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Lipid 5 is an amino lipid that affords efficient mRNA delivery in rodent and primate models. Lipid 5 shows optimal pharmacokinetics and non-toxic side effects .
Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Schisandrin B (γ-Schisandrin) is a biphenylcyclooctadiene derivative isolated from Schisandra chinensis and has been shown to have antioxidant effects on the liver and heart of rodents.
N,N'-diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine is a potent, orally active modulator of contact sensitivity/delayed type hypersensitivity reactions in rodents. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits .
Coenzyme Q9 (Ubiquinone Q9), the major form of ubiquinone in rodents, is an amphipathic molecular component of the electron transport chain that functions as an endogenous antioxidant. Coenzyme Q9 attenuates the diabetes-induced decreases in antioxidant defense mechanisms. Coenzyme Q9 improves left ventricular performance and reduces myocardial infarct size and cardiomyocyte apoptosis .
5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury.5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
Rodent Gnawing Blocks are irradiated and sterilized poplar blocks used for molarization in laboratory rodents such as mice and rats. Rodent Gnawing Blocks can also be autoclaved.
4'-O-Methylpyridoxine is an orally active antivitamin B6 compound found in Ginkgo biloba seeds and leaves. 4'-O-Methylpyridoxine inhibits pyridoxal kinase. 4'-O-Methylpyridoxine reduces brain pyridoxal-5'-phosphate (PLP) levels, decreases gamma-aminobutyric acid/glutamate (GABA/Glu) ratio. 4'-O-Methylpyridoxine increases plasma levels of pyridoxal-5'-phosphate and pyridoxal. 4'-O-Methylpyridoxine induces hyperactivity, convulsions, pathological tissue changes, organ damage in rodent brain and heart .
EBP-IN-1 is an orally active, blood-brain barrier-permeable inhibitor of emopamil binding protein (EBP). EBP-IN-1 has an IC50 of 8.2 μM against human ERG potassium channels (in CHO background). By inhibiting the sterol isomerase activity of EBP, EBP-IN-1 causes the accumulation of Zymostenol (HY-113345), and exhibits strong target binding in the brain after repeated administration in rodents. EBP-IN-1 also promotes oligodendrocyte formation in human cortical organoids and can be used in research related to multiple sclerosis .
Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents[1][2].
BMS 191011 (BMS-A) is a potent BKCa channel opener (large-conductance Ca 2+-activated potassium channel). BMS-191011 shows neuroprotective activities in rodent models of stroke .
7-Dehydro desmosterol is a sterol and an intermediate in cholesterol biosynthesis, which is found in the marine diatom Pseudo-nitzschia multistriata and the nervous system of rodents .
WS3 is a novel proliferative molecule that promotes pancreatic β cell proliferation in rodent and human primary islets. WS3 can be used for the research of type 1 diabetes .
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .
Evenamide (NW-3509) is an orally available voltage-gated sodium channel (VGSC) blocker (Ki=0.4 µM) for the research of schizophrenia. Evenamide shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness .
S-Methylisothiourea sulfate is a potent, selective and competitive inhibitor of inducible nitric oxide synthase (iNOS). S-Methylisothiourea sulfate exerts beneficial effects in rodent models of septic shock .
Acifluorfen, a protoporphyrinogen oxidase (PROTOX) inhibitor herbicide, promotes the accumulation of protoporphyrin IX (PPIX), and induces tumors in the rodent liver. Acifluorfen causes strong photooxidative destruction of pigments and lipids in sensitive plant species .
CP-346086 is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 can lower plasma cholesterol and triglycerides in vivo .
S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests .
Roridin E is a glucose-6-phosphatase (G6Pase) inhibitor and antibiotic, and is a metabolic byproduct of Roridin A (HY-N9599). Roridin E induces significant oxidative stress, characterized by depletion of glutathione in vivo, induction of hepatic lipid peroxidation, and inhibition of renal superoxide dismutase activity. Roridin E reduces blood glucose levels in rats, but exhibits acute toxicity (which is enhanced when co-administered with linoleic acid (HY-N0729)) and causes hepatotoxicity in male albino mice. Roridin E induces a decrease in total blood protein and increases in the levels of total lipids, γ-glutamyltransferase, alkaline phosphatase, and 5'-nucleotidase. Roridin E can be isolated from molds, and possesses cytostatic and antifungal activities similar to those of Verrucarin A (HY-107426) and Roridin A. Roridin E exhibits in vivo activity in rodents and is commonly used in hepatotoxicity-related studies .
Triethyl phosphate is a versatile phosphate ester compound. Triethyl phosphate induces rapid and short-acting anesthesia, and exhibits hypotensive, smooth muscle relaxant, and cardiac inhibitory effects. Triethyl phosphate also modulates cholinergic toxicity; its anesthetic effect shows sex- and age-dependency in rodents, and it interacts with SKF 525-A (HY-B1311) to alter the duration of anesthesia .
Sabcomeline (SB-202026; Memric) hydrochloride is a muscarinic receptor agonist capable of crossing the blood-brain barrier. Sabcomeline hydrochloride exhibits affinity for all hM1 to hM5 subtypes (pKi=6.72-7.23), and shows near-full agonism at the hM3 receptor, inducing extracellular acidification. Sabcomeline hydrochloride alters the binding kinetics of dopamine D2 receptors through neural network regulation. Sabcomeline hydrochloride also causes minimal cardiovascular changes, effectively reverses spatial memory deficits in rodents and induces conditioned taste aversion. Sabcomeline hydrochloride is an important tool compound in studies of Alzheimer's disease and related neurodegenerative diseases .
VH4127 TFA is a cyclic peptide targeting the low density lipoprotein receptor (LDLR) with a KD of 18 nM for hLDLR. VH4127 TFA specifically binds to rodent and human epidermal growth factor (EGF) homology domain of LDLR .
MONNA is a potent transmembrane protein 16A (TMEM16A, Anoctamin-1) blocker with an IC50 of 80 nM. MONNA induces vasorelaxation of rodent resistance arteries in presence or absence of chloride ions .
N-Arachidonoylserotonin (Arachidonyl serotonin; AA-5-HT) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 value of 1~12 µM. N-Arachidonoylserotonin acts also as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels (IC50=70~100 nM). N-Arachidonoylserotonin is analgesic in rodents .
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD) .
Coenzyme Q9 (Standard) is the analytical standard of Coenzyme Q9. This product is intended for research and analytical applications. Coenzyme Q9 (Ubiquinone Q9), the major form of ubiquinone in rodents, is an amphipathic molecular component of the electron transport chain that functions as an endogenous antioxidant. Coenzyme Q9 attenuates the diabetes-induced decreases in antioxidant defense mechanisms. Coenzyme Q9 improves left ventricular performance and reduces myocardial infarct size and cardiomyocyte apoptosis .
Sophoramine ((-)-Sophoramine) is a prejunctional α2-adrenoceptor inhibitor that can be found in the seeds of Sophora alopecuroides. Sophoramine inhibits prejunctional α2-adrenoceptors to facilitate norepinephrine release from adrenergic nerves. Sophoramine shows cytotoxic activity against human cancer cells, positive inotropic activity, and activity in rodent arrhythmia models. Sophoramine can be used for the research of arrhythmias .
Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
DORA-22 is an orally active dual orexinergic receptor antagonist, and improves the sleep disruption and memory impairment. DORA-22 can be used for study of insomnia .
PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
Sulfamethoxazole-NO (SMX-NO) is the major immunogen in sulfonamide allergy, producing modest ascorbic acid depletion and hemoglobin adduct formation. Sulfamethoxazole-NO haptens tissue proteins and is immunogenic in rodents .
CID1231538, a benzothiazole analog, is a potent GPR35 antagonist with no significant activity against rodent orthologs of GPR35, which is also a G protein-coupled receptor (GPCR) .
CP-346086 dihydrate is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 dihydrate can lower plasma cholesterol and triglycerides in vivo .
Amoscanate (cgp4540) is phenyl isothiocyanate in which the hydrogen at the para-position has been replaced by a 4-nitroanilinyl group. Amoscanate is an anti-schistosomal agent. Amoscanate, as an isothiocyanate compound and uncoupler of oxidative phosphorylation, potently injures rodent ependyma .
MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer .
Tetrachlorohydroquinone (TCHQ) is a metabolite of Pentachlorophenol. Tetrachlorohydroquinone induces reactive oxidant stress (ROS), inhibits apoptosis and induces necrosis in primary mouse splenocytes. Tetrachlorohydroquinone increases DNA lesions and induces oxidative stress in rodents .
Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate . Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents .
1-Methylpyrene is a ubiquitous environmental pollutant and rodent carcinogen. Its mutagenic activity depends on sequential activation by various CYP and sulfotransferase (SULT) enzymes. 1-Methylpyrene induces chromosome loss and mitotic disturbance, proba
m3-Huwentoxin IV (m3-HwTx-IV) is a potent NaV inhibitor with IC50s of 3.3, 6.8, 7.2, 8.4, 11.9 and 369 nM against hNaV1.7, hNaV1.6, hNaV1.3, hNaV1.1, hNaV1.2 and hNaV1.4, respectively in QPatch assay. m3-Huwentoxin IV dose-dependently suppresses spontaneous pain induced by the NaV1.7 activator OD1 in a rodent pain model .
MK-8666 is a potent and selective partial GPR40 agonist (EC50 = 0.54 nM for human GPR40). MK-8666 shows selectivity over GPR119, GPR43, GPR41, GPR120, and other G-protein-coupled receptors (GPCRs). MK-8666 reduces glucose in the rodent. MK-8666 can be used for type 2 diabetes research [1][2].
(+)-Schisandrin B is an enantiomer of Schisandrin B. Schisandrin B is an active dibenzocyclooctadiene derivative isolated from the fruit of Schisandra chinensis, has antioxidant effect on rodent liver and heart .
CGP 37849 is a potent, competitive and orally active N-methyl-D-aspartate (NMDA) receptor antagonist. CGP 37849 is an anticonvulsant in rodents and has antidepressant and anxiolytic-like effects .
