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.

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].

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

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.

DL-AP4, also known as 2-Amino-4-phosphonobutyric acid, is a competitive glutamate antagonist with defined binding affinity that is widely used to selectively inhibit glutamatergic neurotransmission, making it an essential experimental compound for probing synaptic signaling mechanisms and functional circuitry in central nervous system and visual system research.

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 is a competitive inhibitor of L-histidine deaminase (Ki = 4.26 mM) and also binds to histidine-tRNA synthetase (Ki = 4.6 μM).

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).