k+-competitive binding

Abeprazan hydrochloride (Fexuprazan hydrochloride) is an effective reversible potassium-competitive acid blocker with oral activity, inhibiting H+, K+ -atPase by competitive binding to potassium ions without acid activation. Abeprazan hydrochloride is a proton pump inhibitor (PPI) that acts by reducing gastric acid production and is used to treat gastric acid-related disorders, such as gastroesophageal reflux disease (GERD) and peptic ulcers.

Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase through K+-competitive binding, with an IC50 of 1.0 μM.

Abeprazan (DWP14012) is a potassium-competitive acid blocker developed as a potential alternative to proton pump inhibitors for treating acid-related diseases. It inhibits H+, K+-ATPase through reversible potassium-competitive ionic binding, without requiring acid activation [1].

K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ that binds to the farnesyl binding pocket of PDEδ (Kd of 8 nM).

AR-H067637 is a rapid-binding, reversible and potent (inhibition constant K(i) = 2-4 nM), competitive inhibitor of thrombin, as well as of thrombin bound to fibrin (clot-bound thrombin) or to thrombomodulin. The total amount of free thrombin generated in

CS-526 is a proton pump inhibitor. The inhibitory mechanism of CS-526 on H+,K+-ATPase was a competitive antagonism to the K+ binding site of H+,K+-ATPase, and it was also a reversible inhibition. CS-526 has a potent antisecretory effect on gastric acid se

14S(15R)-EET is an oxylipin and a cytochrome P450 metabolite of arachidonic acid .114S(15R)-EET binds to isolated guinea pig monocytes with a Kivalue of 612.5 nM in a competitive binding assay using [3H]14(15)-EET.2It induces dilation of precontracted isolated canine epicardial arterioles (EC50= 4 pM) and denuded porcine subepicardial arterioles (EC50= 3 pM).3Unlike 14R(15S)-EET, 14S(15R)-EET does not inhibit COX in enzyme assays or isolated platelets.4 1.Daikh, B.E., Lasker, J.M., Raucy, J.L., et al.Regio- and stereoselective epoxidation of arachidonic acid by human cytochromes P450 2C8 and 2C91J. Pharmacol. Exp. Ther.271(3)1427-1433(1994) 2.Wong, P.Y.-K., Lai, P.-S., and Falck, J.R.Mechanism and signal transduction of 14 (R), 15 (S)-epoxyeicosatrienoic acid (14,15-EET) binding in guinea pig monocytesProstaglandins Other Lipid Mediat.62(4)321-333(2000) 3.Zhang, Y., Oltman, C.L., Lu, T., et al.EET homologs potently dilate coronary microvessels and activate BKCa channelsAm. J. Physiol. Heart Circ. Physiol.280(6)H2430-H2440(2001) 4.Fitzpatrick, F.A., Ennis, M.D., Baze, M.E., et al.Inhibition of cyclooxygenase activity and platelet aggregation by epoxyeicosatrienoic acidsJ. Biol. Chem.261(2)15334-15338(1986)

L-Phenylalanine-15N ((S)-2-Amino-3-phenylpropionic acid-15N) is the 15N-labeled L-Phenylalanine. L-Phenylalanine is an essential amino acid isolated from Escherichia coli . L-Phenylalanine is a α2δ subunit of voltage-dependent Ca + channels antagonist with a K i of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) ( K B of 573 μM ) and non-NMDARs , respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

NBI-42902 is a potent inhibitor of peptide radioligand binding to the human GnRH receptor (K(i) = 0.56 nm). Tritiated NBI-42902 binds with high affinity (K(d) = 0.19 nm) to a single class of binding sites and can be displaced by a range of peptide and nonpeptide GnRH receptor ligands. In vitro experiments demonstrate that NBI-42902 is a potent functional, competitive antagonist of GnRH stimulated IP accumulation, Ca(2+) flux, and ERK1 2 activation. It did not stimulate histamine release from rat peritoneal mast cells. Finally, it is effective in lowering serum LH in castrated male macaques after oral administration. Overall, these data provide a benchmark of pharmacological characteristics required for a nonpeptide GnRH antagonist to effectively suppress gonadotropins in humans and suggest that NBI-42902 may have clinical utility as an oral agent for suppression of the hypothalamic-pituitary-gonadal axis. (source: Endocrinology. 2007 Feb;148(2):857-67. Epub 2006 Nov 9.)

Bosentan-d4, the deuterium-labeled variant of Bosentan, serves as a competitive dual antagonist against endothelin-1 (ET) by targeting both ET A and ET B receptors. It exhibits binding affinities with K i values of 4.7 nM for ET A and 95 nM for ET B in human SMC.

Nonapeptide-1 (Melanostatine-5) acetate salt is a peptide hormone that functions as a selective and competitive antagonist of the melanocortin 1 receptor (MC1R) with a binding affinity (K i) of 40 nM. It effectively inhibits α-MSH-induced increases in intracellular cyclic AMP (cAMP) and melanosome dispersion in melanocytes, with inhibitory concentrations (IC 50) of 2.5 nM and 11 nM, respectively. By inhibiting melanin synthesis, Nonapeptide-1 acetate salt is used in research related to skin pigmentation, adrenal gland steroid production regulation, and skin cancer [1] [2] [3].

Saralasin TFA ([Sar1,Ala8] Angiotensin II) is a synthetic octapeptide analog of angiotensin II, functioning as a competitive antagonist at angiotensin II receptors with a K i value of 0.32 nM for 74% of its binding sites, while also exhibiting partial agonist activity. It is utilized in the study of renovascular and renin-dependent (angiotensinogenic) hypertension [1] [3] [6].

α-Helical CRF(9-41) TFA acts as a competitive antagonist for the CRF2 receptor, with a binding constant (K B) of approximately 100 nM, and serves as a partial agonist for the CRF1 receptor, exhibiting a half-maximal effective concentration (EC 50) of 140 nM [1] [2].

'(D-Arg8)-Inotocin is a potent, selective, and competitive antagonist of the vasopressin receptor (V 1a R), exhibiting a binding affinity (K i) of 1.3 nM. It demonstrates over 3000-fold selectivity for the human V1aR compared to the OTR, V1bR, and V2R subtypes [1].'

N-Formyl-L-histidine demonstrates a binding affinity for histidyl-tRNA synthetase, featuring a K i value of 4.6 μM. Additionally, it acts as a competitive inhibitor against L-histidine ammonia-lyase, suppressing urocanic acid formation from L-histidine with a K i value of 4.26 mM [1] [2].