Proteina G/GPCR

<p>RXFP1 receptor agonist-7 (Example 2) serves as an RXFP1 receptor agonist, effectively inhibiting cAMP production in HEK293 cells that stably express the human</p>

<p>Bimatoprost Serinol Amide (Bima SA), a prostaglandin analog, shows research potential for glaucoma [1].</p>

<p>4-Hydroxy Nebivolol, a primary metabolite of Nebivolol, results from the enzymatic hydroxylation of Nebivolol by the cytochrome P450 (CYP) isoform CYP2D6.</p>

<p>15(S)-Fluprostenol, an isomer of the FP receptor agonist fluprostenol, serves as a potential active metabolite of 15(S)-fluprostenol isopropyl ester. It can function as an agonist at FP receptors, though with lower potency compared to its 15(R) epimer, fluprostenol.</p>

<p>17-Phenyl trinor prostaglandin A2 is a synthetic analog of prostaglandin [1].</p>

<p>Compound 39, or Y1R probe-1, is a fluorescent probe for Neuropeptide Y Y1 Receptor used in cancer research.</p>

<p>Prostaglandin E2 Serinol Amide acts as a weak inhibitor against the hydrolysis of [3H]2-oleoylglycerol, but it is non-hydrolyzable and cannot produce PGE2. Consequently, it is unable to inhibit leukotriene B4 biosynthesis, superoxide production, migration, and the release of antimicrobial peptides [1].</p>

<p>RS 100329 hydrochloride is an antagonist of α1A-adrenergic receptor.</p>

<p>NTNCB hydrochloride is an antagonist of neuropeptide Y (NPY) Y5 receptor.</p>

<p>SKF 81297 hydrobromide, a selective agonist of the dopamine D1-like receptor，exhibits central activity and is widely used to study the neuromodulatory effects.</p>

<p>Xanthine amine congener is an Adenosine receptor antagonist.</p>

<p>RXFP1 receptor agonist-5 (Example 98) is an agonist that targets the RXFP1 receptor and demonstrates its bioactivity by inhibiting cAMP production in HEK293</p>

<p>Hemopressin(rat) TFA, a nonapeptide from hemoglobin α1-chain, selectively inhibits CB1 receptors and reduces inflammatory pain.</p>

<p>CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.</p>

<p>Vatinoxan hydrochloride is an antagonist of the peripheral α2 adrenergic receptors.</p>

<p>Abaperidone is an atypical antipsychotic, antagonizes 5-HT2A (IC50=6.2 nM) and D2 receptors (IC50=17 nM), reduces hsp70 mRNA in rat brains.</p>

<p>L-796568: potent β3 agonist (EC50 = 3.6 nM), &gt;600-fold selectivity vs β1/β2, good oral bioavailability, long action.</p>

<p>TRAP-6-IN-1 inhibits collagen/TRAP-6, IC50: 17.12/11.88 μM, blocks platelet aggregation.</p>

<p>Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective dopamine D2 receptor agonist with antihypertensive activity in vivo.</p>

<p>Alclofenac (W-7320) aids chronic rheumatism by affecting acute phase proteins and L-tryptophan binding.</p>

<p>Prostaglandin D2-1-glyceryl ester (PGD2-G; PGD2 2-glyceryl ester) is a chemical compound known for its significance in various biological processes. This compound, commonly referred to by its abbreviations PGD2-G or PGD2 2-glyceryl ester, plays a crucial role in the mediation of physiological functions.</p>

<p>NBI-34041: High-affinity CRF1 antagonist; reduces endocrine responses to CRF challenges.</p>

<p>Ebopiprant (OBE022) is a prostaglandin F2α (PGF2α) receptor antagonist that can be used to study obesity.</p>

<p>UNC9994 hydrochloride is a selective β-arrestin-biased D2R agonist, Ki of 79 nM, that stimulates β-arrestin and modulates cAMP.</p>

<p>8-iso-15(R)-Prostaglandin F2α (8-iso-15(R) PGF2α) is a chemically distinct member within a broad group of prostaglandin-like eicosanoids, produced through the free radical peroxidation of arachidonic acid contained in membrane phospholipids. It represents the C-15 epimer of 8-isoPGF2α, distinguished as the sole isoprostane isomer extensively examined across numerous biological systems.</p>

<p>AL 8810 methyl ester, a prostaglandin F(2α) analog and receptor agonist, competitively antagonizes FP receptor agonist Fluprostenol effects. It lacks significant potency against TP, DP, EP(2), EP(4) receptor subtypes in cell lines [1].</p>

<p>LK 204-545 is a highly selective antagonist of beta1-adrenoceptor.</p>

<p>L-644,698 is a selective agonist of human prostanoid DP receptor.</p>

<p>CR6086: potent EP4 antagonist with DMARD effects, low Ki (16.6 nM), and specific anti-inflammatory action.</p>

<p>Quinotolast sodium inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner in the concentration range of 1-100 μg/mL.</p>

