colonic

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。

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。

P-XSC 具有抗癌活性，抑制腺瘤性息肉患者结肠上皮细胞增殖，可用于研究乳腺癌。

Quercetagitrin 是分离自非洲万寿菊花 (Tagetes erecta) 中，具有抗炎作用。

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。

(S)-Elobixibat 是 Elobixibat 的 S 型异构体，是一种口服有效的 Apical Sodium-Dependent Bile (IBAT) 抑制剂。它可降低 LDL 胆固醇，增加血清 GLP-1，促进结肠运动，并可能用于治疗代谢综合征。(S)-Elobixibat 还可以用于研究便秘、血脂异常、非酒精性肝炎以及肝脏肿瘤。

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 CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). 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 CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).

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

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

(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。

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

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。

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

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-expressing FRT cells.

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。

Des-4-fluorobenzyl Mosapride, the main metabolite of mosapride, acts as a gastroprokinetic agent improving upper gastrointestinal (GI) motility by stimulating the serotonin receptor 4 (5-HT4; EC50= 74.2 nM, in guinea pig ileal longitudinal muscle myenteric plexus). It has been shown to increase colonic motility in dogs, horses, and guinea pigs in vivo. Mosapride, including this metabolite, is utilized in human and veterinary medicine to mitigate post-surgical and Parkinson's-induced constipation.

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, expression of TNF-α and IL-6, and colonic damage in a mouse model of TNBS-induced ulcerative colitis.4Taurohyodeoxycholic acid MaxSpec standard is a quantitative grade standard of taurohyodeoxycholic acid (sodium salt) that has been prepared specifically for mass spectrometry and related applications where quantitative reproducibility is required. The solution has been prepared gravimetrically and is supplied in a deactivated glass ampule sealed under argon. The concentration was verified by comparison to an independently prepared calibration standard. Verified concentration is provided on the certificate of analysis. This taurohyodeoxycholic acid MaxSpec standard is guaranteed to meet identity, purity, stability, and concentration specifications and is provided with a batch-specific certificate of analysis. Ongoing stability testing is performed to ensure the concentration remains accurate throughout the shelf life of the product.Note: The amount of solution added to the vial is in excess of the listed amount. Therefore, it is necessary to accurately measure volumes for preparation of calibration standards. Follow recommended storage and handling conditions to maintain product quality.

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。

Glycoursodeoxycholic Acid-d4 是 Glycoursodeoxycholic Acid 的氘代化合物。Glycoursodeoxycholic Acid 的 CAS 号为 64480-66-6。Glycoursodeoxycholic acid 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。

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。

Glycodeoxycholate Sodium 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。

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

13,14-Dihydro-15-keto prostaglandin D2 (DK-PGD2), a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway, is a selective agonist for the DP2 receptor and can inhibit ion flux in canine colonic mucosa preparation [1].

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

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。

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 of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.

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

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

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 hydroxy radicals. Unlike sulfasalazine, N-acetyl-5-aminosalicylic acid does not inhibit 15-hydroxy prostaglandin dehydrogenase (PGDH). Urinary levels of N-acetyl-5-aminosalicylic acid have been used as a marker of 5-ASA adherence in patients with inflammatory bowel disease.

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.