Search Result
Results for "
oral+administration
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-100897
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Thrombin
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Cardiovascular Disease
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Sulodexide is a mixture of glycosaminoglycans available in soft capsule form for oral administration. It is composed of low molecular weight heparin (80%) and dermatan sulfate (20%). Sulodexide exhibits antithrombotic activity through interaction with antithrombin III (AT III) and heparin cofactor II (HC II), and inhibition of thrombin formation. Sulodexide exhibits profibrinolytic activity through release of tissue plasminogen activator (tPA). Sulodexide exhibits endothelial protective and anti-inflammatory effect, ameliorates chronic venous disease .
Sulodexide is a glycosaminoglycan mixture available in soft gelatin capsule form for oral administration.
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- HY-N6641
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Keap1-Nrf2
PPAR
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Inflammation/Immunology
Cancer
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Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist .
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- HY-16100
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Fatty Acid Synthase (FASN)
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Metabolic Disease
Cancer
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BI 99179, a chemical probe, is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats .
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- HY-118189
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Prostaglandin Receptor
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Inflammation/Immunology
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Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers . Misoprostol is an oral agent used to induce labor .
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- HY-100634
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(±)-4-hydroxy Propranolol hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
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4-Hydroxypropranolol hydrochloride is a non-cardiac selective β-adrenergic receptor antagonist and a metabolite produced after oral administration of Propranolol (HY-B0573B). 4-Hydroxypropranolol hydrochloride also acts as a membrane stabilizer and possesses intrinsic sympathomimetic inhibitory activity. 4-Hydroxypropranolol hydrochloride blocks β-adrenergic receptors to antagonize the effects of catecholamines, acts as a partial β-adrenergic receptor agonist, and induces membrane stabilization. 4-Hydroxypropranolol hydrochloride alters heart rate, left ventricular contractility, and atrioventricular conduction time. 4-Hydroxypropranolol hydrochloride can be used in research related to cardiovascular and cerebrovascular diseases .
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- HY-Y0850U3
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Polyvinyl alcohol (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization); Poly(Ethenol) (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization)
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Biochemical Assay Reagents
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Others
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PVA (Polyvinyl alcohol) (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) is a water-soluble, biodegradable, biocompatible and non-immunogenic polymer. PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) causes no irritation to rabbit eyes, no skin sensitization in guinea pigs, promotes the proliferation of human skin keratinocytes, and reduces the loss of corneal endothelial cells. The LD50 of PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) in rats and dogs is greater than 10 g/kg. PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) is hardly absorbed by the digestive system, causes no adverse effects upon long-term oral administration, and shows no mutagenicity or carcinogenicity. However, repeated intravenous or portal vein injection of PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) may induce pathological changes such as glomerular lesions, anemia, hypertension or liver fibrosis in rats or dogs. Crosslinked nanofibers prepared by modifying PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) can be used in studies related to wound dressings and other applications .
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- HY-164782
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HDAC
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Neurological Disease
Metabolic Disease
Cancer
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PT3 is a selective inhibitor of HDAC3 with an IC50 value of 0.25 μM. PT3 exhibits good brain penetration ability and bioavailability upon oral administration. PT3 can be used in the research of Alzheimer’s disease .
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- HY-W013762
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Environmental Pollutants
Biochemical Assay Reagents
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Others
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Tributyl citrate is a low-toxicity and orally active citrate ester with no genotoxicity or skin sensitizing activity. Tributyl citrate also acts as a plasticizer, solvent, FDA-approved indirect food additive, and topical anesthetic, among other uses. Tributyl citrate induces a needle-prick insensitivity response that lasts for more than 2 hours, and a 5% suspension of it temporarily eliminates the corneal reflex in rabbits. Tributyl citrate causes no significant systemic toxicity in rats and cats at most tested doses, and only may cause growth retardation and gastrointestinal reactions such as diarrhea and nausea at high doses or with repeated oral administration .
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- HY-N0856
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23-O-Acetylalisol C; Alisol C monoacetate
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Others
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Cardiovascular Disease
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Alisol C 23-acetate, a natural product extracted from Alisma orinentale, can significantly and strongly inhibit DTH response after oral administration.
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- HY-W011309
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1-O-HDG; HXDG
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PPAR
PGE synthase
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Inflammation/Immunology
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1-O-Hexadecylglycerol can up-regulate PPAR-γ expression, inhibit pGE2, and exhibit anti-inflammatory properties . 1-O-Hexadecylglycerol is effective in oral administration .
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- HY-A0234
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Prostenoglycine; TTPG; Tiase
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Chloride Channel
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Endocrinology
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Stepronin (Prostenoglycine) is an orally active expectorant (inhalation administration is preferable to oral administration). Stepronin inhibits airway secretion in vitro by reducing Cl - secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands .
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- HY-108288
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Pivsulbactam; CP 47904
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Beta-lactamase
Antibiotic
Bacterial
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Infection
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Sulbactam pivoxil (Pivsulbactam) is a prodrug of Sulbactam (HY-B0334) with oral activity. Sulbactam is a β-lactamase inhibitor with antibacterial activity. Sulbactam pivoxil is better absorbed than Sulbactam and results in higher serum levels after oral administration .
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- HY-14826
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AVE8112
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Phosphodiesterase (PDE)
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Neurological Disease
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Tilivapram (AVE8112) is an orally active PDE4 inhibitor with procognitive effects. Tilivapram exhibits in vivo efficacy and improves processing speed and psychomotor speed. Oral administration of tilivapram may induce dose-related adverse reactions such as nausea and dizziness, but transdermal delivery enables slow, controlled elevation of plasma concentrations, thereby significantly reducing gastrointestinal discomfort and dizziness. Tilivapram is applicable to research related to neuropsychiatric disorders .
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- HY-N2620
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Cytochrome P450
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Infection
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Rutaevin is an antifungal toxin and CYP3A4 inactivator. Rutaevin requires NADPH-dependent bioactivation to generate cis-but-2-ene-1,4-dial, which then covalently modifies and mechanism-based inactivates human CYP3A4 (IC50=4.48 μM, Ki=15.98 μM), and interacts with substances such as glutathione. Rutaevin disrupts the cellular structure of Sirococcus conigenus, accumulates linearly in resistant larch after pathogen exposure, and induces liver toxicity in mice via oral administration. Rutaevin can be applied to research in fields related to larch shoot blight and other associated areas .
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- HY-N10225
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Prostaglandin Receptor
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Cardiovascular Disease
Endocrinology
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Thielavin A is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin A specifically inhibits the conversion of arachidonic acid into prostaglandin H2. Thielavin A has no anti-inflammatory activity on intravenous injection or on oral administration .
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- HY-100085
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21-desDFZ
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Drug Metabolite
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Inflammation/Immunology
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21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
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- HY-167840
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PD-1/PD-L1
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Neurological Disease
Cancer
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IMMH-010 maleate is a prodrug that serves as a novel PD-L1 inhibitor, exhibiting potential antitumor activity for the treatment of neurological disorders and advanced malignant solid tumors. IMMH-010 maleate is rapidly converted to its active form, YPD-29B, following oral administration. IMMH-010 maleate is poised for advancing research in the field of PD-L1 inhibitors and related therapeutic applications.
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- HY-101122
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SGLT
GLP Receptor
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Metabolic Disease
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LX2761 is an orally active, dual SGLT1/SGLT2 inhibitor with IC50 values of 2.2 nM and 2.7 nM against human SGLT1 and SGLT2, respectively. LX2761 locks human SGLT1 in an outward-open conformation and blocks its putative water permeation pathway. After oral administration, LX2761 is confined exclusively to the intestinal lumen, delays intestinal glucose absorption, regulates intestinal glucose metabolism, increases cecal glucose levels, reduces cecal pH, improves glycemic control and elevates plasma total GLP-1 levels. However, LX2761 induces diarrhea in a dose-dependent manner. LX2761 can be used in diabetes-related research .
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- HY-W276164
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Sodium stearyl sulfate
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Biochemical Assay Reagents
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Others
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Sodium octadecyl sulfate (Sodium stearyl sulfate) is a long-chain alkyl sodium sulfate that functions as an emulsifier, crosslinking agent, and regulator. Sodium octadecyl sulfate has high safety, with a LD50 greater than 3.00 Gm./Kg for both intraperitoneal injection in mice and oral administration in rats. Sodium octadecyl sulfate enhances continuous contraction of the gastrocnemius muscle in frogs and boosts intestinal smooth muscle activity in albino rats. However, Sodium octadecyl sulfate exerts no significant effect on isolated tortoise myocardium and does not alter the conduction function of frog sciatic nerves. Sodium octadecyl sulfate can also be used to coat the surface of starch aggregates, promote crosslinking and increase aggregate size through hydrophobic and electrostatic interactions, and further form a coexistent B-V type crystalline structure with acid-hydrolyzed gelatinized starch, thereby effectively modifying the structure and surface properties of high-starch systems .
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- HY-145461
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5-Hydroxy lenalidomide
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Drug Metabolite
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Others
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Hydroxy lenalidomide (5-Hydroxy lenalidomide) is a metabolite of lenalidomide that is present as a minor component in plasma and excreta, accounting for less than 5% of the total radioactivity, following oral administration of lenalidomide in healthy male subjects.
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- HY-N4173
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Drug Metabolite
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Metabolic Disease
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8-Oxoepiberberine is an alkaloid metabolite in the plasma after oral administration of Zuojin formula, a traditional chinese medicine used to treat gastrointestinal disease .
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- HY-118426
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(Rac)-IND 58359; (Rac)-R115777
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Farnesyl Transferase
Ras
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Cancer
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(Rac)-Tipifarnib ((Rac)-IND 58359; (Rac)-R115777) is a potent farnesyl protein transferase inhibitor that specifically targets the pro-tailation process of Ras proteins. (Rac)-Tipifarnib showed significant in vivo antitumor effects after oral administration to mice .