<p>Velusetrag(TD-5108), a potent 5-HT4 agonist, is in development for gastroparesis, constipation, and IBS.</p>

<p>GLP-1R agonist 17 excels in stimulating GLP-1 receptors, useful for cardiovascular metabolic disease research.</p>

<p>Somatostatin sst4 receptor agonist</p>

<p>Heptadecanoyl ethanolamide, an endogenous cannabinoid, serves as a synthetic analog of PEA, featuring an odd-numbered (17-carbon) fatty acid chain [1].</p>

<p>Nemonapride is a dopamine D2-like receptor antagonist.</p>

<p>Bufuralol hydrochloride is a potent, non-selective, orally active β-blocker with partial agonist effects and a CYP2D6 probe.</p>

<p>NMI 8739 (n-docosahexaenoyl dopamine) is an agonist of D2 autoreceptor.</p>

<p>A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.</p>

<p>Adomeglivant (LY2409021) is a potent and selective glucagon receptor antagonist. Which is used in clinical trial for type 2 diabetes mellitus.</p>

<p>α1 adrenoceptor-MO-1 (S enantiomer) has affinity at alpha 1 adrenergic receptor with alphalytic activity and analgesic action.</p>

<p>TAK-441: oral Hedgehog signal blocker, potent anticancer, IC50=4.4 nM, reduces Gli1 mRNA &amp; tumor growth.</p>

<p>(±)-Prenalterol (H 80/62) is an agonist of beta-2- and beta-1-adrenergic receptors and is used to study chronic congestive heart failure.</p>

<p>CGP-20712 is a selective β 1-adrenoceptor antagonist with an IC50 of 0.7 nM.</p>

<p>AS2717638: oral LPA5 antagonist, IC50 38 nM, reduces PGF2α/PGE2/AMPA allodynia.</p>

<p>Calindol (hydrochloride) is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM.</p>

<p>WAY-639889 is a small molecule compound with selective and potent inhibitory effects on neuropeptide Y-5 receptors.</p>

<p>Lotiglipron (PF-07081532) is a GLP-1R agonist that lowers blood glucose and may be used in the study of type 2 diabetes mellitus (T2DM) and excess obesity.</p>

<p>CCR3 antagonist 1 is a potent CCR3 antagonist, used for the research of inflammatory and immunologic diseases.</p>

<p>GI 181771 is an agonist of the cholecystokinin 1 receptor. GI 181771 can be used in studies about obesity.</p>

<p>GW 833972A: selective CB2 agonist; reduces neural depolarization and citric acid cough in animals.</p>

<p>PSB-603 is a selective antagonist of Adenosine A2B receptor(Ki = 0.553 nM) with anti-inflammatory effects.</p>

<p>OPC-28326: an α2-adrenergic blocker; dilates blood vessels; inhibits α2A/B/C receptors with Ki 2040/285/55 nM.</p>

<p>LGD-6972 is an antagonist of glucagon receptor.</p>

<p>Clazosentan (Ro 61-1790) is a selective ET_A receptor antagonist that inhibits ET-1 vasoconstriction and prevents cerebral vasospasm.</p>

<p>INT-777 (S-EMCA) is a potent TGR5 agonist with an EC50 of 0.82 μM.</p>

<p>Didesmethyl cariprazine, Cariprazine's active metabolite, treats schizophrenia/bipolar with D3/D2 affinity; half-life 1-3 weeks.</p>

<p>ST-1006: histamine H4 agonist, pKi 7.94, anti-inflammatory, anti-pruritic, promotes basophil migration.</p>

<p>Vidupiprant (AMG 853) is an effective dual antagonist of CRTH2 and prostanoid D receptor with IC50s of 8 nM and 35 nM in human plasma.</p>

<p>GV150013 is an antagonist of cholecystokinin-2 (CCK2) receptor.</p>

<p>Selvigaltin (GB1211) is a Gal-3 inhibitor with potential anticancer activity. Selvigaltin is used in the study of cirrhosis and cancer.</p>

<p>SB 216641 hydrochloride (SB-216641A) is a 5-HT1B/D receptor antagonist with anxiolytic properties.</p>

<p>Enerisant (TS-091) is a histamine H3 receptor antagonist that promotes pro-cognitive effects and reverses scopolamine-induced cognitive deficits.</p>

<p>WAY-607695 is a potential 5-HT1A receptor agonist.</p>

<p>dopamine D2 receptor modulator</p>

<p>SAG 21k is an orally bioactive and potent Hedgehog signaling activator that crosses the blood-brain barrier for the study of cartilage regeneration.</p>

<p>Osemozotan is a 5-HT1A receptor agonist potentially for the treatment of generalized anxiety disorder.</p>

<p>Azelaprag (Example 263.0) is a candidate active molecule (EC50= 0.32 nM) for an apelin receptor agonist. treat nervous system diseases. High-Quality, Low-Cost!</p>