ISIS 329993 (ISIS-CRPRx) is an antisense oligonucleotide targeting to C-reactive protein (CRP). ISIS-CRPRx has been tested in a rodent model of rheumatoid arthritis (RA) and was shown to improve the clinical signs of arthritis
Imepitoin (Standard) is the analytical standard of Imepitoin. This product is intended for research and analytical applications. Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
CP-114271 is a potent selective β3-adrenergic receptor agonist. CP-114271 possesses an in vivo efficacy in rodent models. CP-114271 can be used for obesity research .
α-Muricholic acid (Standard) is the analytical standard of α-Muricholic acid. This product is intended for research and analytical applications. α-Muricholic acid is the most abundant primary bile acid in rodents .
Menoctone is an orally active antimalarial agent that demonstrates suppressive effects against blood-induced rodent malaria. Menoctone enhances the anti-malarias effect of chloroquine or quinine and can be utilized in malarias research .
Clonixin (Standard) is the analytical standard of Clonixin. This product is intended for research and analytical applications. Clonixin (SCH-10304) is an orally active non-steroidal anti-inflammatory agent in rodents .
N,N'-Diacetyl-L-cystine (Standard) is the analytical standard of N,N'-Diacetyl-L-cystine. This product is intended for research and analytical applications. N,N'-diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine is a potent, orally active modulator of contact sensitivity/delayed type hypersensitivity reactions in rodents. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits .
LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC50 value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain .
5,7-Dichlorokynurenic acid (5,7-DCKA) sodium is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid sodium reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid sodium increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid sodium exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
MCL-0129 is a compound with anxiolytic and antidepressant activity and is a selective MC4 receptor antagonist that exhibits anxiolytic and antidepressant-like behaviors in multiple rodent models.
Dersalazine (sodium) is a platelet-activating factor (PAF) antagonist. Dersalazine (sodium) can exert intestinal anti-inflammatory activity in rodent colitis models by downregulating IL-17 expression .
ICI 56780 is an antimalarial agent, that exhibits etiological prevention and blood schizonticidal activity in rodent malaria models. ICI 56780 develops parasite resistance in P. berghei infected mice .
ISIS 329993 sodium is an antisense oligonucleotide targeting to C-reactive protein (CRP). ISIS-CRPRx sodium has been tested in a rodent model of rheumatoid arthritis (RA) and was shown to improve the clinical signs of arthritis
LBP1 is an orally active and low brain penetrant CB1 receptor agonist. LBP1 exhibits significant anti-allodynic and anti-hyperalgesic effects in rodent models of neuropathic pain .
BMS-902483 is a quinuclidine-containing spirooxazolidine that is a partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). BMS-902483 improves cognitive ability in preclinical rodent models. .
A-412997 is a selective Dopamine D4 agonist with Ki values of 12 and 7.9 nM for the rat and human receptors. A-412997 improves short term memory and cognitive properties in rodent models .
Butyrylhydroxamic acid (N-Hydroxybutanamide) is a potent inhibitor of histone deacetylase (HDAC). Butyrylhydroxamic acid enhances memory in behavioral models of rodents and can be used as memory enhancers, mood stabilizers, and β-chain hemoglobin disease studies .
Acifluorfen sodium, a protoporphyrinogen oxidase (PROTOX) inhibitor herbicide, promotes the accumulation of protoporphyrin IX (PPIX), and induces tumors in the rodent liver. Acifluorfen sodium causes strong photooxidative destruction of pigments and lipids in sensitive plant species .
Soretolide is an antiepileptic agent. Soretolide is effective in maximal electroshock-induced seizure (MES) test in rodents. Soretolide inhibits metabolism of Phenytoin (HY-B0448). Soretolide exhibits a good pharmacokinetic character in rats model .
LJP 1586 is an amine-based inhibitor of semicarbazide-sensitive amine oxidase (SSAO) activity. LJP 1586 is an orally active, potent and selective inhibitor of rodent and human SSAO activity, with IC50 values between 4 and 43 nM .
Evenamide hydrochloride is an orally available voltage-gated sodium channel (VGSC) blocker (Ki=0.4 μM) for the research of schizophrenia. Evenamide hydrochloride shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness .
Amfenac ethyl ester is an orally active cyclooxygenase (COX) inhibitor. Amfenac ethyl ester exhibits antiinflammatory activity in rodent models. Amfenac ethyl ester can be used for the research of inflammation .
α5β1 integrin-IN-1 (compound 65) is a potent and selective α5β1 integrin inhibitor with a pIC50 of 9.4. α5β1 integrin-IN-1 displays >10000-fold selectivity for α5β1 over αVβ3 (pIC50 = 5.5). α5β1 integrin-IN-1 reduces airway smooth muscle (ASM) tension through the disruption of cellular tethering. α5β1 integrin-IN-1 exhibits excellent inhalation pharmacokinetics in rodent. α5β1 integrin-IN-1 can be used for asthma research .
(S)-Pulegone ((-)-Pulegone) is a cytochrome P450 (CYP450) substrate. (S)-Pulegone induces urothelial cytotoxicity, necrosis, regenerative proliferation and urinary bladder tumors in female rats. (S)-Pulegone induces rodent nephropathy, olfactory metaplasia, gastric hyperplasia/perforation at high dose. (S)-Pulegone can be used for the research of urinary bladder and hepatic neoplasms .
LP-935001 is a Notum carboxylesterase inhibitor with an IC50 of 0.4 nM.LP-935001 prevents palmitoleate group removal from Wnt proteins, restores Wnt/β-catenin signaling.LP-935001 enhances cortical bone thickness in rodent models.LP-935001 can be used for the research of bone loss/nonvertebral fractures .
LY2775240 is an orally active phosphodiesterase 4 (PDE4) inhibitor with potent inhibitory activity against PDE4A (IC50 = 0.09 nM), PDE4B (IC50 = 0.09 nM) and PDE4D (IC50 = 0.14 nM), and exhibits an IC50 of 2.4 nM against PDE4C. LY2775240 is a highly selective agent that reduces TNFα production upon immune activation. LY2775240 decreases TNFα production in rodent and rhesus monkey models. LY2775240 can be used in the research of psoriasis .
R9-13 is a fatty acid-conjugated relaxin and an agonist of LGR7 (RXFP1). R9-13 induces sustained pubic symphysis elongation in estrogen-pretreated mice. R9-13 exhibits long-acting pharmacokinetic profiles in rodents, with in vivo activity lasting up to one week after administration. R9-13 can be used in studies related to acute heart failure .
Satranidazole is an orally active insecticide and antimicrobial agent with high electron affinity. Satranidazole forms reduced nitro intermediates, which interact with DNA, causing helix instability, strand breakage and release of thymidine derivatives. Satranidazole exhibits antitrichomonal activity against Trichomonas vaginalis and Trichomonas foetus, and antiamoebic activity in rodent models of hepatic amoebiasis and caecal amoebiasis. Satranidazole inhibits the replication of bacteriophage φX174 DNA. Satranidazole can be used in research related to caecal amoebiasis, trichomoniasis and anaerobic bacterial infections .
R-MDMA, 4-methylenedioxymethamphetamine (MDMA) isomer, is a 5-HT2A/5-HT2C receptor antagonist with an IC50 of 629 and 61.4 nM. R-MDMA promotes cortical neuron growth. R-MDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDMA can be used for the researches of post-traumatic stress disorder and depression .
NNMT-IN-8 is a non-SAM-mimicking bisubstrate inhibitor and a selective methyltransferase NNMT inhibitor, with IC50 values of 0.0084 μM and 0.0085 μM against human NNMT, and an IC50 of 0.0072 μM against mouse NNMT. NNMT-IN-8 exhibits prominent renal distribution characteristics and moderate bioavailability in rodents. NNMT-IN-8 dose-dependently inhibits renal NNMT in renal fibrosis models, thereby exerting antifibrotic effects. NNMT-IN-8 can be used to investigate the mechanisms of renal fibrosis .
R-MDDMA, 4-methylenedioxymethamphetamine (MDMA) analogue, is a 5-HT2A/5-HT2C receptor modulator. R-MDDMA shows antagonistic activity against 5-HT2A/5-HT2C with IC50values of 642 and 137 nM, and also shows partial agonist activity with EC50 values of 24.5 and 14.4 nM, but does not activate 5-HT2B receptors. R-MDDMA promotes cortical neuron growth. R-MDDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDDMA can be used for the researches of post-traumatic stress disorder and depression .
NMDA receptor antagonist 10 is a NMDA receptor antagonist with an IC50 of 28 μM. NMDA receptor antagonist 10 inhibits glycine action at the NMDA receptor glycine site. NMDA receptor antagonist 10 can be used for research on neurological diseases .
Zoxazolamine (Standard) is the analytical standard of Zoxazolamine. This product is intended for research and analytical applications. Zoxazolamine is widely used for a pharmacologic test that serves as a convenient indicator of changes in cytochrome P-450 activity in rodents.
PMEG is a nuclear DNA polymerases α, δ, and ε inhibitor that causes DNA chain termination, inhibits DNA synthesis, induces cytotoxicity in dividing cells. PMEG is an acyclic nucleotide phosphonate that forms an active phosphorylated metabolite, PMEG diphosphate, within cells. PMEG has activity against leukemia and melanoma in rodent models. PMEG has poor cell permeability; its prodrug is Rabacfosadine (GS-9219) (HY-13640). PMEG shows antiviral activity against against various DNA virus infections including murine cytomegalovirus (MCMV) and human cytomegalovirus (HCMV). PMEG can be used for the research of non-hodgkin's lymphoma[1][2].
KY1070 is a fully human anti-BMP6 antibody with a Kd of 0.00014 μM against the human BMP6. It exhibits high specificity for BMP6, showing no cross-reactivity with other members of the BMP family, and effectively inhibits BMP6-induced BMP receptor heterodimerization and hepcidin expression. KY1070 modulates Ferroportin expression on erythroid progenitor cells and accelerates erythropoiesis. In rodent anemia models, KY1070 reduces the required dose of erythropoietin (EPO) when used in combination with EPO and enhances the responsiveness of mice with chronic kidney disease (CKD)-associated anemia to EPO treatment. KY1070 is applicable for research on anemia of chronic disease [1] [2].