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- HY-U00122
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- HY-N14880
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Antibiotic
Bacterial
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Infection
Cardiovascular Disease
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Oudenone is an oxygen-containing heterocyclic antibiotic. Oudenone has weak antibacterial and fungal activity. Oudenone has antihypertensive effect on spontaneous hypertension in rats by intraperitoneal injection or oral administration .
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- HY-123186
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RG-7348
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HCV
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Infection
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MB-11362 is an orally active, selective HCV NS5B polymerase inhibitor and 4′-azidouridine triphosphate prodrug. MB-11362 can be converted to 4′-azidouridine triphosphate after oral administration. MB-11362 can be used in the research of HCV infection .
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- HY-105215
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Neurokinin Receptor
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Inflammation/Immunology
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FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration .
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- HY-159489
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SHP2
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Cancer
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SDUY038 is a SHP2 allosteric inhibitor, with an IC50 of 1.2 μM and KD of 0.29 μM, respectively. SDUY038 exhibits pan-antitumor activity (IC50 = 7-24 μM) by suppressing pERK expression. SDUY038 exhibits t1/2 of 3.95 h by oral administration .
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- HY-12096
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GnRH Receptor
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Endocrinology
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WAY-207024 is an orally active gonadotropin releasing hormone receptor (GnRH-R) antagonist (human GnRH: IC50 of 12 nM, rat GnRH: IC50 of 71 nM). WAY-207024 inhibits rat LH release with an IC50 of 350 nM. WAY-207024 lowers rat plasma leuteinizing hormone (LH) levels after oral administration .
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- HY-111073
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Y101
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HBV
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Infection
Inflammation/Immunology
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Bentysrepinine (Y101) is an orally active HBV inhibitor with anti-hepatitis B virus infection activity. Bentysrepinine exhibits favorable pharmacokinetic characteristics, with absolute bioavailability of 44.9%, 43.1%, and 19.2% in rats, dogs, and monkeys, respectively, and it does not accumulate in monkeys after 90 days of oral administration. Bentysrepinine is under research in the antiviral and hepatitis fields .
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- HY-108288R
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Pivsulbactam (Standard); CP 47904 (Standard)
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Beta-lactamase
Reference Standards
Antibiotic
Bacterial
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Infection
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Sulbactam pivoxil (Standard) (Pivsulbactam (Standard)) is the analytical standard of Sulbactam pivoxil (HY-108288). This product is intended for research and analytical applications. Sulbactam pivoxil (Pivsulbactam) is a prodrug of Sulbactam (HY-B0334) with oral activity. Sulbactam is a β-lactamase inhibitor with antibacterial activity. Sulbactam pivoxil is better absorbed than Sulbactam and results in higher serum levels after oral administration .
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- HY-107129
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GCGR
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Metabolic Disease
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MK-3577 is an orally effective glucagon receptor (GCGR) antagonist that reduces hepatic glucose production and lowers blood glucose levels by blocking glucagon receptors on target organs, primarily the liver. Pharmacokinetic analysis in domestic cats indicates that MK-3577 reaches peak levels 3 to 4 hours after oral administration, with a half-life of approximately 15 hours. MK-3577 can be used in diabetes research .
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- HY-129756
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N-Phenylthioacetamide
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Biochemical Assay Reagents
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Metabolic Disease
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Thioacetanilide (N-Phenylthioacetamide) is a sulfur-containing thioamide derivative of acetanilide. Thioacetanilide displays a solvent‑dependent Z/E isomeric distribution, preferring the E conformation in polar hydrogen‑bonding solvents and the Z conformation in halogenated solvents. Thioacetanilide serves as a substrate for metabolic desulfurization and aromatic hydroxylation. Thioacetanilide is mainly metabolized via desulfurization and 4‑hydroxylation of the aromatic ring in Rattus norvegicus, and the released sulfur integrates into the total body sulfur pool. Thioacetanilide is well absorbed in rats, and more than 90% of the dose is excreted in urine as conjugated metabolites after oral administration .
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- HY-14977
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LPL Receptor
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Inflammation/Immunology
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CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
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- HY-126835
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Amino Acid Derivatives
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Cancer
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A 924 is an amino acid derivative-based, orally active antitumor agent. A 924 is effective in inhibiting ascites tumors in rat models by intraperitoneal injection or oral administration. The LD50 of A 924 in mice is >1.5 g/kg and >4.5 g/kg by intraperitoneal injection or oral administration, respectively. A 924 does not cause teratogenicity or adverse reactions in normal or pregnant mice .
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- HY-W031110
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- HY-W740380
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Drug Metabolite
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Others
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21-Carboxylic acid triamcinolone acetonide is a metabolite produced in the body after oral administration of [14C]-triamcinolone acetonide .
