administered orally, Tixanox sodium can successfully counteract exercise-induced asthma.
Formula:C₁₅H₉NaO₅S
Color and Shape:Solid
Molecular weight:324.28
Ref: TM-T201247
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H3R antagonist 1
CAS:
- 1448422-61-4
H3R-IN-1 is an effective inverse agonist of the histamine receptor 3 (H3R).
Formula:C₁₉H₂₃N₃O₃
Color and Shape:Solid
Molecular weight:341.4
Ref: TM-T200063
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AM9405
AM9405: peripheral CB1/5-HT3 agonist, suppresses gut motility, relieves GI disorder symptoms in mice.
Formula:C₂₄H₃₃BrN₂O₂
Purity:98%
Color and Shape:Solid
Molecular weight:461.44
Ref: TM-T10294
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CB2R/5-HT1AR agonist 1
CAS:
- 2821085-76-9
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].
Formula:C₂₄H₃₃NO₃
Color and Shape:Solid
Molecular weight:383.52
Ref: TM-T86012