<p>AY 77: Potent, selective PAR2 agonist, favors Ca2+ (ec50=40nM) &amp; ERK1/2 (ec50=2μM), boosts breast cancer cell migration.</p>

<p>K777: Oral cysteine protease inhibitor, CYP3A4 blocker (IC50=60 nM), CCR4 antagonist, anti-Trypanosoma cruzi, antiviral, halts EBOV/SARS-CoV entry (IC50&lt;1 nM).</p>

<p>Ertugliflozin is a potent oral hSGLT2 inhibitor (IC50: 0.877 nM) for type 2 diabetes treatment studies.</p>

0990CL is an effective heterotrimer Gαi subunit specific inhibitor, which can interact with purified Go± in GDP-bound state, and can block α2AR mediated cAMP

<p>Selatogrel (ACT-246475) is a P2Y12 receptor antagonist with antithrombotic activity and inhibits platelet aggregation.</p>

<p>Deriglidole (SL 86-0715), an alpha2 receptor inhibitor, blocks colistin/Idazoxan but not prazosin/α2-adrenergic receptors.</p>

<p>Compound SC9, an anti-inflammatory agent, serves as a potent and selective inhibitor of the Drp1-Fis1 interaction, mitigating FIS1-mediated mitochondrial</p>

<p>Talibegron hydrochloride: β3 adrenoceptor agonist, pD2 3.72, relaxes rat arteries, reduces leptin in mice.</p>

<p>PSB 1115 is an A2B receptor antagonist and can counteract the inhibitory effect of NECA.</p>

<p>SR 142948 is a neurotensin (NT) receptor antagonist.</p>

<p>Lumateperone (ITI 722) is a 5HT2A receptor antagonist and a dopamine receptor phosphoprotein modulator (DPPM).</p>

<p>SB-616234-A is a selective and orally bioavailable antagonist of 5-HT1B receptor, with anxiolytic and antidepressant activity.</p>

<p>INCB3344 is an effective, specific and orally bioavailable CCR2 antagonist with IC50 values of 9.5 nM (mCCR2) and 5.1 nM (hCCR2) in binding antagonism and 7.8</p>

<p>Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.</p>

<p>Pentacosafluorotridecanoic Acid (PFTrDA) is a perfluoroalkyl substance (PFAS) that exhibits various biological impacts across different species. In zebrafish embryos, exposure to PFTrDA induces yolk sac edema and increases mRNA expression of thyroid hormone synthesis genes, including tshβ, at concentrations of 0.1 and 0.3 mg/L. At a dosage of 10 mg/kg, PFTrDA reduces serum testosterone and luteinizing hormone levels, as well as palmitic acid, linoleic acid, and oleic acid levels in the testicular interstitial cells of late adolescent rats. In humans, maternal plasma levels of PFTrDA during pregnancy are positively correlated with the development of eczema in female infants (but not male infants), and PFTrDA levels are higher in the livers of cancerous humans compared to non-cancerous ones. Additionally, PFTrDA is found in marine mammals.</p>

<p>Cendifensine functions as a monoamine reuptake inhibitor, targeting the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT).</p>

<p>CP 481715 is an effective selective CCR1 antagonist with potential therapeutic significance for inflammatory diseases.</p>

<p>PD 135158 is a CCK2 receptor antagonist.</p>

<p>INCB-9471 HCl: a potent CCR5 antagonist, blocks monocyte migration &amp; HIV-1.</p>

<p>A2A receptor antagonist 2 is a highly selective and potent antagonist of the adenosine A2Areceptor (IC50: 8.3 nM).</p>

<p>Serlopitant is a selective antagonist of Neurokinin-1 (NK-1) receptor.</p>

<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>

<p>LY210073 is an antagonist of the Leukotriene B4 (LTB4) receptor (IC50: 6.2 nM).</p>

<p>SJPYT-310 is a selective PXR antagonist, exhibiting no noticeable cytotoxicity.</p>

<p>Alixorexton is an agonist of the orexin-2 receptor (orexin-2 receptor) and is utilized in obesity research.</p>

<p>MrgprX2 antagonist-7 is an anti-allergic agent with significant anti-allergic effects and inhibits mast cell degranulation.</p>

<p>Teoprolol is a blocker of β-adrenergic receptor.</p>

<p>MRS2905 (α,β-Methylene-2-thio-UDP) trisodium is a selective P2Y14R agonist with an EC50 of 0.92 nM. It shows no activity on UDP-activated P2Y6 receptors or other P2Y receptors.</p>

<p>5-HT2/5-HT7 receptor antagonist</p>

<p>SR 142948-C3-NHMe is the methylated form of SR 142948.</p>

<p>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.</p>

<p>Compound 10o, a histamine H3 antagonist-1, functions as both a histamine H3 antagonist and a serotonin reuptake inhibitor, making it useful for research in depression [1].</p>

<p>L-97-1 is an antagonist of the adenosine A1 receptor.</p>