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- HY-122307
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DAN-603
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Bacterial
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Metabolic Disease
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Sulisatin (DAN-603) is an anionic laxative that is hydrolyzed to diphenolic derivatives by bacterial aryl sulfate sulfohydrolases in the colon during oral administration .
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- HY-120639
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HIV
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Others
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BMS-663749 lysine is a prodrug of an HIV-1 attachment inhibitor with the potential to enhance the delivery of the parent compound following oral administration.
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- HY-135245
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SCH 488128; Ezetimibe hydroxy β-D-Glucuronide
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Drug Metabolite
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Cardiovascular Disease
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Ezetimibe hydroxy glucuronide (SCH 488128) is a trace metabolite detected in dog and human plasma samples after oral administration of Ezetimibe (HY-17376) .
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- HY-129579
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Histamine Receptor
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Others
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Linadryl is a compound with antihistamine and other effects. It has a variable effect on gastric acid secretion after oral administration, and its effect is about half that of Diphenhydramine (HY-B0303).
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- HY-122307A
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DAN-603 disodium
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Bacterial
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Metabolic Disease
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Sulisatin (DAN-603) disodium is an anionic diarrhea-promoting compound. During oral administration, Sulisatin disodium is hydrolyzed to diphenolic derivatives by bacterial aryl sulfate sulfohydrolases in the colon .
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- HY-169199
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MAP4K
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Cancer
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BAY-405 (compund 38) is a MAP4K1 inhibitor that exhibits nanomolar potency in biochemical and cellular assays and achieves in vivo exposure after oral administration .
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- HY-102061
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ATI 7505 dihydrochloride
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Others
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Others
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Naronapride (dihydrochloride) (ATI 7505 (dihydrochloride)) is a compound that regulates gastrointestinal motility. It is a 5-HT receptor agonist. It is extensively metabolized after oral administration and is mainly excreted through feces. It has certain pharmacokinetic properties.
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- HY-19899
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Histamine Receptor
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Neurological Disease
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APD-916 is an H3 receptor antagonist. APD-916 shows good pharmacokinetic properties, and oral administration of APD-916 has been shown to enhance wakefulness in various animal models .
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- HY-105919
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Factor Xa
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Cardiovascular Disease
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Naroparcil is an orally active antithrombotic agent. Naroparcil exhibits antithrombotic effects in rabbit Wessler stasis model with EC50s of 21.9 mg/kg and 36.0 mg/kg after respectively intravenous injection and oral administration .
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- HY-149900
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Biochemical Assay Reagents
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Infection
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Antiviral agent 33 (compound 1c) is a double-stranded DNA (dsDNA) virus inhibitor with IC50 values of 0.0790 and 0.1572 µM for VACV and AdV5, respectively. Antiviral agent 33 also has potential for oral administration .
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- HY-147152
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Biochemical Assay Reagents
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Others
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1-Myristoyl-3-chloropropanediol is a 3-monochloropropanediol (3-MCPD) fatty acid ester. 3-MPCD causes nephropathy and tubular hyperplasia and adenomas by chronic oral administration; also reduces fertility, or provokes infertility in rats and suppresses the immune function .
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- HY-105498
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Sodium Channel
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Neurological Disease
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ADD-196022 is an orally active antiepileptic and anticonvulsant agent. ADD-196022 shows ED50 values of 26.2 mg/kg and 5.79 mg/kg for intraperitoneal injection in mice and orally administration in rats. ADD-196022 can be used for the research of neurological disease .
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- HY-162893
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Glycosidase
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Metabolic Disease
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SX29 is an orally active non-competitive α-glucosidase inhibitor with an IC50 value of 2.12 μM. SX29 exhibits hypoglycemic activity, and oral administration of SX29 can reduce blood glucose levels and improve glucose tolerance in diabetic mice .
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- HY-A0234R
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Prostenoglycine (Standard); TTPG (Standard); Tiase (Standard)
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Chloride Channel
Reference Standards
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Endocrinology
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Stepronin (Standard) is the analytical standard of Stepronin. This product is intended for research and analytical applications. Stepronin (Prostenoglycine) is an orally active expectorant (inhalation administration is preferable to oral administration). Stepronin inhibits airway secretion in vitro by reducing Cl - secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands .
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- HY-118543
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HIF/HIF Prolyl-Hydroxylase
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Cardiovascular Disease
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TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. Local administration of TM6089 enhances angiogenesis, and oral administration stimulates HIF activity in transgenic rats expressing a hypoxia-responsive reporter vector .
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- HY-144110
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HCV
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Infection
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HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage .
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- HY-12096A
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GnRH Receptor
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Cardiovascular Disease
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WAY-207024 dihydrochloride is an orally active gonadotropin releasing hormone receptor (GnRH-R) antagonist (human GnRH: IC50 of 12 nM, rat GnRH: IC50 of 71 nM). WAY-207024 dihydrochloride inhibits rat LH release with an IC50 of 350 nM. WAY-207024 dihydrochloride lowers rat plasma leuteinizing hormone (LH) levels after oral administration .
