Search Result
Results for "
oral administration
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-108288
-
|
CP 47904
|
Beta-lactamase
Antibiotic
Bacterial
|
Infection
|
|
Sulbactam pivoxil is a proagent of sulbactam. Sulbactam is a β-lactamase inhibitor which poorly adsorbed from gastrointestinal tract. Sulbactam pivoxil has a better absorption than the parent agent and provides high serum levels after oral administration .
|
-
-
- HY-A0234
-
|
Prostenoglycine; TTPG; Tiase
|
Others
|
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 .
|
-
-
- HY-B0967
-
|
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Bacterial
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Infection
|
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Phthalylsulfacetamide is a sulfa drug, after oral administration, slowly decompose in the intestine,and release sulfacetamide ,generating antibacterial effect.
|
-
-
- HY-N0864
-
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Macranthoiside I
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Others
|
Cancer
|
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Macranthoidin B is a major bioactive saponin in rat plasma after oral administration of extraction of saponins from Flos Lonicerae.
|
-
-
- HY-N10225
-
|
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Prostaglandin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
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 .
|
-
-
- HY-146012
-
|
|
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 .
|
-
-
- HY-118683
-
|
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Others
|
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-A0234R
-
|
|
Others
|
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 .
|
-
-
- HY-U00122
-
|
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Others
|
Inflammation/Immunology
|
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Antiulcer Agent 1 is a 2-(3,4-dimethoxyphenyl)ethylamine derivative for oral administration at an exploratory stage of new agent development.
|
-
-
- HY-W740380
-
|
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Others
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Others
|
|
21-Carboxylic acid triamcinolone acetonide is a metabolite produced in the body after oral administration of [14C]-triamcinolone acetonide .
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-
-
- HY-20559
-
|
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Biochemical Assay Reagents
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Others
|
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4-Chloro-3-nitrobenzoic acid has oral activity, and oral administration can affect the synthesis activity of liver proteins and the activities of urokinase and histidine kinase .
|
-
-
- HY-122307
-
|
DAN-603
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Others
|
Metabolic Disease
|
|
Sulisatin (DAN-603) is an anionic laxative that is hydrolyzed to diphenolic derivatives by bacterial aryl sulfate sulfohydrolases in the colon during oral administration .
|
-
-
- HY-120639
-
|
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Others
|
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.
|
-
-
- HY-147136
-
|
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Others
|
Cancer
|
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MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration .
|
-
-
- HY-N0856
-
|
23-O-Acetylalisol C; Alisol C monoacetate
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Others
|
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.
|
-
-
- HY-N4173
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
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-118543
-
|
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HIF/HIF Prolyl-Hydroxylase
|
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 .
|
-
-
- HY-135245
-
|
SCH 488128; Ezetimibe hydroxy β-D-Glucuronide
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Ezetimibe hydroxy glucuronide (SCH 488128) is a trace metabolite detected in dog and human plasma samples after oral administration of Ezetimibe (HY-17376) .
|
-
-
- HY-123367
-
|
|
Others
|
Others
|
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Rubraxanthone is a compound with multiple biological activities. Its pharmacokinetic parameters were determined in mice and it showed a certain concentration variation pattern in plasma after oral administration.
|
-
-
- HY-105919
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
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-129579
-
|
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Others
|
Others
|
|
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).
|
-
-
- HY-122307A
-
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DAN-603 disodium
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Others
|
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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-
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- HY-135578
-
|
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Parasite
|
Infection
|
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Artelinic acid, a derivative of Artemisinin, is an antimalarial agent for the treatment of multidrug resistant strains of Plasmodium falciparum. Artelinic acid can be administered by various routes of administration, including intravenous, intramuscular and oral routes .
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-
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- HY-24238
-
|
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Others
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Others
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DLCI-1 is a potent and selective oral inhibitor of cytochrome P450 2A6 (CYP2A6) that markedly reduces nicotine self-administration in both male and female mice.
