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19

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T0081 Lafutidine

拉呋替丁,FRG-8813

5-HT Receptor; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Lafutidine (FRG-8813) 是一种组胺受体 H2RA 拮抗剂,可抑制胃酸分泌,具有胃粘膜保护作用,可用于研究胃食管反流疾病。
T13385 Zamifenacin fumarate

扎非那星富马酸盐,UK-76654 fumarate

AChR Neuroscience
Zamifenacin fumarate (UK-76654 fumarate) 是肠道选择性毒蕈碱M3受体的有效拮抗剂, 可显著降低肠易激综合症的结肠蠕动。
T0918 Trimebutine

曲美布汀,Mebutin

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Trimebutine (Mebutin) 是阿片受体激动剂,有抗毒蕈碱活性。它是解痉剂,可调节肠道和结肠运动,并通过抗毒蕈碱和弱μ-阿片受体激动剂作用缓解腹痛。
T36126 TMP-153

Acyl-CoA:cholesterol acyltransferase (ACAT) catalyses the esterification of excess cellular cholesterol with fatty acids and is important for intestinal cholesterol absorption, hepatic lipoprotein secretion, and cholesterol accumulation in vascular tissues. ACAT inhibitors improve plasma lipid profile and ameliorate proteinuria in nephrotic animals. TMP-153 is a quinolyl derivative that inhibits ACAT with IC50 values of 5-10 nM in various animals. At 0.5-1.5 mg/kg, TMP-153 dose-dependently reduc...
T30640 Butyrylcholine

BA 51 090059,BA-51-090059,BA 51090059,BA 51-090059

Butyrylcholine is a novel colonic ion transport regulator produced by colonic epithelial cells that stimulates nicotine and muscarinic receptors.
T34710 STA 2

ONO 11113,STA-2,STA2

STA 2 is an analogue of TXA2, a thromboxane receptor in the colonic epithelium.
T71738 DRAinh-A250

DRAinh-A250 is a SLC26A3 inhibitor which blocks colonic fluid absorption and reduces constipation.
T33443 MK-8970

MK-8970 is an acetal carbonate prodrug of raltegravir with enhanced colonic absorption.
T17283 Zamifenacin

UK-76654

Others Others
Zamifenacin obviously decreases colonic motility in irritable bowel syndrome. Zamifenacin is an effective gut-selective muscarinic M3 receptor antagonist.
T29887 Aloe emodin anthrone

Aloe emodin anthrone is a stimulant-laxative which has been shown to enhance colonic membrane permeability of water-soluble and poorly permeable compounds.
T68735 Ciclotropium (free base)

Ciclotropium (free base) is quaternary ammonium compound with anticholinergic and parasympatholytic activity. Oral Cyclotropium bromide inhibited fasting and meal-stimulated colonic motility significantly without causing adverse side effects. After cyclotropium bromide, there was a significant correlation between antral contraction amplitude and gastric emptying.
T35374L (Ala13)-Apelin-13 acetate

Apelin receptor GPCR/G Protein
(Ala13)-Apelin-13 acetate,一种 APJ 拮抗剂,可调节CRF 诱导的增强的结肠运动、内脏敏感性和肠屏障。
T35708 N-acetyl-5-Aminosalicylic Acid

N-acetyl-5-Aminosalicylic acid is a metabolite of the anti-inflammatory agent 5-aminosalicylic acid and its prodrug form, sulfasalazine . It is formed in the liver, intestinal lumen, and colonic epithelial cells via N-acetyltransferases. It reduces IFN-γ binding to colonic epithelial cells by 24% when used at a concentration of 10 mM. N-acetyl-5-Aminosalicylic acid (100 μM) scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay and inhibits base hydroxylation in DNA stimulated by ...
T76319 Urocortin III (mouse) (free acid)