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- HY-126230
-
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Endogenous Metabolite
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Others
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PAT-494 is an ATX inhibitor with significant activity in biochemical and plasma assays. PAT-494 can reduce LPA levels in rat plasma through oral administration. The structure-activity relationship study of PAT-494 shows that its binding mode with ATX is novel and it can effectively occupy the hydrophobic pockets and channels of ATX .
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- HY-163483
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Parasite
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Others
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ELQ-598, as a prodrug, is converted into the active drug ELQ-596 upon oral administration. ELQ-598 demonstrates potent parasitic growth inhibition capabilities (IC50= 37 nM). ELQ-598 also shows low toxicity towards human cells (IC50= 19 μM). ELQ-598 can be used for research into babesiosis .
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- HY-100085R
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21-desDFZ (Standard)
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Drug Metabolite
Reference Standards
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Inflammation/Immunology
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21-Desacetyldeflazacort (Standard) is the analytical standard of 21-Desacetyldeflazacort. This product is intended for research and analytical applications. 21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
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- HY-103459
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PD156707
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Endothelin Receptor
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Cardiovascular Disease
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CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration .
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- HY-N6641R
-
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Reference Standards
Keap1-Nrf2
PPAR
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Inflammation/Immunology
Cancer
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Monascin (Standard) is the analytical standard of Monascin. This product is intended for research and analytical applications. Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist .
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- HY-170961
-
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Aminopeptidase
Neprilysin
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Neurological Disease
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SDUY816 is an oral active dual APN/NEP inhibitor, with IC50 values of 0.68 μM for APN and 6.9 μM for NEP. SDUY816 exhibits analgesic effects and demonstrates good safety and pharmacokinetic profiles, with an oral bioavailability of 27% and a half-life of 4.02 hours in rats (oral administration, 10 mg/kg). SDUY816 has potential applications in the research of neuropathic pain disorders .
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- HY-W758934
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Prostenoglycine-d5; TTPG-d5; Tiase-d5
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Isotope-Labeled Compounds
Chloride Channel
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Endocrinology
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Stepronin-d5 (Prostenoglycine-d5; TTPG-d5; Tiase-d5) is the deuterium labeled Stepronin (HY-A0234). Stepronin (Prostenoglycine) is an orally active expectorant (inhalation administration is preferable to oral administration). Stepronin inhibits airway secretion in vitro by reducing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands .
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- HY-118189S
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Isotope-Labeled Compounds
Prostaglandin Receptor
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Inflammation/Immunology
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Misoprostol acid-d5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers . Misoprostol is an oral agent used to induce labor .
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- HY-117913
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Renin
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Cardiovascular Disease
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ES-8891 is a renin inhibitor. Oral administration of ES-8891 to normotensive sodium-depleted macaques for one week significantly reduced plasma renin activity, immunoreactive renin concentrations, and plasma angiotensin I concentrations, while mean blood pressure decreased significantly, without significant changes in heart rate. ES-8891 regulates blood pressure by inhibiting plasma renin levels and renal renin synthesis .
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- HY-W759719
-
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21-desDFZ-d4
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Isotope-Labeled Compounds
Drug Metabolite
|
Inflammation/Immunology
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21-Desacetyldeflazacort-d4 (21-desDFZ-d4) is the deuterium labeled 21-Desacetyldeflazacort (HY-100085). 21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
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- HY-146012
-
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HIV
|
Infection
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HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a proagent of atazanavir. HIV-1 protease-IN-4 as a proagent that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent agent .
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- HY-14795
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ZT-1
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Cholinesterase (ChE)
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Neurological Disease
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Mimopezil (ZT-1) is an cholinesterase (ChE) inhibitor that rapidly degrades into the active metabolite Huperzine A (HY-17388) in water or aqueous organic solvents. After oral administration, Mimopezil is rapidly absorbed but has low bioavailability (0.37%) in rats. However, after metabolism, it is converted into Huperzine A, which accumulates in the blood and exhibits strong activity. Following intravenous administration, Mimopezil reaches higher blood concentrations and is also rapidly metabolized into Huperzine A .
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- HY-116790B
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(Rac)-Penbutolol; (±)-Isopenbutolol
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Adrenergic Receptor
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Cardiovascular Disease
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(±)-Penbutolol ((Rac)-Penbutolol) is the racemic mixture of Penbutolol. (±)-Penbutolol is an orally active β-adrenergic receptor antagonist. (±)-Penbutolol antagonizes exercise-induced tachycardia, reduces the increase in peak expiratory flow rate (PEFR) caused by exercise, and decreases resting plasma renin activity (PRA). (±)-Penbutolol reaches peak plasma concentration 1 hour after oral administration, with a half-life of 4.5 hours, and is converted into an active metabolite in the body. (±)-Penbutolol can be used in cardiovascular-related disease research .
