Search Result
Results for "
ileum
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N0340
-
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Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
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mAChR
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Neurological Disease
Inflammation/Immunology
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Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
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- HY-141582
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N-Stearoyl phytosphingosine
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JNK
NF-κB
Interleukin Related
TNF Receptor
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Inflammation/Immunology
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Ceramide 3 (N-Stearoyl phytosphingosine) is an orally active major component of intercellular lipids in the stratum corneum of the skin, and belongs to the ceramide family. Ceramide 3 inhibits c-jun and NF-κB activation induced by Histamine (HY-B1204), and suppresses the expression of IL-4 and TNF-α. Ceramide 3 inhibits scratching behavior and vascular permeability in mice, and exhibits antihistamine effects in guinea pig ileum. Ceramide 3 improves skin barrier function, reduces transepidermal water loss, erythema and the number of circulating epidermal cells, and accelerates barrier repair of irritated or dysfunctional skin .
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- HY-P1714
-
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FE 203799
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GLP Receptor
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Metabolic Disease
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Apraglutide (FE 203799), a synthetic 33-amino-acid peptide and a long-acting GLP-2 analogue, enhances adaptation and linear intestinal growth in a neonatal piglet model of short bowel syndrome with total resection of the ileum .
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- HY-15039
-
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Bradykinin Receptor
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Metabolic Disease
Inflammation/Immunology
Endocrinology
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SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
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- HY-123068
-
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SQ 14551
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Drug Derivative
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Cardiovascular Disease
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Captopril disulfide (SQ 14551) is an orally active disulfide dimer prodrug. Captopril disulfide is metabolized to Captopril and acts as a Bradykinin potentiator. Captopril disulfide enhances the vasodilatory effect of Bradykinin in anesthetized rats and the contractile response of isolated guinea pig ileum to Bradykinin. Captopril disulfide exhibits antihypertensive activity in spontaneously hypertensive rats. Captopril disulfide can be used in hypertension-related research .
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- HY-153508
-
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Chloride Channel
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Others
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ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
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- HY-Y0047
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Picolamine; 3-Pyridinemethanamine; Pyridin-3-ylmethanamine
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Biochemical Assay Reagents
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Inflammation/Immunology
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3-Picolylamine is a primary amine compound containing a pyridine ring structure. 3-Picolylamine inhibits histaminase (diamine oxidase) activity in pig kidneys. 3-Picolylamine significantly enhances the contractile response of isolated guinea pig ileum to Histamine (HY-B1204). 3-Picolylamine can be used to study histamine-related physiological mechanisms or allergic diseases (such as histamine-mediated inflammatory responses) .
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- HY-W013755
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DNOP; Di-n-octyl phthalate; Phthalic acid dioctyl ester
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Biochemical Assay Reagents
Aminotransferases (Transaminases)
Phosphatase
Bacterial
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Inflammation/Immunology
|
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Dioctyl phthalate (DNOP) is a plasticizer. Dioctyl phthalate increases the activities of alanine aminotransferase (ALT) and alkaline phosphatase (ALP) in the liver, as well as the levels of creatinine and urea in the kidney. Exposure to Dioctyl phthalate disrupts the homeostasis of the intestinal microbial community, increases the abundance of pathogenic bacteria, and reduces the abundance of beneficial bacteria such as Lactobacillus. Dioctyl phthalate induces significant and dose-dependent inflammatory responses in the liver, spleen and kidney of mice .
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- HY-108511
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Sigma Receptor
Apoptosis
SARS-CoV
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Infection
Cancer
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PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity .
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- HY-169450
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9-O-Desmethyl mitragynine
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Opioid Receptor
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Neurological Disease
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(-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine), the 9-demethyl analogue of Mitragynine, is a selective and partial agonist of μ-opioid receptor. (-)-9-Hydroxycorynantheidine inhibits electrically stimulated twitch contraction in guinea-pig ileum .
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- HY-P1494
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- HY-P1256C
-
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Neurotensin Receptor
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Neurological Disease
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JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
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- HY-129101
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Eseroline fumarate
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5-HT Receptor
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Neurological Disease
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(-)-Eseroline fumarate is a metabolic of Physostigmine (HY-N6608), an AChE inhibitor. (-)-Eseroline fumarate elicits a leakage of lactic acid dehydrogenase (LDH) from cancer cells. (-)-Eseroline fumarate also induces the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, thus induce cell death. (-)-Eseroline fumarate inhibits the electrically evoked twitches of the mouse vas deferens and of the guinea-pig ileum .
