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39

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8599 Betazole dihydrochloride

盐酸倍他唑,Betazole hydrochloride

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
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。
T2044 Varespladib

LY315920,伐瑞拉地,伐瑞拉迪

Phospholipase Metabolism
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。
T22665 PD 128042

CI 976

Acyltransferase Metabolism
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。
T6928 Pantoprazole

SKF96022,泮托拉唑,BY1023

Apoptosis; Proton pump; Autophagy Apoptosis; Autophagy; Membrane transporter/Ion channel
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。
T0161 Pantoprazole Sodium Hydrate

SKF96022 sodium hydrate,泮托拉唑钠水合物,BY1023 (sodium hydrate),SKF96022 (sodium hydrate)

Apoptosis; Potassium Channel; Proton pump; Autophagy Apoptosis; Autophagy; Membrane transporter/Ion channel
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。
T6929 Pantoprazole sodium

Pantecta,泮托拉唑钠盐,SKF96022 sodium,SKF96022 (sodium),BY1023 (sodium),泮托拉唑钠,BY-1023 sodium,Pantoloc

Apoptosis; Others; Proton pump; HIF; Autophagy Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Membrane transporter/Ion channel; Others
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。
T17218 Varespladib methyl

A-002,LY333013

Others; Phospholipase Metabolism; Others
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。
T4192 hnps-PLA Inhibitor

Phospholipase; LTR Immunology/Inflammation; Metabolism
hnps-PLA Inhibitor 是人类非胰腺分泌型磷脂酶 A (hnps-PLA) 的抑制剂。
T2486 IOWH-032

IOWH032,IOWH 032

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
IOWH-032 (IOWH032) 是一种合成 CFTR 抑制剂,可用于研究治疗霍乱、腹泻和分泌性腹泻,在T84和CHO-CFTR 细胞实验中IC50为1.01 uM。
T0594 Diphenmanil methylsulfate

Diphemanil mesylate,Diphemanil Methylsulfate,甲硫二苯马尼

AChR Neuroscience
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。
T16865 SCH28080

ATPase; Proton pump Membrane transporter/Ion channel
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。
T1756 Ilaprazole sodium

IY-81149 sodium,艾普拉唑钠

Proton pump; TOPK MAPK; Membrane transporter/Ion channel
Ilaprazole sodium (IY-81149 sodium) 是一种具有口服活性质子泵抑制剂,以剂量依赖性方式不可逆地抑制 H+/K+-ATPase,在兔壁细胞制剂中的 IC50为 6 μM。它也是一种有效的 T 细胞起源蛋白激酶(TOPK)抑制剂,用于胃溃疡的研究。
T30290 Bam 1745

Bam1745,Pyroglutamyl peptide bam-1745,Bam-1745

Bam 1745 is a significant adrenomedullary secretory vesicles component.
T29056 UK-9040

UK9040,UK 9040

UK-9040 inhibits gastric secretory.
T23547 YM 26734

Others Others
Competitive inhibitor of secretory phospholipase A2 (sPLA2)
T27539 Hexocyclium metilsulfate

AB803,AB-803,Traline,AB 803

Hexocyclium metilsulfate has anti-gastric secretory effects in humans.
T10008 BTM-1086

Others Others
BTM-1086 is a potent gastric secretory inhibitor and an anti-ulcer agent.
T15672 KU14R

Others Others
KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.
T20755 Trimegestone

RU27987,RU-27987,RU 27987

Trimegestone, a highly effective oral progestogen, is used for endometrial protection, all doses inducing secretory endometrial transformation.
T29288 163-BP3

163-bp3 is an effective photoaffinity probe and can be used as a target γ Secretory enzyme.
T68573 Tigapotide triflutate

Tigapotide triflutate is a synthetic peptide corresponding to amino acids 31-45 of PSP94 (prostate secretory protein) that inhibits matrix metalloproteinase-9 secretion.
T68574 Tigapotide Free Base

Tigapotide Free Base is a synthetic peptide corresponding to amino acids 31-45 of PSP94 (prostate secretory protein) that inhibits matrix metalloproteinase-9 secretion.
T30831 Cgp 43182

