k+-competitive binding

Linaprazan (AZD0865) 通过K+竞争抑制胃中的H+,K+ -ATPase. (IC 50: 1.0 ± 0.2 μM)。Linaprazan 对酸有很强的抑制作用。

Abeprazan hydrochloride (Fexuprazan hydrochloride) 是一种有效的、可逆的、具有口服活性的potassium-competitive acid 阻滞剂，通过竞争性的与钾离子结合抑制 H+，K+- ATPase，而无需酸激活。Abeprazan hydrochloride 是一种质子泵抑制剂(PPI)，通过减少胃酸的产生而起作用，可用于治疗胃酸相关疾病，如胃食管反流病(GERD)和消化性溃疡。

Abeprazan (DWP14012) is a potassium-competitive acid blocker and it is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases[1]. Abeprazan inhibits H+, K+- ATPase by reversible potassium-competitive ionic

K-Ras-PDEδ-IN-1 是新型的 K-Ras-PDEδ 抑制剂，它能够以低纳摩尔Kd8 nM 与 PDEδ 的法尼基结合袋竞争性结合。

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) 是 15N 标记的 L-Phenylalanine。L-Phenylalanine 是从大肠杆菌中分离出来的一种必需氨基酸。 L-Phenylalanine 广泛用于食品香精和药物的生产。

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 是 Bosentan 的氘代物。Bosentan 是一种有效的endothelin-1 (ET)拮抗剂，在人的 SMC 细胞中，作用于ETA 和ETB 受体，Ki 值分别为 4.7 nM 和 95 nM。

Nonapeptide-1 (Melanostatine-5) acetate salt，一种多肽类激素，是 MC1R 选择性拮抗剂 (Ki: 40 nM)。 Nonapeptide-1 acetate salt 是一种竞争性的α-MSH 拮抗剂，可有效抑制黑素细胞中 α-MSH 诱导的细胞内 cAMP 和黑素体扩散 (IC50分别为 2.5 nM 和 11 nM)。 Nonapeptide-1 acetate salt 抑制黑色素合成，可用于研究皮肤色素沉着和肾上腺类固醇生成的调节、皮肤癌。

Saralasin ([Sar1,Ala8] Angiotensin II) TFA，血管紧张素 II (angiotensin II) 的八肽衍生物，作为竞争性血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂，其Ki值达0.32 nM（涵盖74%的结合位点），显示出部分激动剂特性。适应于肾血管性高血压、肾素依赖性（血管紧张素原性）高血压的研究。

α-Helical CRF(9-41) TFA 是一种竞争性 CRF2受体拮抗剂，KB 约为 100 nM。α-Helical CRF(9-41) TFA 也是一种 CRF1受体的部分激动剂，EC50为 140 nM。

(D-Arg8)-Inotocin 是一种对加压素受体V1aR表现出高效、选择性和竞争性拮抗作用的化合物，其Ki值为1.3 nM。该化合物对人类V1aR具有显著的选择性，相较于其他三种亚型(OTR, V1bR, V2R)，其选择性超过3000倍。

N-Formyl-L-histidine 通过与组氨酸-tRNA合成酶结合展示其活性，其Ki值为4.6 μM。此外，N-Formyl-L-histidine作为L-组氨酸解氨酶的竞争性抑制剂，具有4.26 mM的Ki值，能够有效抑制该酶对L-组氨酸的解氨反应，阻止尿苷酸的生成。