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Results for "

MES model

" in MedChemExpress (MCE) Product Catalog:

19

Inhibitors & Agonists

1

Peptides

1

Isotope-Labeled Compounds

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-159819
    Vormatrigine

    		Sodium Channel Neurological Disease
    Vormatrigine is an orally active sodium channel inhibitor with anti-epileptic activity. Vormatrigine has a specific inhibitory effect on overactive NaV channels in vitro and has a good inhibitory effect in the maximal electroconvulsive seizure (MES) model. Vormatrigine can be used to study human focal and generalized epilepsy .
    Vormatrigine
  • HY-101117
    EED226
    Maximum Cited Publications
    10 Publications Verification

    		 Histone Methyltransferase Cancer
    EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
    EED226
  • HY-W012481
    Nirvanol

    Ethylphenylhydantoin; Phenylethyihydantoin; Desmethylmephenytoin

    		 Drug Metabolite Neurological Disease
    Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
    Nirvanol
  • HY-100421
    CPI-455
    5+ Cited Publications

    		 Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
    CPI-455
  • HY-171509
    Mal-N(Me)-C6-N(Me)-PNU-159682

    		Drug-Linker Conjugates for ADC Apoptosis Cancer
    Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) .
    Mal-N(Me)-C6-N(Me)-PNU-159682
  • HY-170833
    Anticonvulsant agent 8

    		GABA Receptor Neurological Disease
    Anticonvulsant agent 8 (compound D4) is an anticonvulsant agent that inhibits GABAA currents with ED50 values of 2.23 and 24.60 mg/kg in the maximum electroshock (MES) and pentylenetetrazol (PTZ) tests in mouse models, respectively .
    Anticonvulsant agent 8
  • HY-106424
    Soretolide

    		Others Neurological Disease
    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 .
    Soretolide
  • HY-114300
    DSP-0565

    		GABA Receptor Neurological Disease
    DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic agent (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin .
    DSP-0565
  • HY-W012481S
    Nirvanol-d5

    Ethylphenylhydantoin-d5; Phenylethyihydantoin-d5; Desmethylmephenytoin-d5

    		 Isotope-Labeled Compounds Drug Metabolite Neurological Disease
    Nirvanol-d5 (Ethylphenylhydantoin-d5) is deuterium labeled Nirvanol (HY-W012481) . Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
    Nirvanol-d5
  • HY-154484
    3’-O-Me-G(iBu)-2’-phosphoramidite

    		Nucleoside Antimetabolite/Analog Cancer
    3’-O-Me-G(iBu)-2’-phosphoramidite is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7) .
    3’-O-Me-G(iBu)-2’-phosphoramidite
  • HY-100421A
    CPI-455 hydrochloride

    		Histone Demethylase Cancer
    CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
    CPI-455 hydrochloride
  • HY-169061
    WQQ-345

    		Histone Methyltransferase Aminotransferases (Transaminases) Lactate Dehydrogenase Cancer
    WQQ-345 is a BCAT1 inhibitor with an IC50 value of 10.8 mM. WQQ-345 can lead to a decrease in α-KG levels, an upregulation of H3K27me3 expression, a reduction in the expression of glycolytic enzymes (PFKP and LDHA), and impaired glycolytic activity in 67R cells. WQQ-345 shows tumor-suppressing activity in a 67R subcutaneous xenograft model .
    WQQ-345
  • HY-P10819
    S9-CMC1 TFA

    		Histone Demethylase Apoptosis Cancer
    S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
    S9-CMC1 TFA
  • HY-108327
    PF-05020182

    		Potassium Channel Neurological Disease
    PF-05020182 is an orally active opener for Kv7 channel, that activates human Kv7.2/7.3, Kv7.4 and Kv7.3/7.5 with EC50 of 334, 625 and 588 nM, respectively. PF-05020182 exhibits anticonvulsant activity in rats corneal electric shock-induced tonic seizure (MES) models. PF-05020182 is blood-brain barrier (BBB) penetrable .
    PF-05020182
  • HY-155313
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE

    		Drug-Linker Conjugates for ADC Cancer
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE
  • HY-169919
    HDM-IN-1

    		Histone Demethylase Fungal Infection
    HDM-IN-1 (Compound A4) is an inhibitor for fungal histone demethylase (HDM), that inhibits the H3K27me3 in Cryptococcus neoformans and in Candida auris with IC50s of 134 and 12 nM. HDM-IN-1 exhibits inhibitory efficacy against C. neoformans and C. auris with MIC80 of 0.5-2 μg/mL, through inhibition of the biofilm and capsule formation. HDM-IN-1 exhibits antifungal activity in ICR mouse model .
    HDM-IN-1
  • HY-149677
    ZK53

    		Mitochondrial Metabolism Cancer
    ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
    ZK53
  • HY-168773
    (R)-AS-1

    		EAAT Neurological Disease
    (R)-AS-1 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. (R)-AS-1 (at doses of 60 and 90 mg/kg) increases spontaneous locomotor activity in mice. Additionally, it demonstrates anticonvulsant activity in mouse models of seizures induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electrical stimuli (32 or 44 mA), with ED50s of 66.3, 36.3, 15.6, and 41.6 mg/kg, respectively. (R)-AS-1 can be used in neurological disease research .
    (R)-AS-1
  • HY-172887
    Kv7.2/Kv7.3 activator-2

    		Potassium Channel Neurological Disease
    Kv7.2/Kv7.3 activator-2 is a BBB-penetrable Kv7.2/7.3 activator (EC50: 0.25 μM). Kv7.2/Kv7.3 activator-2 has good photostability. Kv7.2/Kv7.3 activator-2 has potently antiepileptic effects in maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ)-induced acute mice seizure models .
    Kv7.2/Kv7.3 activator-2

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