Prokineticin 2 Isoform 2 (human) is a hypothalamic neuropeptide. Prokineticin 2 Isoform 2 (human) decreases food intake and involves in thermoregulation and energy metabolism in rodents. Prokineticin 2 has the potential for the research of hyperglycemia, metabolic syndrome (MetS) and obesity .
BVT-74316 is a 5-HT6 receptor antagonist. BVT-74316 can reduce food intake and bodyweight gain in rodent models. BVT-74316 can be used for the research of metabolic disease, such as obesity .
BML-265 is a potent EGFR tyrosine kinase inhibitor. BML-265 disrupts Golgi integrity and abolishes secretory protein transport of diverse cargos. BML-265 affects Golgi integrity and transport in human cells but not in rodent cells .
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
L-703717 is a NMDA receptor antagonist. L-703717 preferentially binds to cerebellar-specific NMDA receptors consisting of a GluRepsilon3 subunit and eventually accumulates in rodent cerebellum. L-703717 can be used for the research of neurological disease .
Schisandrin B (Standard) is the analytical standard of Schisandrin B. This product is intended for research and analytical applications. Schisandrin B (γ-Schisandrin) is a biphenylcyclooctadiene derivative isolated from Schisandra chinensis and has been shown to have antioxidant effects on the liver and heart of rodents.
VH4127 is a cyclic peptide targeting the low density lipoprotein receptor (LDLR) with a KD of 18 nM for hLDLR. VH4127, bearing non-natural amino acid residues, specifically binds to rodent and human epidermal growth factor (EGF) homology domain of LDLR .
Cligosiban (Standard) is the analytical standard of Cligosiban. This product is intended for research and analytical applications. Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents .
KHK6640 is a humanized anti-amyloid beta oligomer-specific antibody. KHK6640 demonstrates high potency and efficacy for cognitive improvement in several rodent Alzheimer’s models. KHK6640 can be studied in research for neurological diseases such as Alzheimer’s disease .
Itasetron (DA 6215) is a selective 5-HT3 receptor antagonist. Itasetron improves spatial learning and memory abilities in the aged rat. Itasetron has potent antiemetic properties. Itasetron is used for age-related memory degeneration in rodents .
Plenolin is an anticancer agent. Plenolin exhibits inhibitory activity against human epidermoid carcinoma cells. Plenolin shows in vivo antitumor activity against ascites carcinosarcoma and lymphocytic leukemia in rodent models. Plenolin can be used for research related to ascites tumors and leukemia .
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
Sucralose-d6 is deuterium labeled Sucralose. Sucralose?(E955; Trichlorosucrose) is a?non-nutritive?artificial?sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Kisspeptin-10 (mouse, rat) is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10 (mouse, rat) is a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Kisspeptin-10 reduces Methotrexate-induced reproductive toxicity as a potential antioxidant compound .
5,7-Dichlorokynurenic acid (Standard) is the analytical standard of 5,7-Dichlorokynurenic acid (HY-100834). This product is intended for research and analytical applications. 5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
XL413 (BMS-863233) hydrochloride is an orally active and selective CDC7 inhibitor (IC50=3.4 nM). XL413 hydrochloride has favorable pharmacokinetic profiles and significantly inhibits tumor growth in rodent models. XL413 hydrochloride can be used in cancer research .
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
N-Butyl-N-(4-hydroxybutyl)nitrosamine is a potent mutagen that can cause high-level of mutagenesis specifically in the epithelial cells (urothelial) of the urinary bladder. N-Butyl-N-(4-hydroxybutyl)nitrosamine is used to induce bladder cancer in rodents .
DF 461 is a sterol synthase inhibitor with significant inhibitory activity. DF 461 shows high selectivity for the liver and can effectively inhibit cholesterol synthesis in rat liver. DF 461 has shown the effect of lowering plasma lipids in repeated dosing studies in non-rodents .
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
L-Cysteine-d3 is the deuterium labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
UR-12633 is a platelet-activating factor (PAF) antagonist. UR-12633 can effectively reverse hypotension, inhibit coagulation abnormalities, increased vascular permeability, and metabolic disorders in rodent models of endotoxic shock. UR-12633 can be used for research on endotoxic shock .
L-Cysteine-d2 is the deuterium labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
S33138 is a D3 receptor antagonist. S33138 inhibits addiction in animal models of addiction. S33138 reduces cognitive impairment in rodent and primate models of schizophrenia and Parkinson's disease. S33138 can be used in research on neurological disorders such as schizophrenia and Parkinson's disease .
Cetoleic acid is a long-chain monounsaturated fatty acid found in deep-sea fish. Cetoleic acid can promote the synthesis of ALA in human HepG2 cells and EPA in vitro in salmon liver cells, affecting cholesterol levels in rodents. Cetoleic acid has potential applications in cardiovascular disease research .
Sucralose (Standard) is the analytical standard of Sucralose. This product is intended for research and analytical applications. Sucralose?(E955; Trichlorosucrose) is a?non-nutritive?artificial?sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Acifluorfen (Standard) is the analytical standard of Acifluorfen. This product is intended for research and analytical applications. Acifluorfen, a protoporphyrinogen oxidase (PROTOX) inhibitor herbicide, promotes the accumulation of protoporphyrin IX (PPIX), and induces tumors in the rodent liver. Acifluorfen causes strong photooxidative destruction of pigments and lipids in sensitive plant species .
L-Cysteine- 15N is the 15N-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists .
XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms .
GPR119 agonist 2 (compound 43) is an orally active GPR119 agonist. GPR119 agonist 2 shows good pharmacokinetic characteristics in rodents and can effectively improve glucose tolerance in mice and rats. GPR119 agonist 2 has the potential to study type 2 diabetes .
L-Cysteine- 13C3 is the 13C-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
L-Cysteine (Standard) is the analytical standard of L-Cysteine. This product is intended for research and analytical applications. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
L-Cysteine-3- 13C is the 13C-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
L-Cysteine (hydrochloride hydrate) (Standard) is the analytical standard of L-Cysteine (hydrochloride hydrate). This product is intended for research and analytical applications. L-Cysteine hydrochloride hydrate is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride hydrate suppresses ghrelin and reduces appetite in rodents and humans .
Kisspeptin-10 (mouse, rat) TFA is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10 (mouse, rat) TFA is a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Kisspeptin-10 (mouse, rat) TFA reduces Methotrexate-induced reproductive toxicity as a potential antioxidant compound .
DC-015 is a selective and orally active alpha 1-adrenoceptor antagonist on plasma lipid and vascular reactivity in hyperlipidaemic rodent model. DC-015 is a synthesized quinazoline derivative. DC-015 decreases mean arterial pressure in rats. DC-015 has antihypertensive activity .
Regadenoson hydrate (NSC 169186) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson hydrate also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
L-Cysteine-1- 13C is the 13C-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
Folitixorin (5,10-methylenetetrahydrofolate) is a cofactor and an analog of leucovorin. Folitixorin is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research .
Folitixorin calcium is a cofactor and an analog of leucovorin. Folitixorin calcium is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research .
BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease .
SDZ 208-912 is a dual-action 5-HT1A/2 receptor agonist and dopamine D1 receptor antagonist. SDZ 208-912 exhibits partial dopamine agonism and atypical neurosedative effects in rodent models. SDZ 208-912 can be used in research on neurological disorders such as schizophrenia .
L-Cysteine-d3, 15N is the deuterium and 15N-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder .
Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
Tetrachlorohydroquinone (Standard) is the analytical standard of Tetrachlorohydroquinone (HY-W144308). This product is intended for research and analytical applications. Tetrachlorohydroquinone (TCHQ) is a metabolite of Pentachlorophenol. Tetrachlorohydroquinone induces reactive oxidant stress (ROS), inhibits apoptosis and induces necrosis in primary mouse splenocytes. Tetrachlorohydroquinone increases DNA lesions and induces oxidative stress in rodents .
Facinicline (RG3487) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
Nefopam (Fenazoxine) is an orally active, non-opioid and non-steroidal centrally acting analgesic agent. Nefopam blocks voltage-sensitive sodium channels (IC50=27 μM) and modulates glutamatergic transmission in rodents. Nefopam can be used in studies of neuropathic pain, anticonvulsant, as well as the prevention of postoperative shivering and hiccups .
Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively. Monocrotaline has antitumor activity and is cytotoxic to hepatocellular carcinoma cells. Monocrotaline is used to induce a model of pulmonary hypertension in rodents. [2][6][8].
GEBR-7b is a selective PDE4D inhibitor with an IC50 of 0.67 μM. GEBR-7b increases hippocampal cAMP and does not influence Aβ levels in rodents. GEBR-7b also improves spatial and can be used for the study of cognitive deficits .
L-Cysteine- 13C3, 15N is the 13C- and 15N-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
GLUT4 activator 2 (C59) is an insulin sensitizer, which can be used for research of diabetic diseases. GLUT4 activator 2 improves glucose uptake and insulin sensitivity in rodents. GLUT4 activator 2 interacts with Unc119 and Unc119B resulting in increased insulin sensitivity and GLUT4 translocation .
Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively. Monocrotaline has antitumor activity and is cytotoxic to hepatocellular carcinoma cells. Monocrotaline is used to induce a model of pulmonary hypertension in rodents. .
VU0650786 (Standard) is the analytical standard of VU0650786 (HY-108710). This product is intended for research and analytical applications. VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .
JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .
Sucralose (GMP Like) (E955 (GMP Like)) is the GMP Like class Sucralose (HY-N0614) that can be used as pharmaceutical excipients. Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Luvadaxistat (TAK-831) is an orally active, highly selective, potent D-amino acid oxidase (DAAO) inhibitor. Luvadaxistat inhibits oxidative deamination of D-serine via the human recombinant DAAO enzyme with an IC50 of 14 nM. Luvadaxistat significantly increases D-serine levels in the rodent brain, plasma, and cerebrospinal fluid. Luvadaxistat has the potential for schizophrenia research .
Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
Etifoxine (hydrochloride) (Standard) is the analytical standard of Etifoxine (hydrochloride). This product is intended for research and analytical applications. Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
Antifungal agent 96 (Compound WZ-2) is an antifungal agent with good blood-brain barrier permeability and brain penetration. Antifungal agent 96 inhibits the growth of C. neoformans H99 and C. albicans 0304103 with MIC values of 0.016 and 32 μg/mL, respectively .
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity . Talampanel (IVAX) has neuroprotective effects in rodent stroke models . Talampanel attenuates caspase-3 dependent apoptosis in mouse brain .
Flubendazole-d3 is the deuterium labeled Flubendazole. Flubendazole is a safe and efficacious anthelmintic agent, which is widely used for anthelmintic to human, rodents and ruminants. Flubendazole exerts anticancer activities by mechanisms including inhibition of microtubule function. Flubendazole induces p53-mediated apoptosis and arrests G2/M cell cycle .
MRT-92 is a Smoothened (Smo) antagonist (Ki=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC50=0.4 nM). MRT-92 can be used in the study of cerebellar glioma .
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases .
Nitrilotriacetic acid is an orally active chelating agent for metal ions. Nitrilotriacetic acid is an aminotricarboxylic acid that can sequester metal ions as water soluble complexes. Nitrilotriacetic acid reacts with strong oxidizing agents such as hypochlorite, chlorine, ozone, or oxygen in the presence of palladium/carbon catalyst. Nitrilotriacetic acid interacts with solid phases such as cell membranes and bone matrices in the mammalian system. Nitrilotriacetic acid is classified as an epigenetic rodent carcinogen .
(6R)-ML753286 is an isomer of ML753286 (HY-116494). ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents .
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
Anti-iNKT Cell Antibody (6B11) recognizes an epitope on T cell receptor (TCR) V alpha 24-J alpha 18. Anti-iNKT Cell Antibody is specific for cloned and primary human but not rodent iNKT and the human invariant TCR-α. Recommend Isotype Controls: Mouse IgG1 kappa, Isotype Control (HY-P99977) .
EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
BMS-955829 is an orally active and selective mGluR5 positive allosteric modulator with an EC50 of 2.6 nM. BMS-955829 has no intrinsic agonist activity and a low glutamate fold shift (2.4). BMS-955829 can effectively improve cognitive and executive function deficits in rodents. BMS-955829 can be used in the research of cognitive impairment diseases such as schizophrenia .
CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease .
Crobenetine hydrochloride (BIII-890 hydrochloride) is the hydrochloride form of Crobenetine (HY-16923). Crobenetine hydrochloride is a selective inhibitor for Na + channel. Crobenetine hydrochloride displaces 3HBTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, exhibits only low binding affinity for other receptors and ion channels. Crobenetine hydrochloride protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
Regadenoson (Standard) is the analytical standard of Regadenoson. This product is intended for research and analytical applications. Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents .
ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM) . ML 145 has no significant activity for GPR35 at either rodent ortholog .
MKP10241 is an orally active GPR119 agonist. MKP10241 elevates cAMP levels in the GPR119 expressing cell line (EC50: 3.7 nM). MKP10241 reduces blood glucose levels and HbA1c in acute models and a chronic diabetic mouse model. MKP10241 also demonstrates excellent preclinical efficacy in acute as well as chronic rodent models of obesity, and MASH .
MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
AZ12943203 (Compound 13e) is a GSK-3 PET radioligand with a Kd of 2.94 nM. AZ12943203 has a significant inhibitory potency toward GSK-3β (IC50 : 4.44 nM), and can specifically bind to GSK-3-rich regions of the rodent brain. AZ12943203 can be used for neurodegenerative diseases imaging, particularly Alzheimer’s disease .
PAOPA (Standard) is the analytical standard of PAOPA (HY-103423). This product is intended for research and analytical applications. PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists .
Rifabutin-vonoprazan conjugate 1 is an orally active acid-responsive bifunctional molecule. Rifabutin-vonoprazan conjugate 1 exhibits anti-Helicobacter pylori activity (MIC ≤ 0.125 μg/mL) and acid-suppressive effects (acid inhibition rate > 85% at a dose of 2 mg/kg). Rifabutin-vonoprazan conjugate 1 also demonstrates anti-ulcer activity. Rifabutin-vonoprazan conjugate 1 can be used in research related to Helicobacter pylori infection and gastric ulcer .
SB-236057 is an inverse agonist of the 5-HT1B receptor that exhibits strong skeletal teratogenicity in rodents and rabbits. SB-236057 affects gene expression during embryonic development through interference with the Notch signaling pathway and interaction with r-esp1. SB-236057 induces somatic patterning and tail extension defects in rat embryos during early organogenesis .
IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy .
ST4070 is a potent, orally active, and selective reversible fatty acid amide hydrolase (FAAH) inhibitor. ST4070 increases endocannabinoid (eCB) brain levels and counteracts neuropathic pain in animal models. ST4070 enhances the endogenous eCB tone in specific brain regions engaged in emotional control, and induces remarkable anxiolytic-like behaviours in rodents. ST4070 can be used for neuropathic pain and anxiety disorders research .
Dipropylene glycol is a mixture of three structural isomers (2-(2-hydroxypropoxy)-1-propanol, 1,1'-oxybis (2-propanol), and 2,2'-oxybis (1-propanol)), and is also a toxic substance used in plasticizers, polyester resins, cosmetics, fragrances, polyurethane polyols, and alkyd resins. Dipropylene glycol induces liver and kidney damage as well as reproductive toxicity in rodents .
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na + channels and N-type Ca 2+ channels, and is effective as a K + channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM) .
COX-2-IN-48 (5-25), a COX-2 inhibitor with an IC50 of 51.7 nM for human COX-2, exerts anti-inflammatory and analgesic effects in various rodent models by inhibiting NF-κB pathway. COX-2-IN-48 (5-25) inhibits the degradation of IκB, the phosphorylation and nuclear translocation of NF-κB p65, and the expression of COX-2 and iNOS .
GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats .
AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals .
GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats .
JNJ-61432059 is a blood-brain barrier-permeable, orally active TARP γ-8-associated AMPAR modulator with anticonvulsant activity. JNJ-61432059 negatively regulates GluA1 and positively modulates GluA2-containing AMPARs. JNJ-61432059 exerts potent protective effects in rodent epilepsy models. JNJ-61432059 is applicable for epilepsy-related research .
WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease .
Crobenetine (BIII-890), a benzomorphan derivative, is a potent, selective, and highly use-dependent Na + channel blocker. Crobenetine displaces [3H]BTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, yet exhibits only low binding affinity for other receptors and ion channels. Crobenetine protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
SSTR4 agonist 4 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 4 has the potential for the research of pain (extracted from patent WO2021233428A1, compound 14) .
Facinicline hydrochloride (Standard) is the analytical standard of Facinicline (hydrochloride) (HY-108057A). This product is intended for research and analytical applications. Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models .
APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease .
AMG 837 is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 can be used in research related to type 2 diabetes and brucellosis .
Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
L-Cysteine (Cysteine) is an orally active conditionally essential amino acid with hypoglycemic effects, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine promotes the proliferation and differentiation of neural stem cells via the CBS/H2S pathway. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans. L-Cysteine can be used as an anorectic agent .
Nitrilotriacetic acid (Standard) is the analytical standard of Nitrilotriacetic acid. This product is intended for research and analytical applications. Nitrilotriacetic acid is an orally active chelating agent for metal ions. Nitrilotriacetic acid is an aminotricarboxylic acid that can sequester metal ions as water soluble complexes. Nitrilotriacetic acid reacts with strong oxidizing agents such as hypochlorite, chlorine, ozone, or oxygen in the presence of palladium/carbon catalyst. Nitrilotriacetic acid interacts with solid phases such as cell membranes and bone matrices in the mammalian system. Nitrilotriacetic acid is classified as an epigenetic rodent carcinogen .
AMG 837 sodium salt is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 sodium salt stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 sodium salt binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 sodium salt can be used in research related to type 2 diabetes and brucellosis .
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14) .
(S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
JNJ-47965567 (Standard) is the analytical standard of JNJ-47965567 (HY-101418). This product is intended for research and analytical applications. JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
NIAID RSVF2-5 is a human monoclonal antibody fragment. NIAID RSVF2-5 binds to conserved, distinct conformational epitopes on RSV fusion glycoprotein, and shows activity against RSVsubgroup A and B strains. NIAID RSVF2-5 reduces pulmonary and lung viral titers in RSV-infected rodents. NIAID RSVF2-5 can be used for the research of respiratory syncytial virus infection .
Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with Ki values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain .
Padsevonil (Standard) is the analytical standard of Padsevonil (HY-109009). This product is intended for research and analytical applications. Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
Nitromemantine (NitroSynapsin) is a nitrate derivative of Memantine (HY-B0591) and is a dual-functional NMDAR antagonist. Nitromemantine exhibits significant efficacy in rodent models of cerebral infarction through a dual mechanism of blocking channels and regulating receptors via NO/redox regulation. Nitromemantine can target ischemic neurons under hypoxic conditions and enhance its activity. Nitromemantine inhibits the current induced by NMDA, with its IC50 being 2.4 μM. Nitromemantine can be used for the study of cerebral ischemic stroke .
CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents . Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension .
RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages .
2-(Tetradecylthio)acetic acid (Standard) is the analytical standard of 2-(Tetradecylthio)acetic acid. This product is intended for research and analytical applications. 2-Tetradecylthio acetic acid is a pan-peroxisome proliferator activated receptor (pan-PPAR) activator. 2-Tetradecylthio acetic acid induces hypolipidemia. 2-Tetradecylthio acetic acid reduces plasma lipids and enhances hepatic fatty acid oxidation in rodents. 2-Tetradecylthio acetic acid increases the expression of genes involved in fatty acid uptake, activation, accumulation, and oxidation .