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-
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- HY-N6910
-
|
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Others
|
Metabolic Disease
|
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Pseudolaric Acid C2, a diterpenoid isolated from Pseudolarix kaempferi, is identified as the specific metabolite of Pseudolaric acid B in plasma, urine, bile and feces after both oral and intravenous administration to rats .
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-
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- HY-165529
-
|
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Others
|
Inflammation/Immunology
|
Camostat is an orally active trypsin inhibitor. Camostat can reduce pancreatic fibrosis induced by repeated administration of superoxide dismutase inhibitors in rats, and decrease the proliferation and activation of pancreatic stellate cells (PSCs) .
|
-
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- HY-102061
-
|
ATI 7505 dihydrochloride
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Others
|
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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-
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- HY-118301
-
|
|
GABA Receptor
|
Neurological Disease
|
|
ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity .
|
-
-
- HY-W011309
-
|
1-O-HDG; HXDG
|
PPAR
PGE synthase
|
Inflammation/Immunology
|
|
1-O-Hexadecylglycerol can up-regulate PPAR-γ expression, inhibit pGE2, and exhibit anti-inflammatory properties . 1-O-Hexadecylglycerol is effective in oral administration .
|
-
-
- HY-145461
-
|
5-Hydroxy lenalidomide
|
Others
|
Others
|
|
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-162893
-
|
|
Glucosidase
|
Metabolic Disease
|
|
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 .
|
-
-
- HY-14795
-
|
ZT-1
|
|
Neurological Disease
|
|
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-19899
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-122309
-
|
|
Antibiotic
|
Infection
|
|
A-71497 is the 3-formyl derivative of the antibiotic Tosufloxacin (HY-B1802). A-71497 can produce high plasma levels of tosufloxacin upon both oral and subcutaneous administration to mice .
|
-
-
- HY-144110
-
|
|
HCV
|
Infection
|
|
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-144878
-
|
|
c-Myc
|
Cancer
|
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VPC-70619 is a potent, orally active N-Myc inhibitor. VPC-70619 blocks the N-Myc-Max heterocomplex from binding to DNA E-boxes and demonstrated strong inhibition activity against N-Myc-dependent cell lines as well as high bioavailability in both oral and intraperitoneal administration .
|
-
-
- HY-118222
-
|
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Others
|
Others
|
|
KBR 2822 is an esterase inhibitor used to inhibit neuropathic target esterase (NTE), the target of delayed organophosphate-induced neuropathy. Experiments have shown that chronic oral administration of KBR-2822 (0.2 or 0.4 mg/kg/day) to chickens does not induce neuropathy and does not exacerbate toxic or traumatic axonopathy, even in the absence of intentional axonal injury. In the control group, administration of non-neuropathic Paraoxon (0.05 mg/kg/day orally) showed a mean AChE inhibition of 45% and no NTE inhibition. After chronic administration of KBR-2822, PMSF (120 mg/kg subcutaneously, 24 hours after the last KBR-2822 dose) was given, and KBR-2822-treated chickens did not develop neuropathy, while chickens treated with neuropathic DFP did. This suggests that sustained facilitatory "stress" is harmless to chicken axons in the absence of concurrent biochemical or neurotoxic insults.
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-
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- HY-149900
-
|
|
Biochemical Assay Reagents
|
Infection
|
|
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 .
|
-
-
- HY-118426
-
|
(Rac)-IND 58359; (Rac)-R115777
|
Others
|
Cancer
|
|
(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 .
|
-
-
- HY-118189
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
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-100085
-
|
21-desDFZ
|
Drug Metabolite
|
Inflammation/Immunology
|
|
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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-
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- HY-122968
-
|
NSD-1065
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Others
|
Neurological Disease
|
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Brocresine (NSD-1065) is an orally active histidine decarboxylase inhibitor and inhibits the formation of histamine from histidine. Brocresine is also a L-amino acid decarboxylase inhibitor with both a peripheral and central action. Brocresine inhibits gastric secretory response to administration of exogenous gastrin .