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- HY-101222
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
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- HY-135399
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FXR
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Inflammation/Immunology
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Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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- HY-P3895A
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Neurokinin Receptor
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Neurological Disease
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Substance P (3-11) acetate is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) acetate has contracting activities on guinea pig ileum. Substance P (3-11) acetate also promotes human monocyte chemotaxis .
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- HY-N12520
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Strophanthidin-digitoxoside
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Others
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Metabolic Disease
Cancer
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Helveticoside (Strophanthidin-digitoxoside) is a helveticosid, possesses an ED50 of 0.17 μM for isolated guinea-pig ileum. Helveticoside has anticancer effect .
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- HY-P1714A
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FE 203799 TFA
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GLP Receptor
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Metabolic Disease
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Apraglutide TFA (FE 203799 TFA), a synthetic 33-amino-acid peptide and a long-acting GLP-2 analogue, enhances adaptation and linear intestinal growth in a neonatal piglet model of short bowel syndrome with total resection of the ileum .
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- HY-P3896
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Neurokinin Receptor
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Neurological Disease
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Substance P (2-11) is a substance P (SP) fragment peptide. Substance P (2-11) has contracting activities on guinea pig ileum. Substance P (2-11) inhibits the permeation of 3H SP in BBMEC monolayers .
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- HY-P3895
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Neurokinin Receptor
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Neurological Disease
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Substance P (3-11) is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) has contracting activities on guinea pig ileum. Substance P (3-11) also promotes human monocyte chemotaxis .
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- HY-P1256
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Neurotensin Receptor
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Neurological Disease
|
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JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.15 nM for inhibition of [ 125I]-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
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- HY-141582S
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N-Stearoyl phytosphingosine-d3
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Isotope-Labeled Compounds
Interleukin Related
TNF Receptor
NF-κB
JNK
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Inflammation/Immunology
|
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Ceramide 3-d3 (N-Stearoyl phytosphingosine-d3) is deuterium labeled Ceramide 3. Ceramide 3 is an orally active major component of intercellular lipids in the stratum corneum of the skin, and belongs to the ceramide family. Ceramide 3 inhibits c-jun and NF-κB activation induced by Histamine (HY-B1204), and suppresses the expression of IL-4 and TNF-α. Ceramide 3 inhibits scratching behavior and vascular permeability in mice, and exhibits antihistamine effects in guinea pig ileum. Ceramide 3 improves skin barrier function, reduces transepidermal water loss, erythema and the number of circulating epidermal cells, and accelerates barrier repair of irritated or dysfunctional skin.
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- HY-16094
-
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BW 467C60
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Adrenergic Receptor
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Cardiovascular Disease
Neurological Disease
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Bethanidine sulfate (BW 467C60) is an orally active antihypertensive agent and adrenergic neuron blocker. Bethanidine sulfate exerts its antihypertensive effect by inhibiting the release of norepinephrine from sympathetic nerve terminals. Bethanidine sulfate exhibits anti-ventricular arrhythmic activity. Bethanidine sulfate can be used in research related to hypertension, ventricular tachycardia, and ventricular fibrillation .
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- HY-P10599
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Neurokinin Receptor
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Neurological Disease
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Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guinea pig ileum .
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- HY-120927A
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Opioid Receptor
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Neurological Disease
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Alvimopan metabolite hydrochloride is a peripherally restricted Opioid Receptor antagonist that inhibits the amplitude of electrically evoked contractions and spontaneous mechanical activity in guinea pig ileum .
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- HY-121020
-
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SARS-CoV
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Infection
Others
Inflammation/Immunology
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Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin induces dose-dependent relaxation of ileum and pulmonary artery smooth muscle, causes slight urinary bladder smooth muscle contraction at highest tested concentrations. Arcapillin binds to the active site of SARS-CoV-2 Mpro via interactions with Gln139, His163, and His164, exhibits antiviral activity against SARS-CoV-2 and MERS-CoV. Arcapillin can be used for the research of gastrointestinal disorders, COVID-19, and Middle East respiratory syndrome (MERS) .