DMT1 blocker 1 is an orally active blocker of divalent metal transporter 1 (DMT1) with an IC50 of 0.64 μM. DMT1 blocker 1 inhibits intestinal cell absorption of non-heme iron, thereby alleviating iron overload by blocking the DMT1 transporter. DMT1 blocker 1 demonstrates significant efficacy in rodent models of acute iron hyperabsorption. DMT1 blocker 1 is useful for studying iron overload disorders such as hereditary hemochromatosis and thalassemia .
AMG 837 calcium hydrate is an orally active, selective GPR40/FFA1 agonist with an EC50 of 1.5 nM against human GPR40. AMG 837 calcium hydrate stimulates insulin secretion in a glucose-dependent manner, and effectively improves glycemic control in both normal and diabetic rodent models . AMG 837 calcium hydrate binds to the BacA protein and impairs the survival and replication of Brucella. AMG 837 calcium hydrate can be used in research related to type 2 diabetes and brucellosis .
L-Cysteine hydrochloride is an orally active conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride suppresses ghrelin and reduces appetite in rodents. L-Cysteine hydrochloride inhibits Aspergillus flavus growth and AFB synthesis by disrupting cell structure and antioxidant system balance. L-Cysteine hydrochloride enhances relaxant responses of rat aortic rings to NO and reduces responses to endothelium-derived relaxing factor (EDRF) .
MOG (35-55), human is a component of CNS myelin. MOG (35-55), human is different from mMOG (35-55) by a proline for serine substitution at position 42. MOG (35-55), human is also immunogenic via bind to H-2b class II MHC and recognized by T cells, but not encephalitogenic, and is only partially cross-reactive with mMOG35–55. MOG (35-55), human induces minimal clinical signs of EAE relative to the rodent peptide .
V-0219 hydrochloride is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 hydrochloride potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 hydrochloride potentiates glucose-dependent insulin secretion. V-0219 hydrochloride improves glucose handling in normal and diabetic rodents. V-0219 hydrochloride can be used for the research of obesity-associated diabetes .
CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease .
V-0219 is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 potentiates glucose-dependent insulin secretion. V-0219 improves glucose handling in normal and diabetic rodents. V-0219 can be used for the research of obesity-associated diabetes .
JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a Ki of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures .
ML 145 (Standard) is the analytical standard of ML 145 (HY-107536). This product is intended for research and analytical applications. ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM) . ML 145 has no significant activity for GPR35 at either rodent ortholog .
(S,S)-TAK-418 is a potent inhibitor of lysine-specific demethylase 1 (LSD1), demonstrating significant normalization of aberrant gene expression in neurodevelopmental disorders. (S,S)-TAK-418 also ameliorates ASD-like behaviors in rodent models affected by maternal exposure to valproate or poly I:C. (S,S)-TAK-418 modulates gene expression differently across various models and ages, indicating its potential as a therapeutic agent for conditions like autism spectrum disorder and schizophrenia.
A-423579 is an orally active non-imidazole histamine H3 receptor antagonist. A-423579 exhibits high affinity and good selectivity for human and rat H3 receptors, and possesses both antagonistic and inverse agonistic activities. A-423579 can effectively reduce body weight in obese rodents, with concomitant decreases in fat content, plasma leptin levels, and triglycerides. A-423579 possesses anti-obesity activity and can be used in the research of obesity and related metabolic disorders .
Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain .
Satranidazole-d3 is the deuterium labeled Satranidazole. Satranidazole is an orally active insecticide and antimicrobial agent with high electron affinity. Satranidazole forms reduced nitro intermediates, which interact with DNA, causing helix instability, strand breakage and release of thymidine derivatives. Satranidazole exhibits antitrichomonal activity against Trichomonas vaginalis and Trichomonas foetus, and antiamoebic activity in rodent models of hepatic amoebiasis and caecal amoebiasis. Satranidazole inhibits the replication of bacteriophage φX174 DNA. Satranidazole can be used in research related to caecal amoebiasis, trichomoniasis and anaerobic bacterial infections.
(S)-Padsevonil (Standard) is the analytical standard of (S)-Padsevonil (HY-109009A). This product is intended for research and analytical applications. (S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma .
Soclenicant (BNC210) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. Soclenicant exhibits acute anxiolytic activity in rodent models of anxiety. Soclenicant inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987 (HY-12560A) with IC50 values in the range of 1.2 to 3 μM. Soclenicant can be used in studies of anxiety, trauma, and stressor-related disorders .
Remogliflozin etabonate-d7 (GSK189075-d7) is the deuterium labeled Remogliflozin etabonate. Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models .
L-Cysteine (hydrochloride) (Standard) is the analytical standard of L-Cysteine (hydrochloride). This product is intended for research and analytical applications. L-Cysteine hydrochloride is an orally active conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride suppresses ghrelin and reduces appetite in rodents. L-Cysteine hydrochloride inhibits Aspergillus flavus growth and AFB synthesis by disrupting cell structure and antioxidant system balance. L-Cysteine hydrochloride enhances relaxant responses of rat aortic rings to NO and reduces responses to endothelium-derived relaxing factor (EDRF) [4].
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents .
Guanosine 5'-O-(2-thiodiphosphate) trisodium (GDPβS trisodium) is a non-hydrolyzable derivative of GDP. Guanosine 5'-O-(2-thiodiphosphate) trisodium acts as an inhibitor of adenylyl cyclase (AC) with a Ki value of 600 nM. In the absence of glutamic-pyruvic transaminase (GPT) in cerebral cortex membranes of rodent models, Guanosine 5'-O-(2-thiodiphosphate) trisodium partially activates AC with an EC50 of 400 nM. Guanosine 5'-O-(2-thiodiphosphate) trisodium prevents norepinephrine-induced nitric oxide release in ventricular myocytes .
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .
Epyrifenacil is a protoporphyrinogen oxidase (PPO) inhibiting herbicide, potently targeting the PPO2 isoform from weeds such as Amaranthus palmeri with an IC50 of 0.637 nM. Epyrifenacil also inhibits liver mitochondrial PPO across species, with IC50 values of 2.2 nM (mouse), 2.6 nM (rat), 12.1 nM (rabbit), 7.6 nM (dog), and 10.2 nM (human). Epyrifenacil induces liver tumor development in mice. Epyrifenacil can be used for weed control, and also used as a tool compound in toxicological research to study the mechanism of PPO inhibition, chemical-induced hepatotoxicity, and the mode of action of non-genotoxic carcinogens in rodents[3].
DNDI-6174 is an orally active Leishmaniacytochrome b (Qi site of cytochrome bc1 complex/complex III) inhibitor. DNDI-6174 binds to the Qi site of Leishmania cytochrome b, inhibits cytochrome bc1 complex activity in the parasite's electron transport chain across promastigote and axenic amastigote stages. DNDI-6174 reduces parasite burden in rodent models, inhibits growth of various Leishmania species, drug-resistant clinical isolates, and Trypanosoma cruzi, with marginal activity against Trypanosoma brucei. DNDI-6174 can be used for the research of visceral leishmaniasis, cutaneous leishmaniasis .
CMF019 (Standard) is the analytical standard of CMF019 (HY-103080). This product is intended for research and analytical applications. CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents . Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension .
Talaglumetad is an orally active prodrug of Eglumegad (HY-18941) and a metabotropic glutamate receptor 2/3 (mGluR2/3) agonist. Talaglumetad undergoes transmembrane transport via the intestinal peptide transporter hPepT1, and is enzymatically hydrolyzed to produce L-alanine and the parent drug Eglumegad after entering the body. Talaglumetad can be used in research related to metabotropic glutamate receptor 2-associated neurological systems .
GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
HUHS2002 is a free fatty acid derivative with the ability to enhance α7 cholinergic receptor activity. HUHS2002 enhances whole-cell membrane currents of α7 ACh receptors expressed in Xenopus oocytes in a concentration-dependent manner. The effects of HUHS2002 were blocked in the presence of the Ca2 /calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93. HUHS2002 activated CaMKII in cultured rodent hippocampal neurons, and this activation was abolished by KN-93. HUHS2002 also partially inhibited the activity of protein phosphatase 1 (PP1) in a cell-free PP1 activity assay .
Saccharin sodium is an orally active, non-caloric artificial sweetener (NAS). Saccharin sodium has bacteriostatic and microbiome-modulating properties. Saccharin binds to and signals via specific taste receptors, not only in the oral cavity but also alongside the gastrointestinal tract. Saccharin has been reported to bind the human and rodent heteromeric guanine nucleotide-binding protein (G protein) coupled sweet taste receptors T1R2/T2R3 as well as the human bitter taste receptor T2R43 and T2R44. Saccharin can inhibit bacterial growth in vitro .
Saviprazole (HOE-731) is a H +,K +-ATPase inhibitor. Saviprazole inhibits gastric acid secretion. Saviprazole inhibits histamine- and dbcAMP-stimulated [ 14C]aminopyrine uptake, dbcAMP-induced oxygen consumption. Saviprazole can be used in research related to gastrointestinal diseases, such as gastric ulcers and acid reflux .
Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
AMG 9090 is characterized as a compound that acts as a partial agonist of rat TRPA1 channels, demonstrating pharmacological activity in pain and inflammation models. TRPA1 is pivotal in sensing reactive compounds, triggering pain responses in humans and rodents. AMG 9090, along with other trichloro(sulfanyl)ethyl benzamides (TCEB compounds), shows differential effects on human and rat TRPA1 channels: it acts as a potent antagonist of human TRPA1 activated by AITC and noxious cold, whereas it behaves as a partial agonist at rat TRPA1. This suggests AMG 9090's potential as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitory activity against TRPM8 noted .
