GPCR/G-Protein

<p>Compound 24, a 5-HT2 agonist-1, selectively activates 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively.</p>

IIIM-8 is a melanogenesis inhibitor that suppresses pigment production in both in vitro and in vivo settings, exhibiting no cytotoxic effects on Human Adult

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

BIM 23056 TFA, a potent linear octapeptide antagonist of sst3 and sst5 somatostatin receptors, exhibits inhibition constants (K_i) of 10.8 for sst3 and 5.7 for

ABO acts as an annexin A7 modulator, specifically binding to Thr286 to inhibit its phosphorylation on threonine (not on serine or tyrosine) residues within human umbilical vein endothelial cells (HUVECs). This compound furthers the annexin A7 interaction with the EF-hand protein GCA, leading to reduced GCA phosphorylation, lowered intracellular calcium levels, and enhanced autophagy in COS-7 cells. Moreover, ABO lessens phosphorylation of the microtubule-associated protein 1 light chain (LC3) in HUVECs and impedes the upregulation of phosphatidylcholine-specific phospholipase C (PC-PLC) due to oxidized low-density lipoprotein in vascular endothelial cells (VECs). In animal models, specifically apoE-/- mice on a Western diet, administration of ABO (50 or 100 mg/kg per day) has been shown to decrease PC-PLC expression, promote autophagy, and reduce apoptosis, lipid accumulation, and the extent of atherosclerotic plaques in the aortic endothelium.

<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>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>

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

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

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

dopamine D2 receptor modulator

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

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

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

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

TAK-441: oral Hedgehog signal blocker, potent anticancer, IC50=4.4 nM, reduces Gli1 mRNA & tumor growth.

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

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

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

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

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

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

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

<p>Deriglidole (SL 86-0715), an alpha2 receptor inhibitor, blocks colistin/Idazoxan but not prazosin/α2-adrenergic receptors.</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>Calindol (hydrochloride) is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM.</p>

<p>WAY-607695 is a potential 5-HT1A receptor agonist.</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>GI 181771 is an agonist of the cholecystokinin 1 receptor. GI 181771 can be used in studies about obesity.</p>

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

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

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

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

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

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

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

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

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

<p>Talibegron hydrochloride: β3 adrenoceptor agonist, pD2 3.72, relaxes rat arteries, reduces leptin in mice.</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>SR 142948 is a neurotensin (NT) receptor antagonist.</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

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

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

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

MDMB-FUBICA is a potent agonist of the cannabinoid receptors and exhibits psychoactive properties. It can be utilized in e-cigarettes.