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- HY-101946
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Leukotriene Receptor
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Inflammation/Immunology
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AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
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- HY-115763
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3-APPA; CGP 27492; CGA 147823
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GABA Receptor
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Neurological Disease
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3-Aminopropylphosphinic acid (3-APPA) is a phosphonic analog of GABA. 3-Aminopropylphosphinic acid is a potent, selective GABAB receptor agonist .
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- HY-10382
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Angiotensin Receptor
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Cardiovascular Disease
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EXP-6803 is a specific nonpeptide angiotensin II receptor antagonist with antihypertensive activity. EXP-6803 inhibits the contractile response to angiotensin II with a pA2 value of 7.20. EXP-6803 effectively blocks responses to angiotensin I and II while not affecting responses to bradykinin or acetylcholine in guinea pig ileum. EXP-6803 can be used for hypertension research .
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- HY-148038
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5-HT Receptor
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Neurological Disease
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5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice .
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- HY-15048
-
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PARP
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Inflammation/Immunology
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GPI 15427 is a potent inhibitor of the enzyme poly (ADP-ribose) polymerase-1 (PARP-1), which plays a harmful role during inflammation. In a rat model of gut injury and inflammation, including splanchnic artery occlusion (SAO) shock and dinitrobenzene sulfonic acid (DNBS)-induced colitis, GPI 15427 demonstrates strong anti-inflammatory effects that reduces inflammatory cell infiltration, histological injury. GPI 15427 also diminishes the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats .
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- HY-136634
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mAChR
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Others
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BTM-1042 is a newly synthesized compound with antispasmodic effects. It can inhibit the twitch reaction of the guinea pig ileum under electrical stimulation and is not affected by naloxone. It has similar effects to atropine and can block muscarinic receptors, but has less effect on other types of receptors. BTM-1042 also has an inhibitory effect on the ileal reaction caused by nicotine and 5-hydroxytryptamine. BTM-1042 showed a dose-dependent inhibitory effect on the spontaneous movement of the rabbit stomach. In general, BTM-1042 is a agent with a strong antispasmodic effect.
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- HY-111918
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Cholecystokinin Receptor
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Metabolic Disease
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A71378 is a selectivity CCK-A receptor agonist the IC50 values of 0.4 nM, 300 nM, and 1,200 nM for the pancreatic CCK-A, cortical CCK-B, and gastrin receptor, respectively. A71378 elicits pancreatic amylase secretion (EC50 = 0.16 nM) and ileal muscle contraction (EC50 = 3.7 nM) .
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- HY-108511A
-
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Sigma Receptor
Apoptosis
SARS-CoV
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Infection
Cancer
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PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity .
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- HY-103296
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- HY-130138A
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Leukotriene Receptor
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Inflammation/Immunology
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(5S,6R)-DiHETE is an enantiomer of (5,6)-DiHETEs. (5S,6R)-DiHETE can be recognized by leukotriene receptors (LTD4 receptors). (5S,6R)-DiHETE can induce guinea pig isolated ileum contraction with an EC50 of 1.3 μM, and this effect can be inhibited by LTD4 receptor antagonists .
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- HY-113465A
-
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Endogenous Metabolite
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Inflammation/Immunology
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11-trans Leukotriene E4 is an isomer of Leukotriene E4 (LTE4). Slow isomerization of the C-11 double bond of LTE4 leads to the formation of 11-trans LTE4. 11-trans Leukotriene E4 is equipotent to LTE4 in contracting guinea pig ileum .
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- HY-130138B
-
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(5S,6R)-(11E)-DiHETE
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Leukotriene Receptor
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Inflammation/Immunology
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(5S,6R)-DiHETEs is the isomer of (5S,6R)-DiHETE (HY-130138A). (5S,6R)-DiHETE can be recognized by leukotriene receptors (LTD4 receptors). (5S,6R)-DiHETE can induce guinea pig isolated ileum contraction with an EC50 of 1.3 μM, and this effect can be inhibited by LTD4 receptor antagonists .
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- HY-113758
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Leukotriene Receptor
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Inflammation/Immunology
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LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guinea pig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4 .
