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oral activity

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8

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122

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15383
    Glyparamide

    		Others Others
    Glyparamide is an orally active chlorophenyl-containing sulfonylurea. Glyparamide shows hypoglycemic activity and rarely causes hepatic injury .
    Glyparamide
  • HY-B1196
    Tiapride hydrochloride

    		Dopamine Receptor Neurological Disease
    Tiapride hydrochloride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride hydrochloride shows anti-dyskinetic activity and anxiolytic activity. Tiapride hydrochloride is a neuroleptic agent .
    Tiapride hydrochloride
  • HY-106499
    Sulfinalol

    		Adrenergic Receptor Cardiovascular Disease
    Sulfinalol is an orally active β-adrenoceptor antagonist with direct vasodilator activity .
    Sulfinalol
  • HY-106584
    Mosapramine

    Clospipramine

    		 Dopamine Receptor Neurological Disease
    Mosapramine (Clospipramine) is an orally active and potent dopamine receptor antagonist with high affinity to dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT 2 receptor. Mosapramine shows antipsychotic activity and can be used in schizophrenia research .
    Mosapramine
  • HY-106578
    Quinupramine

    LM 208

    		 Others Neurological Disease
    Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system[1][2].
    Quinupramine
  • HY-10715
    SSR504734

    		GlyT Neurological Disease
    SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities .
    SSR504734
  • HY-B1656
    Fomocaine

    P 652

    		 Others Cardiovascular Disease Neurological Disease
    Fomocaine (P 652) is an orally active local anaesthetic. Fomocaine shows antiarrhythmic activity .
    Fomocaine
  • HY-N7697F
    Chitobiose

    		Others Others
    Chitobiose, a chitosan oligosaccharide, is a dimer of β-1,4-linked glucosamine units . Chitobiose has orally activity and high antioxidant activity .
    Chitobiose
  • HY-N10379
    19-epi-Scholaricine

    		Reactive Oxygen Species Inflammation/Immunology
    19-epi-Scholaricine is an orally active indole alkaloid that downregulates the expression of collagen fibrosis and increases superoxide dismutase (SOD) activities .
    19-epi-Scholaricine
  • HY-103595
    Epirizole

    Mepirizole; DA-398

    		 Others Inflammation/Immunology
    Epirizole (Mepirizole) is an orally active NSAID (nonsteroidal anti-inflammatory agent). Epirizole shows anti-inflammatory activity, and can be used in chronic rheumatoid arthritis research .
    Epirizole
  • HY-162249
    ASP6918

    		Ras Cancer
    ASP6918 is a potent and orally active KRAS G12C inhibitor with an IC50 value of 0.028 µM. ASP6918 inhibits cell growth. ASP6918 shows antitumor activity .
    ASP6918
  • HY-157585S
    21-Dehydro Budesonide-d8-1

    		Isotope-Labeled Compounds Glucocorticoid Receptor Inflammation/Immunology Cancer
    21-Dehydro Budesonide-d8-1 is deuterated labeled dehydrogenated Budesonide (HY-13580). Budesonide is an orally available glucocorticoid receptor agonist with anti-cancer activity. 21-Dehydro Budesonide-d8-1 acts as a probe for glucocorticoid receptors and is used in isotope tracing studies .
    21-Dehydro Budesonide-d8-1
  • HY-W005130
    2,4,6-Trihydroxybenzaldehyde

    		NF-κB Metabolic Disease
    2,4,6-Trihydroxybenzaldehyde is an orally active NF-ĸB inhibitor. 2,4,6-Trihydroxybenzaldehyde shows anti-tumor activity, anti-cancer cell proliferative activity and anti-obesity activity .
    2,4,6-Trihydroxybenzaldehyde
  • HY-100516
    Cimicoxib

    UR-8880

    		 COX Inflammation/Immunology
    Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar .
    Cimicoxib
  • HY-151460
    GCN2-IN-7

    		Others Cancer
    GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo .
    GCN2-IN-7
  • HY-155463
    NLRP3-IN-25

    		NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM .
    NLRP3-IN-25
  • HY-P3499
    Dolcanatide

    		Guanylate Cyclase Inflammation/Immunology
    Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research .
    Dolcanatide
  • HY-10777
    EMD 495235

    		Factor Xa Cardiovascular Disease
    EMD 495235 is a potent and orally active coagulation factor Xa inhibitor with an IC50 of 5.5 nM and a Ki of 6.8 nM. EMD 495235 shows anticoagulant activities .
    EMD 495235
  • HY-144870
    STAT3-IN-7

