gpcrs

Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.

4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).

MS67 is a potent and selective degrader of WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM, exhibiting no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters, and notably demonstrating significant anticancer properties.

N-phenylthiophene-2-carboximidamide is a thiophene derivative that functions as an inhibitor of protein tyrosine kinases (PTKs) and a ligand for G protein-coupled receptors (GPCRs).

PRX-07034 hydrochloride is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 hydrochloride is both a potent (Ki = 4-8 nM) and highly selective 5-HT(6) receptor antagonist (≥100-fold selectivity for the 5-HT(6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D(3) (Ki = 71 nM) and 5-HT(1B) (Ki = 260 nM) receptors.

Alimemazine (Trimeprazine) is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist. Alimemazine also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs.

VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) is a potent and selective antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels, and transporters.

VU0029767 is a selective positive allosteric modulator of M1, a member of the muscarinic acetylcholine family of GPCRs (mAChRs). VU0029767 increases potency and efficacy of acetylcholine (ACh) at M1.

GRC-17536 is an orally available, potent, and selective transient receptor potential anchor protein 1 (TRPA1) inhibitor that has been shown to be highly effective in the treatment of inflammation and neuropathic pain in animal models. The selectivity of G

PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).

ZK 756326 is a selective, non-peptide CCR8 chemokine receptor agonist (IC50: 1.8 μM, in human; 2.6 μM, in mouse). Displays no activity at CCR4/5 and CXCR3/4 and shows higher 28-fold selectivity over 26 other GPCRs (less selective at α2A and 5-HT receptors). Induces chemotaxis and inhibits Env-mediated (HIV) cell-cell fusion.

C16 Lactosylceramide is an endogenous bioactive sphingolipid. It forms membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs), suggesting a role in cell signaling. Plasma levels of C16 lactosylceramide are elevated in insulin-resistant cattle. C16 Lactosylceramide is also upregulated in a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder.

1-Palmitoyl Lysophosphatidic Acid (sodium salt) is an LPA derivative and endogenous metabolite, suitable for related research in the field of life sciences.

Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.

NCT 501 hydrochloride is a potent and selective ALDH1A1 inhibitor (IC50 = 40 nM). Exhibits >1000-fold selectivity for ALDH1A1 over ALDH3A1, ALDH1B1, ALDH2, HPGD and HSD17β4. Also selective over a panel of 168 GPCRs. Blood-brain barrier permeable.

AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavailability. AM-3189 does not penetrate the rat CNS as indicated by a rat brain to plasma ratio of 0.04 at 3 h after an oral dose of 5 mg kg.

Angiotensin II human TFA is a potent vasoconstrictor in the renin-angiotensin system that regulates blood pressure through interactions with AT1R and AT2R receptors. It activates sympathetic nerve activity, promotes aldosterone synthesis and renal function, induces proliferation of vascular smooth muscle cells, and enhances type I and III collagen production in fibroblasts, leading to vascular and myocardial thickening and fibrosis. It also triggers apoptosis and promotes capillary formation, making it suitable for establishing models of cardiac hypertrophy, hypertension, and abdominal aortic aneurysm.

Argipressin (diacetate) (AVP (diacetate), also known as antidiuretic hormone (ADH)), is a nine-amino acid neuropeptide produced by the posterior pituitary gland. It plays a crucial role in maintaining fluid balance, osmolality, and cardiovascular function through interaction with three distinct G-protein coupled receptors (GPCRs): Avpr1a (V1a), Avpr1b (V1b), and Avpr2 (V2). Argipressin (diacetate) also influences centrally regulated metabolic processes, highlighting its significance in physiological regulation [1].

Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential cell membrane biosynthetic metabolite that mediates signal transduction by interacting with G protein-coupled receptors (GPCRs) (ie, LPA receptors). It is the receptor of LPA1 and LPA2. endogenous agonist.

MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. It effectively crosses the blood-brain barrier (BBB) in mice.

Neurokinin B TFA, a member of the tachykinin family, binds to a series of GPCRs, including neurokinin receptors 1 (NK1R), NK2R, and NK3R, to modulate their biological effects.

Selective, high affinity, non-competitive α1A adrenoceptor antagonist (Ki = 0.35 nM). Exhibits no significant activity against a range of other GPCRs, including α2A, β1 and β2 adrenoceptors. Antagonizes effects of phenylephrine on isolated rabbit prostate

Neuropeptide W-30 (human) serves as a crucial stress mediator within the central nervous system, influencing the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. It acts as an endogenous ligand for the two related orphan G-protein-coupled receptors (GPCRs), GPR7 and GPR8, binding and activating them at comparable effective doses [1] [2] [3].

Neuropeptide W-30 (rat) acts as a crucial stress mediator within the central nervous system, influencing the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. It serves as an endogenous ligand for the two related orphan G-protein-coupled receptors (GPCRs), GPR7 and GPR8. NPW-30 binds and activates both GPR7 and GPR8 at comparable effective doses [1] [2] [3].