Urocortin III (mouse) (free acid) 是一种选择性的 CRF2受体激动剂 (对 CRF2受体具有高亲和力)。Urocortin III (mouse) (free acid) 可显著抑制胃排空而不改变结肠运输。
T64294 Succinic acid sodium

Succinic acid sodium 是一种口服具有活力的抗焦虑剂。Succinic acid sodium 能够下调 KCNMB1 (钾通道亚基 β1) 和TET1(10-11 易位 1) 的表达。Succinic acid sodium 可抑制体内的结肠上皮细胞的增殖。Succinic acid sodium 能够用于研究妊娠期高血压。
T78540 α-CGRP (mouse, rat) TFA

CGRP Receptor GPCR/G Protein; Neuroscience
α-CGRP (mouse, rat) TFA 是神经系统中的一种活性神经肽,位于神经肌肉接合部,具有显著的血管舒张功能。适用于心血管疾病、炎症、偏头痛及代谢研究领域。
T83955 MOMBA

MOMBA是一种针对人类自由脂肪酸2(hFFA2)工程化受体和设计药物激活的设计受体(DREADD)的选择性正交激动剂,对野生型hFFA2、hFFA3和小鼠FFA2无活性。MOMBA能够在表达hFFA2-DREADD受体的细胞中抑制forskolin刺激的cAMP水平,其功效改善且与山梨酸的效力相当。在hFFA2-DREADD转基因小鼠中,MOMBA治疗显著降低肠道传输速度,并促进依赖浓度的结肠隐窝GLP-1释放。该化合物具有口服生物利用度。
T36373 Urocortin II (mouse) (trifluoroacetate salt)

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF...
T65994 (6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation...

化合物

Lafutidine
Cat.No: T0081
Synonym: 拉呋替丁,FRG-8813
Target: 5-HT Receptor, Histamine Receptor
Zamifenacin fumarate
Cat.No: T13385
Synonym: 扎非那星富马酸盐,UK-76654 fumarate
Target: AChR
Trimebutine
Cat.No: T0918
Synonym: 曲美布汀,Mebutin
Target: Opioid Receptor
TMP-153
Cat.No: T36126
Synonym:
Target:
Butyrylcholine
Cat.No: T30640
Synonym: BA 51 090059,BA-51-090059,BA 51090059,BA 51-090059
Target:
STA 2
Cat.No: T34710
Synonym: ONO 11113,STA-2,STA2
Target:
DRAinh-A250
Cat.No: T71738
Synonym:
Target:
MK-8970
Cat.No: T33443
Synonym:
Target:
Zamifenacin
Cat.No: T17283
Synonym: UK-76654
Target: Others
Aloe emodin anthrone
Cat.No: T29887
Synonym:
Target:
Ciclotropium (free base)
Cat.No: T68735
Synonym:
Target:
(Ala13)-Apelin-13 acetate
Cat.No: T35374L
Synonym:
Target: Apelin receptor
N-acetyl-5-Aminosalicylic Acid
Cat.No: T35708
Synonym:
Target:
Urocortin III (mouse) (free acid)
Cat.No: T76319
Synonym:
Target:
Succinic acid sodium
Cat.No: T64294
Synonym:
Target:
α-CGRP (mouse, rat) TFA
Cat.No: T78540
Synonym:
Target: CGRP Receptor
MOMBA
Cat.No: T83955
Synonym:
Target:
Urocortin II (mouse) (trifluoroacetate salt)
Cat.No: T36373
Synonym:
Target:
(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
Cat.No: T65994
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T4S0554 Theaflavine-3,3'-digallate

TFBG,theaflavin digallate,3,3’-二没食子酸酯茶黄素

Others Others
Theaflavine-3,3'-digallate (theaflavin digallate) 和乳酸一起可以减少单纯疱疹病毒的传播。
T5254 Glycodeoxycholate Sodium

Sodium glycyldeoxycholate,Sodium glycodeoxycholate,Glycodeoxycholic acid sodium salt,脱氧甘胆酸钠