PF-03475952 is a fully human IgG2 monoclonal antibody targeting CD44. PF-03475952 binds an epitope in CD44’s constant exons, blocks CD44-hyaluronic acid interaction, reduces cell surface CD44, and does not cross-react with rodentCD44 or LYVE-1. PF-03475952 induces cancer cell apoptosis, inhibits LPS (HY-D1056)-induced leukocyte cytokine release and cancer metastasis, and reduces CD44 expression on circulating CD3+ lymphocytes in cynomolgus monkeys. PF-03475952 can be used for the research of rheumatoid arthritis and hepatocellular carcinoma .
L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 can be used for the study of chronic orofacial pain .
L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 hydrochloride mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 hydrochloride blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 hydrochloride reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 hydrochloride can be used for the study of chronic orofacial pain .
Poricoic acid A can be isolated from Poria cocos. Poricoic acid A is an orally active anti-tumor agent. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis. Poricoic acid A also attenuatea fibroblast activation and abnormal extracellular matrix remodeling in renal fibrosis by activating AMPK and inhibiting Smad3. Poricoic acid A significantly reduces the magnitude of rise in serum creatinine and urea levels in rat model when combined with Melatonin. Poricoic acid A ameliorates renal fibrosis and podocyte injury by attenuating oxidative stress and inflammation through regulating NF-κB and Nrf2 in IRI rodent model in combination with Melatonin .
Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions .
Isosorbide di-(methyl fumarate) (IDMF), topical DMF (HY-17363) derivative, is an NRF2/ARE pathway activator. Isosorbide di-(methyl fumarate) downregulates ANCR targets, modulates epithelial differentiation, represses proinflammatory cytokine genes, IL-17A- and TNF-induced keratinocyte genes, psoriatic skin lesion-specific genes, and immune response genes. Isosorbide di-(methyl fumarate) stimulates oxidative stress response gene transcription, reduces erythema and scaling in Imiquimod (HY-B0180)-induced psoriasiform lesions. Isosorbide di-(methyl fumarate) exhibits no genotoxicity or radiation sensitivity in skin fibroblasts, is nonirritating and nonsensitizing in rodent models. Isosorbide di-(methyl fumarate) can be used for the research of psoriasis vulgaris .
SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .
Alpidem (Standard) is the analytical standard of Alpidem (HY-W013150). This product is intended for research and analytical applications. Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
SB-277011 hydrochloride (Standard) is the analytical standard of SB-277011 (hydrochloride) (HY-10847B). This product is intended for research and analytical applications. SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .
(S,S)-SARM1-IN-9 (Compound MY-13A) is a stereoselective SARM1 inhibitor with covalent binding properties. (S,S)-SARM1-IN-9 covalently modifies Cys311 in the autoregulatory ARM domain of wild-type SARM1, thereby blocking NADase activity, without inhibiting the SARM1C311A or SARM1C311S mutants. (S,S)-SARM1-IN-9 blocks vacor- and vincristine-induced axon degeneration in primary rodent dorsal root ganglion neurons. (S,S)-SARM1-IN-9 can be used for research on axon degeneration-dependent neurological disorders, including chemotherapy-induced peripheral neuropathy .
SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .
THIQ (Standard) is the analytical standard of THIQ (HY-10624). This product is intended for research and analytical applications. THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
Alpidem-d14 is the deuterium labeled Alpidem (HY-W013150) . Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
Saccharin (sodium) (Standard) is the analytical standard of Saccharin (sodium). This product is intended for research and analytical applications. Saccharin sodium is an orally active, non-caloric artificial sweetener (NAS). Saccharin sodium has bacteriostatic and microbiome-modulating properties. Saccharin binds to and signals via specific taste receptors, not only in the oral cavity but also alongside the gastrointestinal tract. Saccharin has been reported to bind the human and rodent heteromeric guanine nucleotide-binding protein (G protein) coupled sweet taste receptors T1R2/T2R3 as well as the human bitter taste receptor T2R43 and T2R44. Saccharin can inhibit bacterial growth in vitro .
Cabotamig is a humanized bispecific T-cell engager antibody targeting CDH17/CD3. Cabotamig is generated from anti-CDH17 monoclonal ARB102 by linking a CD3-binding scFv in the format of IgG4-scFv. Cabotamig can be used for the research of cancer, such as gastric cancer and colon cancers .
Liquid Paraffin is a petroleum-derived mixture of saturated hydrocarbons and an orally active fecal lubricant. Liquid Paraffin is widely used in studies of constipation and fecal incontinence in children through its lubricating effect and the osmotic effect generated by its conversion to hydroxy fatty acids. Liquid Paraffin has high safety, is non-carcinogenic, and does not affect fat-soluble vitamin levels with long-term use. Liquid Paraffin does not cause abdominal pain or electrolyte disorders, but may lead to lipoid pneumonia and granulomas caused by rectal administration. Liquid Paraffin can also be used as a phase change material for thermal energy storage, or combined with nanoparticles to form a protective boundary film to reduce mechanical wear .
Calonysterone is an orally effective IL-6 inhibitor. Calonysterone reduces the level of the proinflammatory cytokine IL-6. Calonysterone prevents diet-induced obesity. Calonysterone normalizes abnormal plasma adiponectin and leptin concentrations. Calonysterone increases the percentage of total DNA methylation. Calonysterone enhances antioxidant activity. Calonysterone is applicable to obesity-related research .
Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain .
Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
Tigemonam is an orally active monobactam antibiotic with a Ki of 0.86 μM against Enterobacter cloacae P99 β-lactamase and 50.8 μM against Escherichia coli TEM-1 β-lactamase. Tigemonam binds to penicillin-binding proteins 1a, 3, and 4, inhibits bacterial cell wall synthesis, and exhibits bactericidal activity against aerobic gram-negative bacteria including Enterobacteriaceae, Haemophilus influenzae, and Neisseria gonorrhoeae. Tigemonam resists hydrolysis by multiple β-lactamase enzymes, reduces bacterial load in systemic, pyelonephritic, lung, and thigh muscle infections in rodents, and shows minimal difference between minimum inhibitory and bactericidal concentrations. Tigemonam can be used for the research of gram-negative bacterial infections, acute pyelonephritis, lung infection, and thigh muscle infection .
GSK1034702 (Standard) is the analytical standard of GSK1034702 (HY-107111). This product is intended for research and analytical applications. GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
FRM-024 is a central nervous system-penetrant, orally active γ-secretase modulator and Aβ42 lowering agent. FRM-024 is used for the research of familial Alzheimer's disease .
Unifiram (DM232) is a AMPA receptor activator and cognitive enhancer. Unifiram activates the AMPA-mediated neurotransmission system. Unifiram reverses NBQX-induced amnesia in the passive avoidance test in mice. Unifiram reverses the antagonistic effect of kynurenic acid on NMDA-mediated [ 3H]NA release in rat hippocampal slices. Unifiram enhances excitatory synaptic transmission in the rat hippocampus in vitro. Unifiram can be used in studies related to amnesia and cognitive dysfunction, including age-related memory decline, neurodegenerative diseases such as Alzheimer's disease or Parkinson's disease, multiple sclerosis, schizophrenia, and attention deficit hyperactivity disorder .
VU6015241 is a selective, blood-brain barrier-permeable M4 mAChR Antagonist with a Ki value of 43.3 nM. VU6015241 is used for the research of dystonia and related movement disorders .
Alixorexton (ALKS 2680) is an orally bioavailable, blood-brain barrier-permeable OX2R-selective activator and wake-promoting agent. Alixorexton can be used for the research of narcolepsy and idiopathic hypersomnia .
SGK1-IN-3 hydrochloride (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 hydrochloride blocks the activity of CDK family members. SGK1-IN-3 hydrochloride serves as a P-glycoprotein substrate. SGK1-IN-3 can be used for the research of osteoarthritis .
CP94253 hydrochloride is an orally active, brain-penetrant and selective 5-HT1B receptor agonist with an Ki of 2 nM. CP94253 hydrochloride induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 hydrochloride can be used for the research of depression and heightened aggressive behavior .
CP94253 is an orally active, brain-penetrant and selective 5-HT1B receptor agonist with an Ki of 2 nM. CP94253 induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 can be used for the research of depression and heightened aggressive behavior .
MEDICA16 is an orally active acetyl-CoA carboxylase and ATP-citrate lyase inhibitor. MEDICA16 limits the acetyl-CoA supply for acetyl-CoA carboxylase, inhibits acetyl-CoA carboxylase activity, exerts citrate-competitive inhibitory effects on ATP-citrate lyase, and reduces hepatic AMPK activity. MEDICA16 can be used in research related to insulin resistance, hyperlipidemia, and obesity .
SGK1-IN-3 (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 blocks the activity of CDK family members. SGK1-IN-3 is a P-glycoprotein substrate. SGK1-IN-3 can be used for research on osteoarthritis .
SARM1-IN-9 (Compound MY-13B) is a stereoselective SARM1 inhibitor. SARM1-IN-9 is applicable to research related to axon degeneration-dependent neurological diseases .
S217879 is an orally active and selective NRF2 activator. S217879 activates the NRF2 pathway by specifically disrupting the KEAP1 (Kd: 4.15 nM)-NRF2 interaction, and upregulates the antioxidant response. S217879 also ameliorates steatohepatitis and reduces the degree of liver fibrosis. S217879 can be used in the research of metabolic dysfunction-associated steatotic liver disease and nonalcoholic steatohepatitis .
KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a Ki value of 5.3 nM for human KOR, and EC50 values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research .
WAY 163909 is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 exhibits an EC50 of 8 nM and a Ki of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia .
CM398 is a highly selective, orally active Sigma-2 receptor ligand with a Ki value of 0.43 nM. CM398 ameliorates age-related macular degeneration. CM398 exerts analgesic effects on visceral pain, inflammatory pain and neuropathic pain. CM398 can be used in research related to age-related macular degeneration, neuropathic pain and inflammatory pain .
AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC50 of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus .
Sulfamethazine (Sulfadimidine) 100 µg/mL in acetonitrile is a brain-penetrant sulfonamide antibiotic. Sulfamethazine 100 µg/mL in acetonitrile inhibits bacterial growth by blocking the synthesis of folic acid. Sulfamethazine 100 µg/mL in acetonitrile can be used for research on bacterial infections .
AZD3676 is an orally active and blood-brain barrier-permeable ligand for 5-HT1A and 5-HT1B receptors, with nanomolar binding affinity for human and monkey receptors (human 5-HT1A: 0.16 nM, monkey 5-HT1A: 0.13 nM, human 5-HT1B: 2.3 nM, monkey 5-HT1B: 2.4 nM). AZD3676 is applicable to research related to cognitive impairment in Alzheimer's disease .
di-Ellipticine-RIBOTAC is a RNase recruiting chimera (RIBOTAC) degrader, capable of specifically binding and degrading expanded G4C2 RNA repeat (r(G4C2) exp). di-Ellipticine-RIBOTAC selectively binds the three-dimensional (3D) structure formed by r(G4C2) exp and that recruits an endogenous ribonuclease (RNase) to cleave r(G4C2) exp. di-Ellipticine-RIBOTAC selectively degrades the mutant chromosome 9 open reading frame 72 (C9orf72) allele and reduces quantities of toxic dipeptide repeat proteins (DPRs) translated from r(G4C2) exp. di-Ellipticine-RIBOTAC significantly improves the pathological phenotype of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) in cells and mouse models. di-Ellipticine-RIBOTAC can be used for the study of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) .
di-Ellipticine-RIBOTAC TFA is a RNase recruiting chimera (RIBOTAC) degrader, capable of specifically binding and degrading expanded G4C2 RNA repeat (r(G4C2) exp). di-Ellipticine-RIBOTAC TFA selectively binds the three-dimensional (3D) structure formed by r(G4C2) exp and that recruits an endogenous ribonuclease (RNase) to cleave r(G4C2) exp. di-Ellipticine-RIBOTAC TFA selectively degrades the mutant chromosome 9 open reading frame 72 (C9orf72) allele and reduces quantities of toxic dipeptide repeat proteins (DPRs) translated from r(G4C2) exp. di-Ellipticine-RIBOTAC TFA significantly improves the pathological phenotype of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) in cells and mouse models. di-Ellipticine-RIBOTAC TFA can be used for the study of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) .
Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate . Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents .
1-Methylpyrene is a ubiquitous environmental pollutant and rodent carcinogen. Its mutagenic activity depends on sequential activation by various CYP and sulfotransferase (SULT) enzymes. 1-Methylpyrene induces chromosome loss and mitotic disturbance, proba
Sucralose (GMP Like) (E955 (GMP Like)) is the GMP Like class Sucralose (HY-N0614) that can be used as pharmaceutical excipients. Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Lipid 5 is an amino lipid that affords efficient mRNA delivery in rodent and primate models. Lipid 5 shows optimal pharmacokinetics and non-toxic side effects .
Sucralose (GMP Like) (E955 (GMP Like)) is the GMP Like class Sucralose (HY-N0614) that can be used as pharmaceutical excipients. Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
MOG (35-55), human is a component of CNS myelin. MOG (35-55), human is different from mMOG (35-55) by a proline for serine substitution at position 42. MOG (35-55), human is also immunogenic via bind to H-2b class II MHC and recognized by T cells, but not encephalitogenic, and is only partially cross-reactive with mMOG35–55. MOG (35-55), human induces minimal clinical signs of EAE relative to the rodent peptide .
VH4127 TFA is a cyclic peptide targeting the low density lipoprotein receptor (LDLR) with a KD of 18 nM for hLDLR. VH4127 TFA specifically binds to rodent and human epidermal growth factor (EGF) homology domain of LDLR .
Kisspeptin-10 (mouse, rat) is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10 (mouse, rat) is a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Kisspeptin-10 reduces Methotrexate-induced reproductive toxicity as a potential antioxidant compound .
Kisspeptin-10 (mouse, rat) TFA is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10 (mouse, rat) TFA is a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Kisspeptin-10 (mouse, rat) TFA reduces Methotrexate-induced reproductive toxicity as a potential antioxidant compound .
m3-Huwentoxin IV (m3-HwTx-IV) is a potent NaV inhibitor with IC50s of 3.3, 6.8, 7.2, 8.4, 11.9 and 369 nM against hNaV1.7, hNaV1.6, hNaV1.3, hNaV1.1, hNaV1.2 and hNaV1.4, respectively in QPatch assay. m3-Huwentoxin IV dose-dependently suppresses spontaneous pain induced by the NaV1.7 activator OD1 in a rodent pain model .
Prokineticin 2 Isoform 2 (human) is a hypothalamic neuropeptide. Prokineticin 2 Isoform 2 (human) decreases food intake and involves in thermoregulation and energy metabolism in rodents. Prokineticin 2 has the potential for the research of hyperglycemia, metabolic syndrome (MetS) and obesity .
VH4127 is a cyclic peptide targeting the low density lipoprotein receptor (LDLR) with a KD of 18 nM for hLDLR. VH4127, bearing non-natural amino acid residues, specifically binds to rodent and human epidermal growth factor (EGF) homology domain of LDLR .
Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
Connexin mimetic peptide 40,37GAP26 is a biological active peptide. (This peptide corresponds to the GAP26 domain of the extracellular loop of the major vascular connexins (Cx37, Cx40), designated as 37, 40Gap 26 according to Cx homology. It was used to investigate the role of gap junctions in the spread of endothelial hyperpolarizations evoked by cyclopiazonic acid (CPA) through the wall of the rodent iliac artery. The gap junction plaques constructed from Cx37 and Cx40 were abundant in the endothelium. This peptide provides inhibitory effects against subintimal hyperpolarization.)
R9-13 is a fatty acid-conjugated relaxin and an agonist of LGR7 (RXFP1). R9-13 induces sustained pubic symphysis elongation in estrogen-pretreated mice. R9-13 exhibits long-acting pharmacokinetic profiles in rodents, with in vivo activity lasting up to one week after administration. R9-13 can be used in studies related to acute heart failure .
Obestatin(11-23)mouse, rat is a polypeptide involved in regulating energy balance and inhibiting eating. Obestatin(11-23)mouse, rat causes reduced food intake, body weight, and jejunal contractions in rodents .
Cabotamig is a humanized bispecific T-cell engager antibody targeting CDH17/CD3. Cabotamig is generated from anti-CDH17 monoclonal ARB102 by linking a CD3-binding scFv in the format of IgG4-scFv. Cabotamig can be used for the research of cancer, such as gastric cancer and colon cancers .
KHK6640 is a humanized anti-amyloid beta oligomer-specific antibody. KHK6640 demonstrates high potency and efficacy for cognitive improvement in several rodent Alzheimer’s models. KHK6640 can be studied in research for neurological diseases such as Alzheimer’s disease .
KY1070 is a fully human anti-BMP6 antibody with a Kd of 0.00014 μM against the human BMP6. It exhibits high specificity for BMP6, showing no cross-reactivity with other members of the BMP family, and effectively inhibits BMP6-induced BMP receptor heterodimerization and hepcidin expression. KY1070 modulates Ferroportin expression on erythroid progenitor cells and accelerates erythropoiesis. In rodent anemia models, KY1070 reduces the required dose of erythropoietin (EPO) when used in combination with EPO and enhances the responsiveness of mice with chronic kidney disease (CKD)-associated anemia to EPO treatment. KY1070 is applicable for research on anemia of chronic disease [1] [2].
Anti-iNKT Cell Antibody (6B11) recognizes an epitope on T cell receptor (TCR) V alpha 24-J alpha 18. Anti-iNKT Cell Antibody is specific for cloned and primary human but not rodent iNKT and the human invariant TCR-α. Recommend Isotype Controls: Mouse IgG1 kappa, Isotype Control (HY-P99977) .
NIAID RSVF2-5 is a human monoclonal antibody fragment. NIAID RSVF2-5 binds to conserved, distinct conformational epitopes on RSV fusion glycoprotein, and shows activity against RSVsubgroup A and B strains. NIAID RSVF2-5 reduces pulmonary and lung viral titers in RSV-infected rodents. NIAID RSVF2-5 can be used for the research of respiratory syncytial virus infection .
PF-03475952 is a fully human IgG2 monoclonal antibody targeting CD44. PF-03475952 binds an epitope in CD44’s constant exons, blocks CD44-hyaluronic acid interaction, reduces cell surface CD44, and does not cross-react with rodentCD44 or LYVE-1. PF-03475952 induces cancer cell apoptosis, inhibits LPS (HY-D1056)-induced leukocyte cytokine release and cancer metastasis, and reduces CD44 expression on circulating CD3+ lymphocytes in cynomolgus monkeys. PF-03475952 can be used for the research of rheumatoid arthritis and hepatocellular carcinoma .
Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively. Monocrotaline has antitumor activity and is cytotoxic to hepatocellular carcinoma cells. Monocrotaline is used to induce a model of pulmonary hypertension in rodents. [2][6][8].
L-Cysteine (Cysteine) is an orally active conditionally essential amino acid with hypoglycemic effects, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine promotes the proliferation and differentiation of neural stem cells via the CBS/H2S pathway. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans. L-Cysteine can be used as an anorectic agent .
L-Cysteine hydrochloride is an orally active conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride suppresses ghrelin and reduces appetite in rodents. L-Cysteine hydrochloride inhibits Aspergillus flavus growth and AFB synthesis by disrupting cell structure and antioxidant system balance. L-Cysteine hydrochloride enhances relaxant responses of rat aortic rings to NO and reduces responses to endothelium-derived relaxing factor (EDRF) .
Folitixorin (5,10-methylenetetrahydrofolate) is a cofactor and an analog of leucovorin. Folitixorin is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research .
Schisandrin B (γ-Schisandrin) is a biphenylcyclooctadiene derivative isolated from Schisandra chinensis and has been shown to have antioxidant effects on the liver and heart of rodents.