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- HY-162033
-
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Chloride Channel
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Others
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PAT1inh-A0030 is a selective PAT1 (SLC26A6) inhibitor (IC50= 1.0 μM). PAT1inh-A0030 inhibits fluid absorption in the ileum of wild-type and cystic fibrosis (CF) mice (CftrdelF508/delF508) in a closed-loop model of intestinal fluid absorption. PAT1inh-A0030 can be used in the study of intestinal diseases related to CF .
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- HY-107563
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Histamine Receptor
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Inflammation/Immunology
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ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access .
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- HY-107563A
-
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Histamine Receptor
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Inflammation/Immunology
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ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access .
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- HY-P3809
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Neurokinin Receptor
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Neurological Disease
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[D-Pro2,D-Phe7,D-Trp9] Substance P is a Substance P (HY-P0201) analogue. [D-Pro2,D-Phe7,D-Trp9] Substance P is an inhibitor of Substance P. [D-Pro2,D-Phe7,D-Trp9] Substance P contracts guinea-pig ileum (GPI) indirectly .
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- HY-136831
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QMPB
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Leukotriene Receptor
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Inflammation/Immunology
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SR2640 is a highly efficient and selective LTD4/LTE4 antagonist that can specifically inhibit the smooth muscle contractions induced by LTD4 in the guinea pig ileum and trachea in a concentration-dependent manner, without affecting the contractions caused by histamine. SR2640 can concentration-dependently prevent the binding of 0.4 nM [3H] LTD4 to membrane receptors in guinea pig lung tissue, with an IC50 of 23 nM. SR2640 can shift the dose-response curve for bronchoconstriction induced by intravenous LTD4 in guinea pigs to the right, and the extent of this shift is positively correlated with the dose of SR2640 administered. SR2640 can be used in asthma research .
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- HY-N3136
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Histamine Receptor
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Others
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Onitin is a natural product, that can be isolated from Onychium siliculosum. Onitin is also a non-competitive antagonist of histamine. Onitin shows activity in blocking the peristaltic reflex of the guinea-pig ileum, in inhibition of the responses of guinea-pig ileum to histamine and of inhibition of the responses of guinea-pig tracheal muscle to histamine .
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- HY-U00127
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Drug Derivative
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Neurological Disease
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Pyridazinediones-derivative-1 has potential in treating neurodegenerative disorders. It shows an ED50 of 2.1 μM for inhibiting glutamate-induced contractions of isolated guineapig ileum.
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- HY-P10006
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Opioid Receptor
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Neurological Disease
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Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
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- HY-N8671R
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Reference Standards
Others
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Neurological Disease
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Withanoside V (Standard) is the analytical standard of Withanoside V. This product is intended for research and analytical applications. Withanoside V, a withanolide glycoside, exhibits inhibitory activity for tachyphylaxis to Clonidine in isolated guinea-pig ileum .
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- HY-136947
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nAChR
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Neurological Disease
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RJR-2429 is a nAChR agonist (EC50: 59 nM). RJR-2429 binds with high affinity to α4β2 receptor subtype (Ki = 1 nM). RJR-2429 induces ileum contraction .
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- HY-W747554
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nAChR
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Neurological Disease
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SM 32 is an analgesic. SM 32 produces an increase in ACh release. SM 32 amplifies electrically- and nicotine- evoked guinea-pig ileum contractions. SM32 induces antinociceptive effects through a central cholinergic mechanism .
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- HY-112707
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Cannabinoid Receptor
5-HT Receptor
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Neurological Disease
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AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. AM9405 inhibits twitch contraction of the ileum and the colon with IC50s of 45.71 and 0.076 nM, respectively.
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- HY-135400
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FXR
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Inflammation/Immunology
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Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
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- HY-130432
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nAChR
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Neurological Disease
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DBO-83 dihydrochloride is a brain-penetrant nicotinic acetylcholine receptor (nAChR) agonist. DBO-83 dihydrochloride activates peripheral nicotinic acetylcholine receptors to evoke non-stimulated ileum contractions. DBO-83 dihydrochloride shows antinociceptive and anti-amnesic activities .
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- HY-N0081A
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Calcium Channel
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Cardiovascular Disease
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(-)-Praeruptorin A is a nature product that could be isolated from the roots of Peucedanum praeruptorum Dunn. (-)-Praeruptorin A relaxes ileum and tracheal smooth muscles by activating NO/cGMP signaling pathway. (-)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker .
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- HY-106323
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KW-5139
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Motilin Receptor
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Metabolic Disease
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[Leu13]-Motilin (KW-5139) is a motilin analogue. [Leu13]-Motilin stimulates gastrointestinal motility in the rabbit. [Leu13]-Motilin causes concentration-dependent contractions of the gastric antrum, duodenum, jejunum, ileum and the descending colon in vitro .
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- HY-100724
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Leukotriene Receptor
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Inflammation/Immunology
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YM-17690 is a LTD4 and LTE4 agonist, with a pKi value of 9.28 for [3H]LTD4. It induces dose-dependent contractions in guinea pig ileum, lung parenchyma, and trachea, with EC50 values of 16, 3.9, and 22 nM, respectively. YM-17690 can be used in research related to asthma and inflammation .
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- HY-160932
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Adrenergic Receptor
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Endocrinology
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RS-15385-198 is the enantiomer of Delequamine (RS-15385-197) (HY-106874). RS-15385-198 exhibits a pKi of 6.32 for α2-adrenoceptors in the rat cortex. RS-15385-198 is an antagonist for UK-14304 (HY-B0659) in the rat vas deferens and in the guinea-pig ileum .
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- HY-120915
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mAChR
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Neurological Disease
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L 689660 maleate, a cholinomimetic agent, is a selective M1 and M3 muscarinic receptors agonist. L 689660 maleate is a potent M1 muscarinic receptor full agonist in the rat superior cervical ganglion (pEC50 of 7.3). L 689660 maleate is a potent M3 receptors agonist in the guinea-pig ileum myenteric plexus-longitudinal muscle or in trachea (pEC50 of 7.5 and 7.7, respectively) .
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- HY-167689
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Adrenergic Receptor
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Neurological Disease
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Parethoxycaine hydrochloride is an anesthetic with nerve conduction blocking activity. Parethoxycaine hydrochloride exhibits non-selective inhibitory effects on responses to various stimulants in rat vas deferens and guinea pig ileum muscles. Parethoxycaine hydrochloride has an enhanced effect on the action of norepinephrine, and its methyl bromide derivative also exhibits the same properties on the action of norepinephrine and potassium ions. Derivatives of parethoxycaine hydrochloride have significant effects on calcium dose-response curves, displaying different tissue and stimulant selectivities. The mechanism of action of Parethoxycaine hydrochloride involves the regulation of calcium transport processes .
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- HY-164010
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- HY-W747563
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11-trans LTD4
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Drug Isomer
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Others
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11-trans Leukotriene D4 (11-trans LTD4) is a C-11 double bond isomer of LTD4. LTD4 undergoes slow temperature-dependent isomerization to 11-trans LTD4 during storage. 11-trans LTD4 retains about 10-25 % of the potency for contraction of guinea pig ileum, trachea and parenchyma compared to LTD4. It exhibits an ED50 ranging between 12-60 nM for contraction of guinea pig trachea.
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-
- HY-105572
-
|
MC-838 calcium
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Moveltipril calcium (MC-838 calcium) is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Moveltipril calcium binds via a stable thioester bond and exhibits relative resistance to enzymatic hydrolysis in rat liver homogenate. Moveltipril calcium effectively inhibits ACE extracted from rabbit lung in a concentration-dependent manner. Moveltipril calcium is able to highly specifically inhibit the contractile response to angiotensin-I (AI) in free rat aortic rings and guinea pig ileum preparations, while enhancing the contractile response to calcitonin .
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-
- HY-U00244A
-
|
P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride
|
Adrenergic Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Benzquinamide (P2647; BZQ; Benzoquinamide) hydrochloride is an orally active binder of dopamine receptors and adrenergic receptors. Benzquinamide hydrochloride specifically targets dopamine D2, D3, D4 receptors and α-2A, α-2B, α-2C adrenergic receptors. Benzquinamide hydrochloride regulates blood pressure and heart rate, attenuates the pressor effect of adrenaline, and exhibits activities such as antiemesis, anxiolysis, and reduction of histamine-induced bronchoconstriction. Benzquinamide hydrochloride has good safety and does not deplete serotonin or norepinephrine in the brain. Benzquinamide hydrochloride can be used in studies related to nausea/vomiting, mental disorders, anxiety states, neurosis, and psychosis .
|
-
- HY-N17361
-
|
|
Drug Isomer
|
Endocrinology
|
|
Methylgerambullone is a constitutional isomer of Methylisogerambullone. Methylgerambullone can be isolated from the methanolic leaf extract of Glycosmis angustifolia. Methylgerambullone shows the relaxatory effect on guinea-pig isolated ileum precontracted with Acetylcholine .
