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24

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T2319 Acotiamide monohydrochloride trihydrate

Acotiamide hydrochloride,YM-443 HCl,盐酸阿考替胺,Z-338 HCl

AChE Neuroscience
Acotiamide monohydrochloride trihydrate (Z-338 HCl) 是一种首创的、具有口服活性的胃肠动力药。它通过促毒蕈碱受体拮抗作用和乙酰胆碱酯酶(AChE)抑制作用增强肠神经元释放的乙酰胆碱,从而增强胃排空和胃部适应性,有潜力用于功能性消化不良的研究。
T31597 Ecabapide

DQ2511,DQ 2511,DQ-2511

Others Others
Ecabapide (DQ-2511) 是一种新型促胃肠蠕动剂,能显著增强SHRSP的胃排空能力。Ecabapide 可激活的兔胃壁细胞中的环状 GMP 依赖性管家 Cl- 通道。
T68100 Mifentidine

DA 4577

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Mifentidine (DA 4577) 是一种可口服的 H2 受体拮抗剂,可用于研究胃排空和实验性胃和十二指肠溃疡。
T1291 Cisapride

西沙必利,西沙比利,Prepulsid,R 51619,Pridesia,Kaudalit,(±)-Cisaprid,Kinestase

Potassium Channel; 5-HT Receptor; HER Angiogenesis; GPCR/G Protein; JAK/STAT signaling; Membrane transporter/Ion channel; Neuroscience; Tyrosine Kinase/Adaptors
Cisapride (R 51619) 是一种5-HT4受体激动剂,还是 hERG 抑制剂。它可作用于肠道中的血清素受体,促进肠道蠕动,增加胃排空并减少食管反流。
T21385 Cinitapride

西尼必利,Paxapride,Cidine,cinitapride tartrate,Blaston,Cintapro,Cinmove

5-HT Receptor GPCR/G Protein; Neuroscience
Cinitapride (Blaston) 是一种促胃药。它减缓肌肉的活动,以减轻诸如胃酸反流、胃排空延迟和溃疡性消化不良等病症的症状。 Cinitapride 作为 5-HT2 受体的拮抗剂和 5-HT1 和 5-HT4 受体的激动剂。
T34281 Relamorelin

BIM28131,RM 131,BIM-28131,BIM-28163,BIM 28163,BIM28163,BIM 28131

GHSR GPCR/G Protein
Relamorelin (RM-131)是一种具有选择性和有效性的生长素释放肽/生长激素促分泌素受体 (GHSR) 激动剂,是一种有效的生长素释放肽模拟物,对 GHS-1a 受体具有很高的亲和力。Relamorelin 是一种具有中枢渗透性的五肽,可增加生长激素水平,加速胃排空,具有研究恶病质的潜力。
T31214 Dazopride fumarate

AHR-5531C

Dazopride fumarate is a peristaltic used to enhance gastric emptying and block emesis.
T27550 HMR-1426

HMR 1426,HMR1426

HMR-1426 is gastric emptying inhibitor. HMR1426 shows an anorectic potential in rats and decreased body weight and fat mass. This was achieved solely by reducing food intake without influencing overall energy expenditure or behavior.
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.
T63237 Acotiamide hydrochloride

Acotiamide hydrochloride 是选择性的、口服具有活力的、可逆的乙酰胆酶碱酯 (AChE) 抑制剂 (IC50: 1.79 μM),能够提高胃收缩性,加速胃排空延迟,能够用于研究胃动力障碍的功能性消化不良及肠道炎症。
TP2095 Astressin 2B

Potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist (IC50 values are 1.3 and > 500 nM for CRF2 and CRF1 respectively). Antagonizes CRF2-mediated inhibition of gastric emptying.
T22230 Acotiamide

Acotiamide 是一种具有口服活性、选择性和可逆性的乙酰胆酶碱酯 (AChE) 抑制剂,IC50值为1.79 μM。Acotiamide 是一种胃促动力剂,可增强胃收缩性并加速胃排空延迟。Acotiamide 可用于胃动力障碍的功能性消化不良及肠道炎症的研究。
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。
T39236 Relamorelin acetate