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- HY-119221A
-
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LPL Receptor
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Neurological Disease
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AUY 954 hydrochloride is a potent and selective sphingosine-1-phosphate (S1P(1)) receptor agonist, exhibiting significant immunomodulatory activity. AUY 954 hydrochloride induces a profound and reversible reduction of circulating lymphocytes upon oral administration. AUY 954 hydrochloride has demonstrated efficacy in prolonging cardiac allograft survival when used in combination with RAD001 in a stringent transplantation model. AUY 954 hydrochloride effectively prevents experimental autoimmune neuritis in rats, showcasing its therapeutic potential in autoimmune conditions.
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- HY-163983
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Microtubule/Tubulin
Apoptosis
PARP
Caspase
|
Cancer
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Tubulin polymerization-IN-68 (compound 32) is a tubulin inhibitor that can inhibit tubulin polymerization and destroy the cellular microtubule network. Tubulin polymerization-IN-68 can upregulate the expression of PARP-1 and caspase-3 and induce cell apoptosis, and has anticancer activity. Tubulin polymerization-IN-68 can effectively inhibit HepG2 (IC50=93 nM) and significantly inhibit the growth of HepG2 xenograft tumors in nude mice by oral administration .
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- HY-172148
-
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Interleukin Related
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Inflammation/Immunology
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Itaconic acid prodrug-1 (Compound P2) is an orally active prodrug of Itaconic acid (HY-Y0520) that efficiently delivers the active ingredient Itaconic acid to skin tissue following oral administration. Itaconic acid prodrug-1 possesses immunomodulatory properties, significantly inhibiting Poly(I:C)/IFNγ-induced inflammatory cytokines in human epidermal keratinocytes. Itaconic acid prodrug-1 can be utilized for the research of alopecia areata and other inflammatory skin diseases .
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- HY-W328882
-
|
|
Endogenous Metabolite
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Cardiovascular Disease
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|
3-(2-Aminopropyl)phenol is a biologically active compound with significant blood pressure-raising activity. 3-(2-Aminopropyl)phenol can effectively improve the symptoms of orthostatic hypotension in patients. 3-(2-Aminopropyl)phenol can significantly increase blood pressure at rest and when standing after oral administration. 3-(2-Aminopropyl)phenol can help reduce pathological orthostatic adjustment disorders. 3-(2-Aminopropyl)phenol has a relatively small effect on heart rate, and no significant side effects have been observed .
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- HY-15042
-
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Bradykinin Receptor
|
Metabolic Disease
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MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
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- HY-W013762R
-
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Reference Standards
Biochemical Assay Reagents
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Others
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Tributyl citrate (Standard) is the analytical standard of Tributyl citrate. This product is intended for research and analytical applications. Tributyl citrate is a low-toxicity and orally active citrate ester with no genotoxicity or skin sensitizing activity. Tributyl citrate also acts as a plasticizer, solvent, FDA-approved indirect food additive, and topical anesthetic, among other uses. Tributyl citrate induces a needle-prick insensitivity response that lasts for more than 2 hours, and a 5% suspension of it temporarily eliminates the corneal reflex in rabbits. Tributyl citrate causes no significant systemic toxicity in rats and cats at most tested doses, and only may cause growth retardation and gastrointestinal reactions such as diarrhea and nausea at high doses or with repeated oral administration .
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- HY-118243
-
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Amyloid-β
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Others
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KMS88009 is a potent small molecule that directly interferes with the formation of amyloid-β oligomers, thereby preserving cognitive behavior when used preventively and reversing cognitive behavior decline when used therapeutically. Oral administration of KMS88009 around the onset of Alzheimer's disease symptoms significantly reduced the assembly of amyloid-β oligomers and improved cognitive behavior in the APP/PS1 double transgenic mouse model. This unique dual mode of action suggests that KMS88009 may be a powerful therapeutic candidate for the treatment of Alzheimer's disease. In an evaluation, the physicochemical properties, pharmacokinetics and toxicity of this anti-amyloidogenic small molecule KMS88009 were studied, as well as post-mortem analysis of APP/PS1 TG mice after behavioral testing.
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- HY-139124
-
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15(R)-Carboprost; 15(R)-15-methyl PGF2α
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Prostaglandin Receptor
|
Metabolic Disease
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15(R)-15-Methyl Prostaglandin F2α (15(R)-Carboprost; 15(R)-15-methyl PGF2α) is a metabolically stable analog of PGF2α. 15(R)-15-Methyl Prostaglandin F2α is an inactive, prodrug PGF agonist designed for activation by gastric acid after oral administration. Acid-catalyzed epimerization of 15(R)-15-Methyl Prostaglandin F2α converts it into the active 15(S)-isomer. The 15(S)-isomer induces luteolysis when injected in rhesus monkeys at a dose of about 12 mg/animal, while the 15(R)-isomer does not.