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-
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- HY-111073
-
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Y101
|
HBV
|
Infection
Inflammation/Immunology
|
|
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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-
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- HY-147152
-
|
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Others
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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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-
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- HY-156466
-
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JAK
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Inflammation/Immunology
|
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QL-1200186 is anorally activeand selective inhibitor ofTYK2. Oral administration of QL-1200186, dose-dependently inhibitsinterferon-γ(IFNγ) production afterinterleukin-12(IL-12) challenge and significantly ameliorates skin lesions in psoriatic mice .
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-
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- HY-103459
-
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PD156707
|
Endothelin Receptor
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Cardiovascular Disease
|
|
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-114452
-
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BTRX-246040
|
Opioid Receptor
|
Neurological Disease
|
|
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models .
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-
-
- HY-N7103R
-
|
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Others
|
Others
|
|
Ethyl oleate (Standard) is the analytical standard of Ethyl oleate. This product is intended for research and analytical applications. Ethyl Oleate is a fatty acid ester formed by the condensation of oleic acid and ethanol. Ethyl oleate is the liquid lipid component in nanostructured lipid carriers (NLCs). NLC is a promising vehicle for oral trans-Ferulic acid (TFA) administration .
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-
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- HY-103442
-
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DAPH
|
EGFR
Amyloid-β
|
Neurological Disease
Cancer
|
|
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease .
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- HY-16100
-
|
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Fatty Acid Synthase (FASN)
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Metabolic Disease
Cancer
|
|
BI 99179 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-145427
-
|
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DNA-PK
|
Cancer
|
|
NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect .
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- HY-W339484
-
|
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Others
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Others
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1-Ethyl-2-methyl-3-hydroxypyrid-4-one is an α-ketohydroxypyridinium iron chelator that increases iron excretion in iron-overloaded rabbits after oral or parenteral administration and is highly specific for iron, with no specific activity for copper, zinc, calcium, and magnesium.
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-
- HY-110197
-
6bK TFA
1 Publications Verification
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Others
|
Metabolic Disease
|
|
6bK TFA is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK TFA increases circulating insulin in high-fat-fed mice. Acute administration of 6bK TFA enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice .
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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-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
|
Cancer
|
|
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-118189S
-
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Isotope-Labeled Compounds
Prostaglandin Receptor
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Inflammation/Immunology
|
|
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[1]. Misoprostol is an oral agent used to induce labor[2].
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- HY-107129
-
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GCGR
|
Metabolic Disease
|
|
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-16622B
-
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Others
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Endocrinology
|
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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-126230
-
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Others
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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-114452A
-
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BTRX-246040 tartrate
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Opioid Receptor
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Neurological Disease
|
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LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models .
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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-124185
-
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Others
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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-159702
-
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Mucin
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Others
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Eudragit RS 100 is a mucoadhesive, nonbiodegradable positively charged polymer,which can be used for research of developing nanoparticles (NPs) for the ophthalmic and oral administration of Ibuprofen (HY-78131) and Cyclosporins (HY-100731), as well as nano- and micro-fibres used as scaffolds. Eudragit RS 100 NPs interacts efficiently with mucin and promotes glutathione (GSH) transmucosal absorption .
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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-100085R
-
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Drug Metabolite
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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-N0307
-
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Bcl-2 Family
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Neurological Disease
|
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Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory .
Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation .
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- HY-15883
-
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
|
|
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
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-
- HY-101478
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mGluR
Apoptosis
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Neurological Disease
Cancer
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Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .
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- HY-101478A
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mGluR
Apoptosis
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Neurological Disease
Cancer
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Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .
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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-126230A
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Others
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Cancer
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(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-167840
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Others
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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-167679
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Others
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Inflammation/Immunology
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Scio-323 is an orally available p38 mitogen-activated protein kinase (MAPK) inhibitor with the potential to inhibit chronic inflammatory responses associated with polyethylene particles. Scio-323's oral inhibition pattern had a minimal effect on bone formation. Scio-323 administration inhibited net bone formation after the establishment of a chronic inflammatory response to polyethylene particles. Osteoblast-like activity remained low in all cases of Scio-323 inhibition. Scio-323 failed to improve bone growth in the presence of polyethylene particles .