Relamorelin acetate,RM-131 acetate,BIM-28131acetate

Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for it...
T76195 Stresscopin-related peptide (human)

Stresscopin-related peptide (human) 是 2 型 CRH 受体的特异性配体。Stresscopin-related peptide (human) 抑制食物摄入,延迟胃排空,并减少热引起的水肿。Stresscopin-related peptide (human) 在应激后维持体内平衡,可用于应激相关疾病的研究。
T83694 Gastric Inhibitory Peptide (1-42) (porcine) TFA

GIP (1-42),Glucose-dependent Insulinotropic Polypeptide (1-42)

胃抑制肽(GIP) (1-42)是一种内源性的42氨基酸肽类肠促素激素,能诱导胰岛素分泌。该激素在肠道神经内分泌K细胞和颌下腺中表达,并在餐后释放到循环中。GIP (1-42)抑制由组胺、五肽和胰岛素引起的胃酸和胃蛋白酶分泌,增加葡萄糖诱导的胰岛素释放,并在大鼠中刺激胃排空。
T75787 Amylin, amide, human TFA

Amylin, amide, human TFA 是一种含有37个氨基酸的胰腺多肽,与胰岛素共同分泌,对代谢和维持葡萄糖稳态具有重要作用。该化合物能够抑制胰高血糖素的分泌,延缓胃排空速度,同时作为增加饱腹感的因子。
T76263 Beinaglutide

Beinaglutide 是一种重组人 GLP-1(rhGLP-1) 多肽,与人 GLP-1(7-36) 具有几乎 100% 的同源性。Beinaglutide 在血糖控制、抑制食物摄入和胃排空和促进体重减轻方面表现出依赖于剂量的作用。Beinaglutide 具有研究超重/肥胖和非酒精性脂肪性肝炎 (NASH) 的潜力。
T70267 ADL 08-0011 HCl

ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg/kg) reverse...
T75262 Relamorelin TFA

Relamorelin (RM-131) TFA,一种生长素类似物,是一种选择性的生长素释放肽/生长激素促分泌素受体 (GHSR) 激动剂,对GHS-1a 受体的Ki 值为 0.42 nM。Relamorelin TFA 是一种五肽,具有中枢渗透性。Relamorelin TFA 增加生长激素水平,加速胃排空,具有用于恶病质、胃轻瘫和胃/肠运动障碍研究的潜力。
T35627 Amylin (human) (trifluoroacetate salt)

Amylin is a 37-residue peptide hormone secreted from pancreatic β-cells that reduces food intake, decreases glucagon secretion, slows gastric emptying, and increases satiety. It binds to amylin receptors with IC50 values of 2 and 0.2 nM for porcine and guinea pig nucleus accumbens membrane preparations, respectively. Amylin is present in amyloid aggregates derived from the pancreatic islets of humans with type 2 diabetes. Amylin forms fibrils that react to thioflavin T and are organized in a cro...
T14382 AZD7687

Others Others
AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1). IC50 value: 80 nM [1] Target: DGAT1 in vitro: Plasma AZD7687 exposure was measured repeatedly. AZD7687 markedly reduced postprandial TAG excursion with a steep concent
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...
T35787 Obestatin (human) (trifluoroacetate salt)

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manne...