Cgp-43182,Cgp43182

CGP 43182 is an effective inhibitor of group IIA secretory phospholipase A2 (Group IIA sPLA2) activity in vitro, which can be used to prevent the synergistic effect of pro-inflammatory genes stimulated by cytokines mediated by NFkappaB.
T37309 Diadenosine pentaphosphate pentaammonium

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].
T76538 Pancreatic polypeptide

Pancreatic polypeptide 是由胰腺内分泌的 PP 细胞所分泌的多肽,具有调节胰腺分泌功能、影响肝糖原储存及胃肠分泌的作用。
T41088 Diadenosine pentaphosphate pentalithium

Diadenosine pentaphosphate pentalithium is an endogenous vasoactive purine dinucleotide, isolated from thrombocytes. It is a member of the diadenosine polyphosphates (ApnA, n=2–7) and is found in secretory vesicles of platelets, chromaffin cells, Torpedo synaptic terminals, and brain synaptosomes.
T39173 Varespladib sodium

LY315920 sodium,伐瑞拉迪钠;伐瑞拉地钠

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.
T28331 PD 136450

Cam1189,PD136450,Cam-1189,PD-136450,Cam 1189

Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Gastrin (cholecystokinin type B (CCK-B)) receptor antagonists may help to elucidate the physiological role o
T37310 Diadenosine pentaphosphate pentasodium

Diadenosine pentaphosphate pentasodium, an endogenous vasoactive purine dinucleotide isolated from thrombocytes, serves as a key component of secretory vesicles in platelets, chromaffin cells, Torpedo synaptic terminals, and brain synaptosomes. This compound, along with other diadenosine polyphosphates (ApnA, n=2-7), plays a crucial role in physiological processes[1][2].
T81183 Sec61-IN-5

Sec61-IN-5 (Compound 16c)是一种Sec61抑制剂,在A549细胞中展现出细胞毒性(IC50: 0.27 nM),并且能够抑制Sec61依赖性分泌功能(IC50: 0.08 nM)。
T76480 Amylin (1-37) (human)

Amylin (1-37) (human) (hIAPP (1-37)) 为胰岛β细胞分泌颗粒中的肽类激素,其C端经酰胺化处理,第2和第7个半胱氨酸残基间形成二硫键。
T61265 Exo2

Exo2 is a secretion inhibitor that hinders the trafficking of Shiga toxin from endosomes to the trans-Golgi network. It inhibits the exit of secretory cargo from the endoplasmic reticulum (ER) and disrupts the Golgi apparatus. Notably, Exo2 does not impact the morphology of the trans-Golgi network (TGN). Additionally, Exo2 has the ability to induce calcium-dependent exocytosis in permeabilized adrenal chromaffin cells [1] [2].
T72005 Betazole

Ametazole

Betazole (Ametazole) 为一种吡唑类组胺,具有口服活性,作为H2受体激动剂发挥作用。该化合物能诱导胃酸分泌并立即显著提高胆总管压力。Betazole 作为一种称为histalog的诊断剂,应用于评估胃酸分泌功能。
T76320 FIZZ-1 (32-51) (mouse)

FIZZ-1 (32-51) (mouse) 是一种富含半胱氨酸的分泌性蛋白,主要在过敏性气道炎症中被巨噬细胞、支气管上皮细胞及II型肺泡上皮细胞高度表达,具有对肺成纤维细胞的抗凋亡功能,广泛应用于过敏性肺炎的研究领域。
T74891 Apratoxin S4

Apratoxin S4(Apra S4)是一种Sec61抑制剂,能够有效阻止分泌蛋白的共翻译转运进入内质网(ER)。它对flaviviruses类病毒显示出抗病毒效果,IC50值在0.46 nM至170 nM不等。此外,Apratoxin S4通过抑制多条血管生成通路,能够抑制视网膜血管细胞活化,适用于病毒感染、血管生成相关疾病和癌症的研究。
T37331 Pyrrophenone

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 py...
T38052 CRA-2059 TFA

CRA-2059 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 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...
T38051 CRA-2059 hydrochloride