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- HY-162423
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5-HT Receptor
Androgen Receptor
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Neurological Disease
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CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration .
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- HY-106720C
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(+)-YM 09538
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Others
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Others
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(+)-Amosulalol ((+)-YM 09538) is an α,β-blocker with pharmacokinetic and metabolic activities in mice. In mice, the plasma concentration of (+)-Amosulalol decreased in a biphasic manner after intravenous injection. The time to reach the maximum plasma concentration after oral administration was 0.25h, and then decreased. The systemic bioavailability was 38.7%, and it was mainly excreted through urine. Multiple metabolites were detected in urine, and a new metabolite amosulalol carbamoyl glucuronide was found in bile samples.
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- HY-106720B
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(-)-YM 09538
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Others
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Others
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(-)-Amosulalol ((-)-YM 09538) is an α,β-blocker with pharmacokinetic and metabolic activities in mice. In mice, the plasma concentration of (-)-Amosulalol decreased in a biphasic manner after intravenous injection. The time to reach the maximum plasma concentration after oral administration was 0.25h, and then decreased. The systemic bioavailability was 38.7%, and it was mainly excreted through urine. Multiple metabolites were detected in urine, and a new metabolite amosulalol carbamoyl glucuronide was found in bile samples.
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- HY-18157
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Others
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Neurological Disease
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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-146434
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TGF-beta/Smad
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Inflammation/Immunology
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TGFβ-IN-2 (Compound 9d) inhibits TGF-β-induced total collagen accumulation in NRK-49F cells with the IC50 of 4.31 μM. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 can be used as a potential effective compound for anti-fibrosis in vivo by oral administration .
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- HY-163983
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Microtubule/Tubulin
Apoptosis
PARP
Caspase
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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-119221A
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Others
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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-N7545
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Antibiotic
Reverse Transcriptase
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Infection
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Protorubradirin is an antibiotic that can be isolated from Streptomyces achromogenes var. rubradirin together with Rubradirin. Protorubradirin has inhibitory activity against HIV reverse transcriptase. In vitro studies have shown that Protorubradirin also inhibits Staphylococcus aureus strains and Streptococci. In infected mice, subcutaneous injection of Protorubradirin showed in vivo inhibitory efficacy against antibiotic-resistant Staphylococcus aureus strains. However, oral administration may result in a significant reduction in the activity of Protorubradirin, possibly due to faster cleavage of its C-nitroso sugar in the acidic gastric environment compared to Rubradirin .
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- HY-139792
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SHR117887
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Others
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Metabolic Disease
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Besigliptin tosylate (SHR117887) is a DPP-4 inhibitor with activity to improve metabolic control and β-cell function. Besigliptin tosylate can effectively reduce serum DPP-4 activity and improve oral glucose tolerance. Besigliptin tosylate significantly reduces fasting blood glucose levels and improves lipid profiles in a diabetic mouse model. The effect of besigliptin tosylate is comparable to that of the known compound vildagliptin (HY-14291) at the same concentration. Besigliptin tosylate increases insulin staining of pancreatic islet cells in chronic administration, indicating improved β-cell function .
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- HY-W328882
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Others
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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
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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-13590
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Others
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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-124110
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nAChR
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Neurological Disease
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TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2 ∗ and α4β2 ∗ nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2 ∗ nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2 ∗ nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease .
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- HY-N0469R
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Endogenous Metabolite
Virus Protease
HSV
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Infection
Metabolic Disease
Inflammation/Immunology
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L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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- HY-139124
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15(R)-Carboprost; 15(R)-15-methyl PGF2α
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Others
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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-118243
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Others
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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-116275
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Others
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Cancer
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KRM-II-81 is a gamma-aminobutyric acid type A (GABAA) receptor ligand with analgesic, anxiolytic and anti-epileptic activities. KRM-II-81 exhibits positive allosteric modulation of GABAA receptors selective for the α2/3 subunit. KRM-II-81 reduces formalin-induced pain response after oral administration. KRM-II-81 significantly reduces pain behavior induced by chronic spinal nerve ligation. Analysis of KRM-II-81 showed that its plasma and brain concentrations were positively correlated with analgesic effects. The enhancement effect of KRM-II-81 on GABA current shows its key role in the analgesic mechanism. KRM-II-81 was less effective in respiratory depression, demonstrating its safety and tolerability .
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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-163403
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VEGFR
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Cardiovascular Disease
Cancer
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VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
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- HY-118185
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Others
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Others
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SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 μmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 μmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 μmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.
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- HY-117991
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Others
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Cancer
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DW10075 is a novel, highly selective VEGFR inhibitor that targets the VEGF/VEGF receptor (VEGFR) pathway, which has been shown to be an effective anti-angiogenic approach for cancer therapy. Studies have found that DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3 among 21 kinases, while having no effect on the other 18 kinases, including FGFR and PDGFR. In human umbilical vein endothelial cells (HUVECs), DW10075 significantly prevented VEGF-induced activation of VEGFR and its downstream signaling, thereby inhibiting VEGF-induced HUVEC proliferation. In addition, DW10075 dose-dependently inhibited VEGF-induced HUVEC migration and tube formation, and suppressed angiogenesis in the rat aortic ring model and the chick embryo chorionic membrane model. DW10075 also exhibited antiproliferative activity against 22 different human cancer cell lines, with IC50 values ranging from 2.2 μmol/L (for U87-MG human glioblastoma cells) to 22.2 μmol/L (for A375 melanoma cells). In the nude mouse U87-MG xenograft tumor model, oral administration of DW10075 significantly inhibited tumor growth and reduced the expression of CD31 and Ki67 in tumor tissues. In summary, DW10075 is a potential anti-tumor angiogenesis agent that deserves further development.
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HY-L061
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3,666 compounds
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Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 3,666 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
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| Cat. No. |
Product Name |
Type |
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- HY-20559
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Cell Assay Reagents
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4-Chloro-3-nitrobenzoic acid has oral activity, and oral administration can affect the synthesis activity of liver proteins and the activities of urokinase and histidine kinase .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0864
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-
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- HY-N0856
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- HY-N4173
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- HY-N6910
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- HY-N6641
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- HY-N0307
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- HY-N10225
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- HY-N7103R
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- HY-N7545
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Structural Classification
Microorganisms
Antibiotics
Source classification
Other Antibiotics
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Antibiotic
Reverse Transcriptase
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Protorubradirin is an antibiotic that can be isolated from Streptomyces achromogenes var. rubradirin together with Rubradirin. Protorubradirin has inhibitory activity against HIV reverse transcriptase. In vitro studies have shown that Protorubradirin also inhibits Staphylococcus aureus strains and Streptococci. In infected mice, subcutaneous injection of Protorubradirin showed in vivo inhibitory efficacy against antibiotic-resistant Staphylococcus aureus strains. However, oral administration may result in a significant reduction in the activity of Protorubradirin, possibly due to faster cleavage of its C-nitroso sugar in the acidic gastric environment compared to Rubradirin .
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- HY-N0469R
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Structural Classification
Microorganisms
Source classification
Disease markers
Endocrine diseases
Amino acids
Nervous System Disorder
Endogenous metabolite
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Endogenous Metabolite
Virus Protease
HSV
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L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-118189S
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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[1]. Misoprostol is an oral agent used to induce labor[2].
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| Cat. No. |
Product Name |
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Classification |
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- HY-N7103
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Solvents
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Ethyl Oleate is a fatty acid ester formed by the condensation of oleic acid and ethanol. Ethyl oleate is the liquid lipid component in nanostructured lipid carriers (NLCs). NLC is a promising vehicle for oral trans-Ferulic acid (TFA) administration .
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