Others; Endogenous Metabolite Metabolism; Others
Glycodeoxycholate Sodium (Glycodeoxycholic acid sodium salt) 诱导肝细胞凋亡的机制与内切酶的DNA裂解有关。它是一种次级胆汁酸,由结肠环境中微生物菌群中存在的酶的作用产生。
T5259 Glycochenodeoxycholic acid sodium salt

GCDCA,甘氨鹅脱氧胆酸钠,Sodium glycochenodeoxycholate

Apoptosis; Others; Endogenous Metabolite Apoptosis; Metabolism; Others
Glycochenodeoxycholic acid sodium salt (GCDCA) 是一种从脱氧鹅胆酸和甘氨酸在肝脏中形成的胆汁盐,可诱导肝细胞凋亡。它起到洗涤剂的作用,可溶解脂肪吸收,并本身被吸收。
T5234 Glycoursodeoxycholic acid

Ursodeoxycholylglycine,甘氨熊胆酸,GUDCA

Others; Endogenous Metabolite Metabolism; Others
Glycoursodeoxycholic acid (Ursodeoxycholylglycine) 是一种酰基甘氨酸和胆汁酸-甘氨酸缀合物,是熊去氧胆酸的代谢物。
T29888 Aloe-emodin-glucoside

Aloe-emodin-glucoside is a stimulant-laxative which has been shown to enhance colonic membrane permeability of water-soluble and poorly permeable compounds.
TN1834 Kobusin

去甲槟郎碱,自旋七叶素

Others; NOS; NF-κB Immunology/Inflammation; NF-κB; Others
Kobusin, a Calmodulin inhibitor, shows mild antiplasmodial,anti-inflammatory, and cytotoxic activities; it may be beneficial for the treatment of neuro-inflammatory diseases through the inhibition of iNOS expression and peroxynitrite scavenging potential. Kobusin can mildly reduce gastrointestinal motility in mice, it activates CFTR and CaCCgie chloride channel activities in mouse colonic epithelia and shows inhibitory effects toward ANO1/CaCC-mediated short-circuit currents in ANO1/CaCC-express...
T37770 Taurohyodeoxycholic acid

Taurohyodeoxycholic acid (THDCA) is a taurine-conjugated form of the secondary bile acid hyodeoxycholic acid .1THDCA decreases the size and weight of human gallstonesin vitro. It increases bile flow, biliary cholesterol secretion, and biliary lipid secretion in rats.2Co-administration of THDCA with taurochenodeoxycholic acid prevents TCDCA-induced hepatotoxicity, increasing bile flow as well as biliary acid and phospholipid secretion in rats.3THDCA also reduces myeloperoxidase activity, expressi...

天然产物

Theaflavine-3,3'-digallate
Cat.No: T4S0554
Synonym: TFBG,theaflavin digallate,3,3’-二没食子酸酯茶黄素
Target: Others
Glycodeoxycholate Sodium
Cat.No: T5254
Synonym: Sodium glycyldeoxycholate,Sodium glycodeoxycholate,Glycodeoxycholic acid sodium salt,脱氧甘胆酸钠
Target: Others, Endogenous Metabolite
Glycochenodeoxycholic acid sodium salt
Cat.No: T5259
Synonym: GCDCA,甘氨鹅脱氧胆酸钠,Sodium glycochenodeoxycholate
Target: Apoptosis, Others, Endogenous Metabolite
Glycoursodeoxycholic acid
Cat.No: T5234
Synonym: Ursodeoxycholylglycine,甘氨熊胆酸,GUDCA
Target: Others, Endogenous Metabolite
Aloe-emodin-glucoside
Cat.No: T29888
Synonym:
Target:
Kobusin
Cat.No: TN1834
Synonym: 去甲槟郎碱,自旋七叶素
Target: Others, NOS, NF-κB
Taurohyodeoxycholic acid
Cat.No: T37770
Synonym:
Target:
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