secretory

PD 128042 (CI 976) 是口服有效的ACAT (酰基辅酶 A: 胆固醇酰基转移酶)选择性抑制剂。它也是LPAT(溶血磷脂酰基转移酶) 抑制剂。它抑制高尔基体相关 LPAT 活性 (IC50=15 μM)。它抑制多种膜运输步骤，包括在内吞和分泌途径中发现的步骤。

Betazole dihydrochloride (Betazole hydrochloride) 是吡唑类组胺，是一种口服活性 H2受体激动剂，能诱导胃酸分泌，导致胆总管压力立即显著升高。它作为一种诊断剂，用于研究胃酸分泌能力。

Tris(2,4-di-tert-butylphenyl)phosphate (TDTBPP) 分离自 Vitex negundoL，可以抑制分泌性磷脂酶 A2 (sPLA2)。Tris(2,4-di-tert-butylphenyl)phosphate 具有抗炎活性。

Varespladib (LY315920) 是选择性group IIA, secretory phospholipase A2(sPLA2)抑制剂，其IC50=9 nM。它对大鼠，兔，豚鼠和人等各种物种血清的sPLA2活性具有明显的抑制作用，IC50分别为 8.1 nM，5.0 nM，3.2 nM 和 6.2 nM。

Pantoprazole sodium (Pantecta) 是一种具有口服活性的质子泵抑制剂，是一种取代的苯并咪唑，是H+ K+-ATPase 抑制剂，IC50为 6.8 μM。它可以改善 pH 值稳定性，具有抗分泌和抗溃疡的作用。它联合阿霉素可显著增加肿瘤生长延迟。

Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) 是一种具有口服活性的质子泵抑制剂。它是取代的苯并咪唑，是H+ K+-ATPase 抑制剂。它可改善 pH 值稳定性，具有抗分泌和抗溃疡的作用。它联合阿霉素可显著增加肿瘤生长延迟。

Pantoprazole (BY1023) 是一种质子泵抑制剂，用于短期治疗由胃食管反流病引起的食管糜烂和溃疡。它联合阿霉素可显著增加肿瘤生长延迟。它是一种取代的苯并咪唑，是H+ K+-ATPase 抑制剂，可改善 pH 值稳定性，具有抗分泌和抗溃疡的作用。

Pasireotide (SOM230) acetate是长效的环己肽生长激素抑制素类似物，具有抗分泌、抗增殖和促凋亡活性。Pasireotide (SOM230) acetate可抑制 GH、IGF-I 和 ACTH 的分泌，可用于研究肢端肥大症和库欣病。Pasireotide (SOM230) acetate还可以提高生长抑素受体的激动剂活性，对sst1、2、3、4、5的pKi 分别为 8.2、9.0、9.1、小于7.0 和 9.9。

Varespladib methyl (LY333013) 是 Varespladib 的生物可利用前药，是一种特异性 II 组分泌型磷脂酶 A2 抑制剂。

BTM-1086 is a potent gastric secretory inhibitor and an anti-ulcer agent.

Diphenmanil methylsulfate (Diphemanil mesylate) 是一种抗胆碱能季铵盐，可与毒蕈碱乙酰胆碱受体结合，从而减少胃酸、汗液和唾液的分泌。

SCH28080 是一种可逆且具有 K+ 竞争性的胃 H+ K+-ATP 酶 (H+ K+-ATPase) 抑制剂，IC50 值为 20 nM (家兔微粒体膜)。SCH28080 在体内是有效的酸分泌抑制剂，具有抗溃疡活性、抗分泌和细胞保护活性。

Diadenosine pentaphosphate pentaammonium, an endogenous vasoactive purine dinucleotide isolated from thrombocytes, is one component of the diadenosine polyphosphates (ApnA, n=2-7) family. These compounds are found in secretory vesicles, including those in platelets, chromaffin cells, Torpedo synaptic terminals, and brain synaptosomes[1][2].

Bam 1745 is a significant adrenomedullary secretory vesicles component.

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM.

LY433771 is a compound that inhibits the activity of Type X secretory phospholipase A2.

hnps-PLA Inhibitor 是人类非胰腺分泌型磷脂酶 A (hnps-PLA) 的抑制剂。

Varespladib sodium (LY315920 sodium) is a highly potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), with an IC50 of 9 nM. It demonstrates significant inhibitory activity against sPLA2 in serum samples from multiple species, including rat, rabbit, guinea pig, and human, with IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively.

BML-265 是一种高效的EGFR酪氨酸激酶 (EGFR tyrosine kinase) 抑制剂。它能够破坏高尔基体的完整性，并阻止分泌蛋白的物质转运。在人类细胞中，BML-265 会影响高尔基体的完整性和转运，但对啮齿动物细胞中的高尔基体无显著影响。

Ro 23-9358 是一种具抗炎特性的强效分泌型磷脂酶 A2 抑制剂。

Dehydroabietic acid (Dehydroabietate) 是 EBV-EA 活化抑制剂。 它是食物衍生化合物，可通过降低血浆葡萄糖、胰岛素水平、血浆甘油三酯 (TG) 和肝 TG 水平来治疗肥胖相关疾病。它的衍生物在动物模型中表现出抗分泌和抗胃蛋白酶作用。

Serpinin 作为蛋白酶抑制剂 Nexin-1 (PN-1) 的激动剂，通过 cAMP-PKA-Sp1 信号通路增强 PN-1 的表达，并促进内分泌细胞的颗粒生成。此外，Serpinin 亦作为β-肾上腺素能受体的选择性激动剂，通过与 β1-肾上腺素能受体的相互作用激活 AC-cAMP-PKA 途径，从而调控心肌的收缩与舒张。其衍生物 pGlu-serpinin 通过上调 Bcl2 mRNA 的转录具有神经保护功能，常用于研究分泌功能的调节。

CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2]. Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 hydrochloride has the potential for inflammatory bowel disease research[1]. [1]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002;16(3):407-413.[2]. Selwood T, et al. Potent bivalent inhibition of human tryptase-beta by a synthetic inhibitor. Biol Chem. 2003;384(12):1605-1611.

Competitive inhibitor of secretory phospholipase A2 (sPLA2)