Coenzyme Q9 (Ubiquinone Q9), the major form of ubiquinone in rodents, is an amphipathic molecular component of the electron transport chain that functions as an endogenous antioxidant. Coenzyme Q9 attenuates the diabetes-induced decreases in antioxidant defense mechanisms. Coenzyme Q9 improves left ventricular performance and reduces myocardial infarct size and cardiomyocyte apoptosis .
Poricoic acid A can be isolated from Poria cocos. Poricoic acid A is an orally active anti-tumor agent. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis. Poricoic acid A also attenuatea fibroblast activation and abnormal extracellular matrix remodeling in renal fibrosis by activating AMPK and inhibiting Smad3. Poricoic acid A significantly reduces the magnitude of rise in serum creatinine and urea levels in rat model when combined with Melatonin. Poricoic acid A ameliorates renal fibrosis and podocyte injury by attenuating oxidative stress and inflammation through regulating NF-κB and Nrf2 in IRI rodent model in combination with Melatonin .
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
4'-O-Methylpyridoxine is an orally active antivitamin B6 compound found in Ginkgo biloba seeds and leaves. 4'-O-Methylpyridoxine inhibits pyridoxal kinase. 4'-O-Methylpyridoxine reduces brain pyridoxal-5'-phosphate (PLP) levels, decreases gamma-aminobutyric acid/glutamate (GABA/Glu) ratio. 4'-O-Methylpyridoxine increases plasma levels of pyridoxal-5'-phosphate and pyridoxal. 4'-O-Methylpyridoxine induces hyperactivity, convulsions, pathological tissue changes, organ damage in rodent brain and heart .
7-Dehydro desmosterol is a sterol and an intermediate in cholesterol biosynthesis, which is found in the marine diatom Pseudo-nitzschia multistriata and the nervous system of rodents .
Roridin E is a glucose-6-phosphatase (G6Pase) inhibitor and antibiotic, and is a metabolic byproduct of Roridin A (HY-N9599). Roridin E induces significant oxidative stress, characterized by depletion of glutathione in vivo, induction of hepatic lipid peroxidation, and inhibition of renal superoxide dismutase activity. Roridin E reduces blood glucose levels in rats, but exhibits acute toxicity (which is enhanced when co-administered with linoleic acid (HY-N0729)) and causes hepatotoxicity in male albino mice. Roridin E induces a decrease in total blood protein and increases in the levels of total lipids, γ-glutamyltransferase, alkaline phosphatase, and 5'-nucleotidase. Roridin E can be isolated from molds, and possesses cytostatic and antifungal activities similar to those of Verrucarin A (HY-107426) and Roridin A. Roridin E exhibits in vivo activity in rodents and is commonly used in hepatotoxicity-related studies .
L-Cysteine (Standard) is the analytical standard of L-Cysteine. This product is intended for research and analytical applications. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
Coenzyme Q9 (Standard) is the analytical standard of Coenzyme Q9. This product is intended for research and analytical applications. Coenzyme Q9 (Ubiquinone Q9), the major form of ubiquinone in rodents, is an amphipathic molecular component of the electron transport chain that functions as an endogenous antioxidant. Coenzyme Q9 attenuates the diabetes-induced decreases in antioxidant defense mechanisms. Coenzyme Q9 improves left ventricular performance and reduces myocardial infarct size and cardiomyocyte apoptosis .
Sophoramine ((-)-Sophoramine) is a prejunctional α2-adrenoceptor inhibitor that can be found in the seeds of Sophora alopecuroides. Sophoramine inhibits prejunctional α2-adrenoceptors to facilitate norepinephrine release from adrenergic nerves. Sophoramine shows cytotoxic activity against human cancer cells, positive inotropic activity, and activity in rodent arrhythmia models. Sophoramine can be used for the research of arrhythmias .
Schisandrin B (Standard) is the analytical standard of Schisandrin B. This product is intended for research and analytical applications. Schisandrin B (γ-Schisandrin) is a biphenylcyclooctadiene derivative isolated from Schisandra chinensis and has been shown to have antioxidant effects on the liver and heart of rodents.
(+)-Schisandrin B is an enantiomer of Schisandrin B. Schisandrin B is an active dibenzocyclooctadiene derivative isolated from the fruit of Schisandra chinensis, has antioxidant effect on rodent liver and heart .
Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
α-Muricholic acid (Standard) is the analytical standard of α-Muricholic acid. This product is intended for research and analytical applications. α-Muricholic acid is the most abundant primary bile acid in rodents .
L-Cysteine (hydrochloride hydrate) (Standard) is the analytical standard of L-Cysteine (hydrochloride hydrate). This product is intended for research and analytical applications. L-Cysteine hydrochloride hydrate is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride hydrate suppresses ghrelin and reduces appetite in rodents and humans .
Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively. Monocrotaline has antitumor activity and is cytotoxic to hepatocellular carcinoma cells. Monocrotaline is used to induce a model of pulmonary hypertension in rodents. .
L-Cysteine (hydrochloride) (Standard) is the analytical standard of L-Cysteine (hydrochloride). This product is intended for research and analytical applications. L-Cysteine hydrochloride is an orally active conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride suppresses ghrelin and reduces appetite in rodents. L-Cysteine hydrochloride inhibits Aspergillus flavus growth and AFB synthesis by disrupting cell structure and antioxidant system balance. L-Cysteine hydrochloride enhances relaxant responses of rat aortic rings to NO and reduces responses to endothelium-derived relaxing factor (EDRF) [4].
(S)-Pulegone ((-)-Pulegone) is a cytochrome P450 (CYP450) substrate. (S)-Pulegone induces urothelial cytotoxicity, necrosis, regenerative proliferation and urinary bladder tumors in female rats. (S)-Pulegone induces rodent nephropathy, olfactory metaplasia, gastric hyperplasia/perforation at high dose. (S)-Pulegone can be used for the research of urinary bladder and hepatic neoplasms .
Calonysterone is an orally effective IL-6 inhibitor. Calonysterone reduces the level of the proinflammatory cytokine IL-6. Calonysterone prevents diet-induced obesity. Calonysterone normalizes abnormal plasma adiponectin and leptin concentrations. Calonysterone increases the percentage of total DNA methylation. Calonysterone enhances antioxidant activity. Calonysterone is applicable to obesity-related research .
L-Cysteine-d3 is the deuterium labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
Sucralose-d6 is deuterium labeled Sucralose. Sucralose?(E955; Trichlorosucrose) is a?non-nutritive?artificial?sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
L-Cysteine-3- 13C is the 13C-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
L-Cysteine- 13C3, 15N is the 13C- and 15N-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
Flubendazole-d3 is the deuterium labeled Flubendazole. Flubendazole is a safe and efficacious anthelmintic agent, which is widely used for anthelmintic to human, rodents and ruminants. Flubendazole exerts anticancer activities by mechanisms including inhibition of microtubule function. Flubendazole induces p53-mediated apoptosis and arrests G2/M cell cycle .
L-Cysteine- 13C3 is the 13C-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
L-Cysteine- 15N is the 15N-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
L-Cysteine-1- 13C is the 13C-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
L-Cysteine-d2 is the deuterium labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
L-Cysteine-d3, 15N is the deuterium and 15N-labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans .
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents .
Alpidem-d14 is the deuterium labeled Alpidem (HY-W013150) . Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
Satranidazole-d3 is the deuterium labeled Satranidazole. Satranidazole is an orally active insecticide and antimicrobial agent with high electron affinity. Satranidazole forms reduced nitro intermediates, which interact with DNA, causing helix instability, strand breakage and release of thymidine derivatives. Satranidazole exhibits antitrichomonal activity against Trichomonas vaginalis and Trichomonas foetus, and antiamoebic activity in rodent models of hepatic amoebiasis and caecal amoebiasis. Satranidazole inhibits the replication of bacteriophage φX174 DNA. Satranidazole can be used in research related to caecal amoebiasis, trichomoniasis and anaerobic bacterial infections.
Remogliflozin etabonate-d7 (GSK189075-d7) is the deuterium labeled Remogliflozin etabonate. Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models .
Lipid 5 is an amino lipid that affords efficient mRNA delivery in rodent and primate models. Lipid 5 shows optimal pharmacokinetics and non-toxic side effects .
Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Liquid Paraffin is a petroleum-derived mixture of saturated hydrocarbons and an orally active fecal lubricant. Liquid Paraffin is widely used in studies of constipation and fecal incontinence in children through its lubricating effect and the osmotic effect generated by its conversion to hydroxy fatty acids. Liquid Paraffin has high safety, is non-carcinogenic, and does not affect fat-soluble vitamin levels with long-term use. Liquid Paraffin does not cause abdominal pain or electrolyte disorders, but may lead to lipoid pneumonia and granulomas caused by rectal administration. Liquid Paraffin can also be used as a phase change material for thermal energy storage, or combined with nanoparticles to form a protective boundary film to reduce mechanical wear .
Inactive ASO (in vivo) sodium is an inactive Antisense Oligonucleotide. ASO is a class of oligonucleotide molecules, usually composed of 20-30 bases, used to interfere with or regulate gene expression. Inactive ASO (in vivo) sodium is not targeted in the rodent genome and can be used as a negative control for Tofersen. Inactive ASO (in vivo) sodium contains thiophosphate skeleton modification and MOE modification. Cytosine in Inactive ASO (in vivo) is 5' methylcytosine. See References for the location of chemical modifications
ISIS 329993 (ISIS-CRPRx) is an antisense oligonucleotide targeting to C-reactive protein (CRP). ISIS-CRPRx has been tested in a rodent model of rheumatoid arthritis (RA) and was shown to improve the clinical signs of arthritis
ISIS 329993 sodium is an antisense oligonucleotide targeting to C-reactive protein (CRP). ISIS-CRPRx sodium has been tested in a rodent model of rheumatoid arthritis (RA) and was shown to improve the clinical signs of arthritis
Sucralose (GMP Like) (E955 (GMP Like)) is the GMP Like class Sucralose (HY-N0614) that can be used as pharmaceutical excipients. Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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