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. Ali...
T38286 C26 Sphingomyelin (d18:1/26:0)

C26 Sphingomyelin (d18:1/26:0)

C26 Sphingomyelin is a sphingolipid that has been found in serum and cell or brain extracts.1,2,3C26 sphingomyelin levels are increased in the serum of patients with hemophagocytic lymphohistiocytosis, an inflammatory condition characterized by excessive immune activation.3C26 sphingomyelin has been used a component of monolayers to study the influence of sphingomyelin acyl chain length on sphingomyelin-sterol interactions.4[Matreya, LLC.] 1.Wang, J.-R., Zhang, H., Yau, L.D., et al.Improved sphi...

化合物

Betazole dihydrochloride
Cat.No: T8599
Synonym: 盐酸倍他唑,Betazole hydrochloride
Target: Histamine Receptor
Varespladib
Cat.No: T2044
Synonym: LY315920,伐瑞拉地,伐瑞拉迪
Target: Phospholipase
PD 128042
Cat.No: T22665
Synonym: CI 976
Target: Acyltransferase
Pantoprazole
Cat.No: T6928
Synonym: SKF96022,泮托拉唑,BY1023
Target: Apoptosis, Proton pump, Autophagy
Pantoprazole Sodium Hydrate
Cat.No: T0161
Synonym: SKF96022 sodium hydrate,泮托拉唑钠水合物,BY1023 (sodium hydrate),SKF96022 (sodium hydrate)
Target: Apoptosis, Potassium Channel, Proton pump, Autophagy
Pantoprazole sodium
Cat.No: T6929
Synonym: Pantecta,泮托拉唑钠盐,SKF96022 sodium,SKF96022 (sodium),BY1023 (sodium),泮托拉唑钠,BY-1023 sodium,Pantoloc
Target: Apoptosis, Others, Proton pump, HIF, Autophagy
Varespladib methyl
Cat.No: T17218
Synonym: A-002,LY333013
Target: Others, Phospholipase
hnps-PLA Inhibitor
Cat.No: T4192
Synonym:
Target: Phospholipase, LTR
IOWH-032
Cat.No: T2486
Synonym: IOWH032,IOWH 032
Target: CFTR, Autophagy
Diphenmanil methylsulfate
Cat.No: T0594
Synonym: Diphemanil mesylate,Diphemanil Methylsulfate,甲硫二苯马尼
Target: AChR
SCH28080
Cat.No: T16865
Synonym:
Target: ATPase, Proton pump
Ilaprazole sodium
Cat.No: T1756
Synonym: IY-81149 sodium,艾普拉唑钠
Target: Proton pump, TOPK
Bam 1745
Cat.No: T30290
Synonym: Bam1745,Pyroglutamyl peptide bam-1745,Bam-1745
Target:
UK-9040
Cat.No: T29056
Synonym: UK9040,UK 9040
Target:
YM 26734
Cat.No: T23547
Synonym:
Target: Others
Hexocyclium metilsulfate
Cat.No: T27539
Synonym: AB803,AB-803,Traline,AB 803
Target:
BTM-1086
Cat.No: T10008
Synonym:
Target: Others
KU14R
Cat.No: T15672
Synonym:
Target: Others
Trimegestone
Cat.No: T20755
Synonym: RU27987,RU-27987,RU 27987
Target:
163-BP3
Cat.No: T29288
Synonym:
Target:
Tigapotide triflutate
Cat.No: T68573
Synonym:
Target:
Tigapotide Free Base
Cat.No: T68574
Synonym:
Target:
Cgp 43182
Cat.No: T30831
Synonym: Cgp-43182,Cgp43182
Target:
Diadenosine pentaphosphate pentaammonium
Cat.No: T37309
Synonym:
Target:
Pancreatic polypeptide
Cat.No: T76538
Synonym:
Target:
Diadenosine pentaphosphate pentalithium
Cat.No: T41088
Synonym:
Target:
Varespladib sodium
Cat.No: T39173
Synonym: LY315920 sodium,伐瑞拉迪钠;伐瑞拉地钠
Target:
PD 136450
Cat.No: T28331
Synonym: Cam1189,PD136450,Cam-1189,PD-136450,Cam 1189
Target:
Diadenosine pentaphosphate pentasodium
Cat.No: T37310
Synonym:
Target:
Sec61-IN-5
Cat.No: T81183
Synonym:
Target:
Amylin (1-37) (human)
Cat.No: T76480
Synonym:
Target:
Exo2
Cat.No: T61265
Synonym:
Target:
Betazole
Cat.No: T72005
Synonym: Ametazole
Target:
FIZZ-1 (32-51) (mouse)
Cat.No: T76320
Synonym:
Target:
Apratoxin S4
Cat.No: T74891
Synonym:
Target:
Pyrrophenone
Cat.No: T37331
Synonym:
Target:
CRA-2059 TFA
Cat.No: T38052
Synonym:
Target:
CRA-2059 hydrochloride
Cat.No: T38051
Synonym:
Target:
C26 Sphingomyelin (d18:1/26:0)
Cat.No: T38286
Synonym: C26 Sphingomyelin (d18:1/26:0)
Target:
Cat. No. Product Name Target Signaling Pathways
T13206 Tris(2,4-di-tert-butylphenyl)phosphate