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-
- HY-N11727
-
|
|
Drug Derivative
|
Inflammation/Immunology
|
|
Boeravinone F is a Rotenoid derivative. Boeravinone F can be isolated from Boerhaavia diffusa and Boerhavia repens. Boeravinone F inhibits Acetylcholine-induced contraction of isolated guinea pig ileum .
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-
- HY-167129
-
|
|
nAChR
|
Neurological Disease
|
|
DBO-83 free base is a brain-penetrant nicotinic acetylcholine receptor (nAChR) agonist. DBO-83 free base activates peripheral nicotinic acetylcholine receptors to evoke non-stimulated ileum contractions. DBO-83 free base shows antinociceptive and anti-amnesic activities .
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-
- HY-182557
-
|
|
Lipoxygenase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
KC-11404 is an orally active antihistamine and 5-lipoxygenase inhibitor, with an IC50 of 0.9 μM against guinea pig 5-lipoxygenase. KC-11404 inhibits histamine-induced contraction of isolated guinea pig ileum with an IC50 of 0.26 μM. KC-11404 inhibits PAF-induced rabbit platelet aggregation with an IC50 of 2.0 μM. It inhibits the histamine phase of antigen-induced bronchoconstriction and PAF-induced bronchoconstriction in guinea pigs. KC-11404 can be used for the research of asthma .
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-
- HY-120695
-
|
|
Others
|
Neurological Disease
|
|
Nafiverine is an antispasmodic agent. Nafiverine shows a high myolytic activity on the smooth muscles of the ileum, uterus, and coronary vessels .
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-
- HY-182563
-
|
|
Opioid Receptor
|
Endocrinology
|
|
Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide is a μ/δ opioid receptor ligand with high μ opioid receptor selectivity and agonist activity. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide has an IC50 of 237 nM for μ receptors and 1050 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide shows Ki values of 17 nM for μ receptors and 480 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide inhibits electrically evoked contractions of guinea pig ileum and mouse vas deferens. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide serves as a starting compound for structure-activity relationship investigations of μ receptor recognition .
|
-
- HY-182701
-
-
- HY-N9554
-
|
|
Neurokinin Receptor
Endogenous Metabolite
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
WIN-64821 is a secondary metabolite produced by Aspergillus species, and acts as a Neurokinin Receptor antagonist. The Ki values of WIN-64821 for NK1, NK2 and NK3 receptors are 0.24 (human astrocytoma cells), 0.26 (rat duodenum) and 15.2 (guinea pig forebrain) μM, respectively. WIN-64821 inhibits apamin-induced contraction of rat vas deferens, blocks substance P-induced contraction of guinea pig ileum and Ca 2+ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research .
|
-
- HY-182407
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
CV 5975 is an orally active angiotensin converting enzyme (ACE) competitive inhibitor with a rabbit lung ACE IC50 of 3.1 nM and Ki values of 2.6 nM. CV 5975 inhibits ACE in plasma, aorta, kidney, and brain, intensifying inhibition with repeated administration. CV 5975 inhibits Angiotensin I (HY-P1032)-induced pressor responses and ileum contraction, and augments bradykinin-induced ileum contraction and depressor responses. CV 5975 reduces blood pressure via ACE-independent mechanisms, with sustained action across multiple hypertensive and normotensive animal models, intensified by repeated dosing or Hydrochlorothiazide (HY-B0252) co-administration. CV 5975 can be used for the research of hypertension .
|
-
- HY-N18490
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
5α-Cyprinol sulfate is an orally active bile salt and heterospecific pheromone. 5α-Cyprinol sulfate promotes lipid digestion in fish. 5α-Cyprinol sulfate inhibits taurocholic acid uptake mediated by apical bile salt transporters in rat ileum. 5α-Cyprinol sulfate can be used in studies of fish toxic acute renal failure .