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- HY-159922
-
|
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Androgen Receptor
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Cancer
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AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
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- HY-13590
-
|
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VEGFR
|
Cancer
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CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
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- HY-118683
-
|
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Potassium Channel
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Others
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|
KR-31378 is a neuroprotectant with dose-dependent pharmacokinetic properties and relevant activity in rats. After intravenous and oral administration of KR-31378 in rats, its pharmacokinetic parameters showed dose-dependent changes, such as decreased clearance with increasing doses, good oral absorption, and comparable AUCs for intravenous and oral administration at different doses.
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- HY-W721612
-
|
|
Drug Metabolite
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Cancer
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|
Bromobric acid is a derivative of bromoacrylic acid with cytostatic and antineoplastic activity that can form ionic complexes with glucosamine to achieve controlled-release oral administration
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-
- HY-W026747
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|
|
Drug Derivative
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Others
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|
Isobutyl salicylate is an irritant substance, an ester formed from salicylic acid and isobutanol, which serves as a flavor and fragrance additive. The median lethal dose (LD50) of Isobutyl salicylate via oral administration in rats is 1560 mg/kg.
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- HY-N18296
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|
|
Drug Derivative
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Others
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Karelinine is a steroidal alkaloid found in the bulbs of Fritillaria ussuriensis Maxim and Fritillaria karelinii. Karelinine shows accelerated absorption and elimination rates, and increased area under the curve (AUC0-t) when administered as part of the nanodispersion preparation (FUN) in rat plasma following oral administration .
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- HY-182365
-
|
|
Histone Demethylase
|
Neurological Disease
Inflammation/Immunology
|
|
EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC50=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis .
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-
- HY-124185
-
|
|
Others
|
Others
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|
LC 6 is an anti-allergic compound that has the activity of inhibiting passive cutaneous allergic reactions in rats. Its half effective dose (ED50) is 35 mg/kg body weight. Oral administration is effective and long-lasting, and the effect is obviously dose-dependent. Its long-term binding to mast cells makes it a valuable tool for studying allergic reaction receptors.
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-
- HY-N18029
-
|
|
Drug Derivative
|
Inflammation/Immunology
Cancer
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(24S)-Ginsenoside V is a monooxygenated derivative of Ginsenoside Rb1 (HY-N0039). (24S)-Ginsenoside V is the major circulating metabolite of Ginsenoside Rb1 in rat plasma. (24S)-Ginsenoside V appears in rat urine after intravenous and oral administration of Ginsenoside Rb1 to rats .
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-
- HY-126230A
-
|
|
Endogenous Metabolite
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Cancer
|
|
(Rac)-PAT-494 is a type II autotaxin inhibitor with the activity of inhibiting the production of lysophosphatidic acid (LPA) in the blood. (Rac)-PAT-494 can participate in the inhibition of diseases related to cancer, fibrosis and inflammation by antagonizing the function of autotaxin. (Rac)-PAT-494 shows high activity in biochemical and plasma tests. (Rac)-PAT-494 can reduce plasma LPA levels after oral administration to rats .
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-
- HY-16622B
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
GSK 1842799 hydrochloride is a selective S1P1 receptor agonist with potent agonist activity and exceptional selectivity over S1P3. GSK 1842799 hydrochloride demonstrates good oral bioavailability and rapid conversion to its active phosphorylated form. GSK 1842799 hydrochloride significantly reduces blood lymphocyte counts in vivo following oral administration. GSK 1842799 hydrochloride has shown efficacy comparable to FTY720 in the mouse EAE model of multiple sclerosis.
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-
- HY-181558
-
|
|
Others
|
Cancer
|
|
Anticancer agent 303 is a selective, orally active anticancer agent belonging to the pyrazolopyridine derivatives. Anticancer agent 303 exhibits low cytotoxicity to healthy cells, with a selective window of approximately 2-fold between cancer cells and healthy cells. Anticancer agent 303 produces detectable systemic exposure in mice following intraperitoneal or oral administration. Anticancer agent 303 effectively inhibits the proliferation of prostate cancer and breast cancer cells .
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-
- HY-18157
-
|
|
Amyloid-β
|
Neurological Disease
|
|
SCH 900229 is a potent γ-secretase inhibitor with selective activity against PS1. The Aβ40 IC50 value of SCH 900229 is 1.3 nM, showing its excellent ability in reducing Aβ. SCH 900229 has shown good Aβ-lowering effects after oral administration in preclinical animal models. SCH 900229 has been advanced to human clinical trials for further development of compounds for the inhibition of Alzheimer's disease .
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-
- HY-182774
-
|
|
CXCR
|
Cancer
|
|
YU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma .
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-
- HY-182366
-
|
|
Histone Methyltransferase
|
Neurological Disease
Inflammation/Immunology
|
|
EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC50 value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis .
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-
- HY-175991S
-
|
Sodium stearyl sulfate sulfate-d37
|
Isotope-Labeled Compounds
Biochemical Assay Reagents
|
Others
|
|
Sodium octadecyl sulfate-d37 (Sodium stearyl sulfate-d37) is the deuterium labeled Sodium octadecyl sulfate (HY-W276164). Sodium octadecyl sulfate (Sodium stearyl sulfate) is a long-chain alkyl sodium sulfate that functions as an emulsifier, crosslinking agent, and regulator. Sodium octadecyl sulfate has high safety, with a LD50 greater than 3.00 Gm./Kg for both intraperitoneal injection in mice and oral administration in rats. Sodium octadecyl sulfate enhances continuous contraction of the gastrocnemius muscle in frogs and boosts intestinal smooth muscle activity in albino rats. However, Sodium octadecyl sulfate exerts no significant effect on isolated tortoise myocardium and does not alter the conduction function of frog sciatic nerves. Sodium octadecyl sulfate can also be used to coat the surface of starch aggregates, promote crosslinking and increase aggregate size through hydrophobic and electrostatic interactions, and further form a coexistent B-V type crystalline structure with acid-hydrolyzed gelatinized starch, thereby effectively modifying the structure and surface properties of high-starch systems .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-Y0850U3
-
|
Polyvinyl alcohol (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization); Poly(Ethenol) (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization)
|
Biochemical Assay Reagents
|
|
PVA (Polyvinyl alcohol) (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) is a water-soluble, biodegradable, biocompatible and non-immunogenic polymer. PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) causes no irritation to rabbit eyes, no skin sensitization in guinea pigs, promotes the proliferation of human skin keratinocytes, and reduces the loss of corneal endothelial cells. The LD50 of PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) in rats and dogs is greater than 10 g/kg. PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) is hardly absorbed by the digestive system, causes no adverse effects upon long-term oral administration, and shows no mutagenicity or carcinogenicity. However, repeated intravenous or portal vein injection of PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) may induce pathological changes such as glomerular lesions, anemia, hypertension or liver fibrosis in rats or dogs. Crosslinked nanofibers prepared by modifying PVA (Mw 125000, 98-99% hydrolyzed, ~2800 polymerization) can be used in studies related to wound dressings and other applications .
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-
- HY-W276164
-
|
Sodium stearyl sulfate
|
Biochemical Assay Reagents
|
|
Sodium octadecyl sulfate (Sodium stearyl sulfate) is a long-chain alkyl sodium sulfate that functions as an emulsifier, crosslinking agent, and regulator. Sodium octadecyl sulfate has high safety, with a LD50 greater than 3.00 Gm./Kg for both intraperitoneal injection in mice and oral administration in rats. Sodium octadecyl sulfate enhances continuous contraction of the gastrocnemius muscle in frogs and boosts intestinal smooth muscle activity in albino rats. However, Sodium octadecyl sulfate exerts no significant effect on isolated tortoise myocardium and does not alter the conduction function of frog sciatic nerves. Sodium octadecyl sulfate can also be used to coat the surface of starch aggregates, promote crosslinking and increase aggregate size through hydrophobic and electrostatic interactions, and further form a coexistent B-V type crystalline structure with acid-hydrolyzed gelatinized starch, thereby effectively modifying the structure and surface properties of high-starch systems .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-W758934
-
|
|
|
Stepronin-d5 (Prostenoglycine-d5; TTPG-d5; Tiase-d5) is the deuterium labeled Stepronin (HY-A0234). Stepronin (Prostenoglycine) is an orally active expectorant (inhalation administration is preferable to oral administration). Stepronin inhibits airway secretion in vitro by reducing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands .
|
-
-
- HY-118189S
-
|
|
|
Misoprostol acid-d5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers . Misoprostol is an oral agent used to induce labor .
|
-
-
- HY-W759719
-
|
|
|
21-Desacetyldeflazacort-d4 (21-desDFZ-d4) is the deuterium labeled 21-Desacetyldeflazacort (HY-100085). 21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
|
-
-
- HY-175991S
-
|
|
|
Sodium octadecyl sulfate-d37 (Sodium stearyl sulfate-d37) is the deuterium labeled Sodium octadecyl sulfate (HY-W276164). Sodium octadecyl sulfate (Sodium stearyl sulfate) is a long-chain alkyl sodium sulfate that functions as an emulsifier, crosslinking agent, and regulator. Sodium octadecyl sulfate has high safety, with a LD50 greater than 3.00 Gm./Kg for both intraperitoneal injection in mice and oral administration in rats. Sodium octadecyl sulfate enhances continuous contraction of the gastrocnemius muscle in frogs and boosts intestinal smooth muscle activity in albino rats. However, Sodium octadecyl sulfate exerts no significant effect on isolated tortoise myocardium and does not alter the conduction function of frog sciatic nerves. Sodium octadecyl sulfate can also be used to coat the surface of starch aggregates, promote crosslinking and increase aggregate size through hydrophobic and electrostatic interactions, and further form a coexistent B-V type crystalline structure with acid-hydrolyzed gelatinized starch, thereby effectively modifying the structure and surface properties of high-starch systems .
|
-
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