Phospholipase Metabolism
Tris(2,4-di-tert-butylphenyl)phosphate 是一种从 Vitex negundoL 中分离的活性化合物,能够通过分子对接抑制了分泌性磷脂酶 A2(sPLA2),具有抗炎作用。
TN1419 Rhamnetin

beta-Rhamnocitrin,鼠李素

Others; Phospholipase Metabolism; Others
Rhamnetin (beta-Rhamnocitrin) 是一种槲皮素衍生物,在芫荽中被发现,具有抗氧化和抗炎活性。Rhamnetin 可抑制分泌型磷脂酶 A2。
TCS1772 Dehydroabietic acid

Dehydroabietate,脱氢松香酸

Antifection Microbiology/Virology
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。
TN5221 (-)-Variabilin

Variabilin, a novel inhibitor of human platelet aggregation, it is a potent RGD (Arg-Gly-Asp)-containing antagonist of the fibrinogen receptor glycoprotein IIb-IIIa (GPIIb-IIIa; αIIbβ3) and the vitronectin receptor αvβ3.Variabilin is also an antimicrobial furanosesterterpene. Variabilin is an inhibitor of human secretory and cytosolic phospholipase A2 (PLA2) activities that controls eicosanoid production in vitro and in vivo, inhibits neutrophil degranulation and superoxide generation in vitro a...
TN4659 Nimbin

COX Immunology/Inflammation; Neuroscience
Nimbin is an anti-pyretic, can be used to treat arthritis, hypoglycaemia, peptic ulcers, anti-secretory activity, and it can also be used as an antibiotic. Nimbin requires to elicit a 50% inhibition of this steroid hydroxylase activity in the three insect
T75540 Ipomoeassin F

Ipomoeassin F 是一种高效且具有选择性的内质网(ER)蛋白转位抑制剂,它通过作用于ER膜上的Sec61复合物(Sec61α)的成孔亚基来实现其功能。此化合物能特异性抑制SARS-CoV-2蛋白在ER膜上的转位,同时阻碍分泌蛋白和I型跨膜蛋白(TMP)的ER转运,但对III型TMP的转运不产生影响。

天然产物

Tris(2,4-di-tert-butylphenyl)phosphate
Cat.No: T13206
Synonym:
Target: Phospholipase
Rhamnetin
Cat.No: TN1419
Synonym: beta-Rhamnocitrin,鼠李素
Target: Others, Phospholipase
Dehydroabietic acid
Cat.No: TCS1772
Synonym: Dehydroabietate,脱氢松香酸
Target: Antifection
(-)-Variabilin
Cat.No: TN5221
Synonym:
Target:
Nimbin
Cat.No: TN4659
Synonym:
Target: COX
Ipomoeassin F
Cat.No: T75540
Synonym:
Target:
TargetMol Loading
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