Proteina G/GPCR

KF26777 is a potent and selective antagonist of adenosine A3 receptor.

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.

UMB24 is an effective antagonist of the σ2 receptor, exhibiting dissociation constants (Ki values) of 170 nM for the σ2 receptor and 322 nM for the σ1 receptor. This compound mitigates cocaine-induced convulsions and hyperactivity without causing mortality.

AH22921 is an EP4 prostaglandin receptor antagonist with the ability to antagonize the activation of adenylyl cyclase by prostaglandins in CHO cells. It induces a rightward shift in the PGE? concentration-response curve in these cells, functioning as a non-competitive antagonist. AH22921 is selective for the EP4 receptor, inhibiting its activity in CHO cells without affecting the PGE? concentration-response curve in NPE cells that contain the EP2 receptor.

SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8 for

P2Y2 and P2Y4 receptor agonist

Teoprolol is a blocker of β-adrenergic receptor.

AA 497, a beta-2 agonist, causes relaxation and suppresses Ca spike frequency.

EP3 and EP1 receptor agonist

MSX-3 is an antagonist of the A2A adenosine receptor and a prodrug of MSX-2.

inhibitor of human CCR5 binding to HIV-1 gp120

Disulergine is a dopamine receptor agonist. It also prolactin release-inhibiting 8 alpha-amino-ergoline.

CP-865569 is a CCR1 antagonist useful in the research of inflammatory and autoimmune diseases, including conditions such as rheumatoid arthritis and multiple sclerosis.

Enprostil: synthetic PGE2 analog, reduces gastric acid, protects mucosa, lowers post-meal gastrin, treats ulcers effectively and safely.

(E/Z)-Ozagrel (sodium) [(E/Z)-OKY-046 (sodium)] is a mixture of the EZ isomers of Ozagrel (sodium). It acts as a thromboxane A2 (TXA2) synthase inhibitor. As an antiplatelet agent, Ozagrel (sodium) selectively inhibits human platelet aggregation, with an IC50 of 53.12 μM.

RS 61756-007 is a selective thromboxane receptor (TP) agonist.

RU 52583 is an alpha 2-adrenergic receptor antagonist.

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg

GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. It exhibits an IC50 of 10.1 μM against the hERG potassium ion channel. This compound is applicable for research in the diabetes field.

(+)-15-epi Cloprostenol is a synthetic analogue of prostaglandin F2α (PGF2α) and functions as a potent FP receptor agonist. The compound (+)-15-epi Cloprostenol is the 15(S) or 15β-hydroxy enantiomer of (+)-(+)-15-epi Cloprostenol. Compared to the 15(R)-(+)-15-epi Cloprostenol, this epimer exhibits significantly lower activity as an FP receptor ligand. However, the specific activity of this isomer remains inadequately studied.