化合物

Acotiamide monohydrochloride trihydrate
Cat.No: T2319
Synonym: Acotiamide hydrochloride,YM-443 HCl,盐酸阿考替胺,Z-338 HCl
Target: AChE
Ecabapide
Cat.No: T31597
Synonym: DQ2511,DQ 2511,DQ-2511
Target: Others
Mifentidine
Cat.No: T68100
Synonym: DA 4577
Target: Histamine Receptor
Cisapride
Cat.No: T1291
Synonym: 西沙必利,西沙比利,Prepulsid,R 51619,Pridesia,Kaudalit,(±)-Cisaprid,Kinestase
Target: Potassium Channel, 5-HT Receptor, HER
Cinitapride
Cat.No: T21385
Synonym: 西尼必利,Paxapride,Cidine,cinitapride tartrate,Blaston,Cintapro,Cinmove
Target: 5-HT Receptor
Relamorelin
Cat.No: T34281
Synonym: BIM28131,RM 131,BIM-28131,BIM-28163,BIM 28163,BIM28163,BIM 28131
Target: GHSR
Dazopride fumarate
Cat.No: T31214
Synonym: AHR-5531C
Target:
HMR-1426
Cat.No: T27550
Synonym: HMR 1426,HMR1426
Target:
Ciclotropium (free base)
Cat.No: T68735
Synonym:
Target:
Acotiamide hydrochloride
Cat.No: T63237
Synonym:
Target:
Astressin 2B
Cat.No: TP2095
Synonym:
Target:
Acotiamide
Cat.No: T22230
Synonym:
Target:
Urocortin III (mouse) (free acid)
Cat.No: T76319
Synonym:
Target:
Relamorelin acetate
Cat.No: T39236
Synonym: Relamorelin acetate,RM-131 acetate,BIM-28131acetate
Target:
Stresscopin-related peptide (human)
Cat.No: T76195
Synonym:
Target:
Gastric Inhibitory Peptide (1-42) (porcine) TFA
Cat.No: T83694
Synonym: GIP (1-42),Glucose-dependent Insulinotropic Polypeptide (1-42)
Target:
Amylin, amide, human TFA
Cat.No: T75787
Synonym:
Target:
Beinaglutide
Cat.No: T76263
Synonym:
Target:
ADL 08-0011 HCl
Cat.No: T70267
Synonym:
Target:
Relamorelin TFA
Cat.No: T75262
Synonym:
Target:
Amylin (human) (trifluoroacetate salt)
Cat.No: T35627
Synonym:
Target:
AZD7687
Cat.No: T14382
Synonym:
Target: Others
Urocortin II (mouse) (trifluoroacetate salt)
Cat.No: T36373
Synonym:
Target:
Obestatin (human) (trifluoroacetate salt)
Cat.No: T35787
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5S1389 Escin IB

七叶皂苷B,七叶皂苷 IB

5-HT Receptor; NO Synthase GPCR/G Protein; Immunology/Inflammation; Neuroscience
Escin IB 是一种皂苷,分离自马栗子种子的皮和胚乳中,能够抑制 pancreatic lipase 的活性。
T5S2360 Corydaline

Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline

P450; Virus Protease; Opioid Receptor; AChE Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
Corydaline (Corydalin) 是从 Corydalis yanhusuo 提取的一种异喹啉生物碱,是一种新型促动力植物药的主要活性成分之一。它促进胃排空和小肠转运,促进胃的调节,具有抗乙酰胆碱酯酶、抗过敏和镇痛活性。
T3727 Methyl syringate

Syringic Acid Methyl Ester,丁香酸甲酯

TRP/TRPV Channel Membrane transporter/Ion channel
Methyl syringate (Syringic Acid Methyl Ester) 是水仙花蜜的化学标记物,是有效的细菌和真菌漆酶酚介质。它也是TRPA1激动剂。
T81080 Strictinin

Strictinin 是从普洱茶 (Pu'er teas) 分离得到的酚类化合物,展现出潜在的抗病毒、抗菌和通便活性。这些活性是由于它加速小肠转运所致,并非因增强胃排空、增加食物摄入或诱导大鼠腹泻而发挥作用。

天然产物

Escin IB
Cat.No: T5S1389
Synonym: 七叶皂苷B,七叶皂苷 IB
Target: 5-HT Receptor, NO Synthase
Corydaline
Cat.No: T5S2360
Synonym: Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline
Target: P450, Virus Protease, Opioid Receptor, AChE
Methyl syringate
Cat.No: T3727
Synonym: Syringic Acid Methyl Ester,丁香酸甲酯
Target: TRP/TRPV Channel
Strictinin
Cat.No: T81080
Synonym:
Target:
TargetMol Loading
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