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-
- HY-118945
-
|
|
Prostaglandin Receptor
Bradykinin Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
FR191413 is a selective bradykinin B2 receptor agonist that stimulates prostaglandin E2 production in WI-38 cells and activates BK B2 receptor-mediated pathways such as vasodilation and organ protection. FR191413 competitively binds to [ 3H]-BK in guinea pig ileum (GPI) membranes and CHO cells transfected with the human BK B2 receptor, with IC50 values of 20.0 nM and 2.60 nM, respectively. FR191413 can be used in research related to cardiovascular diseases and diabetes, including hypertension, myocardial hypertrophy, myocardial infarction, arrhythmias, and diabetic nephropathy .
|
-
- HY-108511R
-
|
|
Reference Standards
Sigma Receptor
Apoptosis
SARS-CoV
|
Infection
Cancer
|
|
PB28 dihydrochloride (Standard) is the analytical standard of PB28 (dihydrochloride) (HY-108511). This product is intended for research and analytical applications. PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity .
|
-
- HY-N19001
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
(rac)-5-Hydroxykynurenine is a urinary metabolite. (rac)-5-Hydroxykynurenine is generated via indole ring oxidative cleavage of 5-hydroxytryptophan (HY-N0122) catalyzed by indoleamine 2,3-dioxygenase .
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-
- HY-182640
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
SM-11044 is a β-adrenoceptor agonist with Ki values of 18.1 μM (β1), 4.1 μM (β2) and 1.3 μM (β3), showing higher binding selectivity for the β3-adrenoceptor. SM-11044 stimulates cAMP accumulation in cells expressing this receptor. SM-11044 mediates ileal relaxation, tracheal relaxation, pulmonary parenchymal relaxation, increased right atrial heart rate and adipocyte lipolysis .
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-
- HY-P2593
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L-659874 is a selective NK2 receptor antagonist with an IC50 value of 0.49 μM in hamsters. L-659874 inhibits NK2 receptor-mediated hydrolysis of inositol phospholipids. L-659874 could be used for research on the correlation between pain signal transduction and smooth muscle responses. .
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-
- HY-183921
-
|
|
Calcium Channel
|
Cardiovascular Disease
Inflammation/Immunology
|
|
SQ 32547 is a dihydropyridine calcium channel inhibitor with antihypertensive and anti-ischemic activities. SQ 32547 modulates sarcolemmal voltage-dependent calcium channels to inhibit calcium influx, and exerts direct anti-ischemic activity by suppressing myocardial contracture formation and reducing lactate dehydrogenase (LDH) release. SQ 32547 can be used in research related to hypertension, angina pectoris and neurogenic inflammation .
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-
- HY-180401
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
DMP 811 is a potent, orally active and selective angiotensin II subtype receptor AT1 antagonist. DMP 811 exhibits selectivity for AT1 (IC50 = 6 nM) over AT2 (IC50 >10 μM). DMP 811 exhibits potent antihypertensive activity in rats and dogs. DMP 811 can be used for the research of hypertension .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-141582
-
|
N-Stearoyl phytosphingosine
|
Biochemical Assay Reagents
|
|
Ceramide 3 (N-Stearoyl phytosphingosine) is an orally active major component of intercellular lipids in the stratum corneum of the skin, and belongs to the ceramide family. Ceramide 3 inhibits c-jun and NF-κB activation induced by Histamine (HY-B1204), and suppresses the expression of IL-4 and TNF-α. Ceramide 3 inhibits scratching behavior and vascular permeability in mice, and exhibits antihistamine effects in guinea pig ileum. Ceramide 3 improves skin barrier function, reduces transepidermal water loss, erythema and the number of circulating epidermal cells, and accelerates barrier repair of irritated or dysfunctional skin .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1714
-
|
FE 203799
|
GLP Receptor
|
Metabolic Disease
|
|
Apraglutide (FE 203799), a synthetic 33-amino-acid peptide and a long-acting GLP-2 analogue, enhances adaptation and linear intestinal growth in a neonatal piglet model of short bowel syndrome with total resection of the ileum .
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-
- HY-P1494
-
-
- HY-P1256C
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
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-
- HY-P3895A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Substance P (3-11) acetate is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) acetate has contracting activities on guinea pig ileum. Substance P (3-11) acetate also promotes human monocyte chemotaxis .
|
-
- HY-P1714A
-
|
FE 203799 TFA
|
GLP Receptor
|
Metabolic Disease
|
|
Apraglutide TFA (FE 203799 TFA), a synthetic 33-amino-acid peptide and a long-acting GLP-2 analogue, enhances adaptation and linear intestinal growth in a neonatal piglet model of short bowel syndrome with total resection of the ileum .
|
-
- HY-P3896
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Substance P (2-11) is a substance P (SP) fragment peptide. Substance P (2-11) has contracting activities on guinea pig ileum. Substance P (2-11) inhibits the permeation of 3H SP in BBMEC monolayers .
|
-
- HY-P3895
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Substance P (3-11) is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) has contracting activities on guinea pig ileum. Substance P (3-11) also promotes human monocyte chemotaxis .
|
-
- HY-P1256
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.15 nM for inhibition of [ 125I]-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
|
-
- HY-P10599
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guinea pig ileum .
|
-
- HY-P3809
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
[D-Pro2,D-Phe7,D-Trp9] Substance P is a Substance P (HY-P0201) analogue. [D-Pro2,D-Phe7,D-Trp9] Substance P is an inhibitor of Substance P. [D-Pro2,D-Phe7,D-Trp9] Substance P contracts guinea-pig ileum (GPI) indirectly .
|
-
- HY-P10006
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
|
-
- HY-106323
-
|
KW-5139
|
Motilin Receptor
|
Metabolic Disease
|
|
[Leu13]-Motilin (KW-5139) is a motilin analogue. [Leu13]-Motilin stimulates gastrointestinal motility in the rabbit. [Leu13]-Motilin causes concentration-dependent contractions of the gastric antrum, duodenum, jejunum, ileum and the descending colon in vitro .
|
-
- HY-P2593
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L-659874 is a selective NK2 receptor antagonist with an IC50 value of 0.49 μM in hamsters. L-659874 inhibits NK2 receptor-mediated hydrolysis of inositol phospholipids. L-659874 could be used for research on the correlation between pain signal transduction and smooth muscle responses. .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0340
-
|
Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
|
Alkaloids
Structural Classification
Other Alkaloids
Datura metel L.
Solanaceae
Plants
Source Classification
|
mAChR
|
|
Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
|
-
-
- HY-N12520
-
-
-
- HY-121020
-
|
|
Structural Classification
Flavonoids
Flavones
Plants
Compositae
Artemisia capillaris Thunb.
Source Classification
|
SARS-CoV
|
|
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin induces dose-dependent relaxation of ileum and pulmonary artery smooth muscle, causes slight urinary bladder smooth muscle contraction at highest tested concentrations. Arcapillin binds to the active site of SARS-CoV-2 Mpro via interactions with Gln139, His163, and His164, exhibits antiviral activity against SARS-CoV-2 and MERS-CoV. Arcapillin can be used for the research of gastrointestinal disorders, COVID-19, and Middle East respiratory syndrome (MERS) .
|
-
-
- HY-113465A
-
-
-
- HY-N3136
-
-
-
- HY-N8671R
-
-
-
- HY-N0081A
-
-
-
- HY-N17361
-
-
-
- HY-N11727
-
-
-
- HY-N9554
-
-
-
- HY-N18490
-
|
|
Structural Classification
Animals
Steroids
Source Classification
|
Drug Derivative
|
|
5α-Cyprinol sulfate is an orally active bile salt and heterospecific pheromone. 5α-Cyprinol sulfate promotes lipid digestion in fish. 5α-Cyprinol sulfate inhibits taurocholic acid uptake mediated by apical bile salt transporters in rat ileum. 5α-Cyprinol sulfate can be used in studies of fish toxic acute renal failure .
|
-
-
- HY-N19001
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-141582S
-
|
|
|
Ceramide 3-d3 (N-Stearoyl phytosphingosine-d3) is deuterium labeled Ceramide 3. Ceramide 3 is an orally active major component of intercellular lipids in the stratum corneum of the skin, and belongs to the ceramide family. Ceramide 3 inhibits c-jun and NF-κB activation induced by Histamine (HY-B1204), and suppresses the expression of IL-4 and TNF-α. Ceramide 3 inhibits scratching behavior and vascular permeability in mice, and exhibits antihistamine effects in guinea pig ileum. Ceramide 3 improves skin barrier function, reduces transepidermal water loss, erythema and the number of circulating epidermal cells, and accelerates barrier repair of irritated or dysfunctional skin.
|
-
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