    		STAT Cancer
    STAT3-IN-7, an aryl sulfonamido azetidine compound, is an orally active STAT3 inhibitor. STAT3-IN-7 has anticancer activities (WO2021016333A1, H182) .
    STAT3-IN-7
  • HY-144300
    Rifasutenizol

    TNP-2198

    		 Bacterial Infection
    Rifasutenizol (TNP-2198) is a potent and orally bioavailable dual-targeted antibacterial agent. Rifasutenizol has potent activity against microaerophilic and anaerobic bacterial pathogens .
    Rifasutenizol
  • HY-122844
    Ifebemtinib

    BI-853520; IN-10018

    		 FAK Cancer
    Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively .
    Ifebemtinib
  • HY-146662
    HPGDS inhibitor 3

    		PGE synthase Inflammation/Immunology
    HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .
    HPGDS inhibitor 3
  • HY-120350
    BI-1347
    1 Publications Verification

    		 CDK Cancer
    BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity .
    BI-1347
  • HY-147570
    ATR-IN-18

    		ATM/ATR Cancer
    ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity .
    ATR-IN-18
  • HY-123777
    VT-1598

    		Fungal Infection Inflammation/Immunology
    VT-1598 is an orally active and selective fungal inhibitor targeting CYP51. VT-1598 shows anti-fungal activity against Candida auris . VT-1598 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    VT-1598
  • HY-151111
    SPH3127

    		Renin Cardiovascular Disease
    SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research .
    SPH3127
  • HY-150076
    BLU2864

    		Others Metabolic Disease Cancer
    BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research .
    BLU2864
  • HY-14336
    SB 271046

    		5-HT Receptor Neurological Disease
    SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity .
    SB 271046
  • HY-160019
    MTX115325

    		Deubiquitinase Mitophagy Neurological Disease
    MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
    MTX115325
  • HY-149726
    EZH2-IN-17

    		Histone Methyltransferase Cancer
    EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively) .
    EZH2-IN-17
  • HY-14578
    Taxiresinol

    		Others Neurological Disease Inflammation/Immunology
    Taxiresinol is an orally active and potent lignan, that can be isolated from the heartwood of Taxus baccata. Taxiresinol shows significant antinociceptive activity .
    Taxiresinol
  • HY-15297
    Vesnarinone
    1 Publications Verification

    OPC-8212

    		 Phosphodiesterase (PDE) Infection Cardiovascular Disease
    Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research .
    Vesnarinone
  • HY-109169
    Bomedemstat

    IMG-7289

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat
  • HY-109169B
    Bomedemstat hydrochloride

    IMG-7289 hydrochloride

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat hydrochloride
  • HY-109169C
    Bomedemstat dihydrochloride

    IMG-7289 dihydrochloride

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat dihydrochloride
  • HY-113974
    trans-AUCB
    1 Publications Verification

    t-AUCB

    		 Epoxide Hydrolase Cancer
    trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity .
    trans-AUCB
  • HY-109169A
    Bomedemstat ditosylate

    IMG-7289 ditosylate

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat ditosylate
  • HY-146684
    HDAC-IN-36

    		HDAC Autophagy Apoptosis Cancer
    HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research .
    HDAC-IN-36
  • HY-143894
    FLT3-IN-11

    		FLT3 Cancer
    FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM) .
    FLT3-IN-11
  • HY-144107
    HCV-IN-34

    		HCV Infection
    HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM .
    HCV-IN-34
  • HY-N10225
    Thielavin A

    		Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Thielavin A is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin A specifically inhibits the conversion of arachidonic acid into prostaglandin H2. Thielavin A has no anti-inflammatory activity on intravenous injection or on oral administration .
    Thielavin A
  • HY-106560
    Proglumetacin

    		COX SARS-CoV Inflammation/Immunology
    Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoV Mpro (main protease of the SARS-CoV-2), with an AC50 of 8.9 μM (activity concentration at half maximal activity). Proglumetacin has anti-inflammatory activity, can be used for inflammation (such as Rheumatoid arthritis, and Allergic air pouch inflammation) research[1][2][3].
    Proglumetacin
  • HY-147015
    HOE961

    		Orthopoxvirus Infection
    HOE961, the diacetate ester proagent of S2242, is active against respiratory cowpox virus infections, is orally active in infection models. Anti-orthopoxvirus activity .
    HOE961
  • HY-144109
    HCV-IN-36

    		HCV Infection
    HCV-IN-36 (compound (S)-3h) is an orally active and potent HCV entry inhibitor. HCV-IN-36 shows excellent antiviral activity, with an EC50 of 0.016 μM and a CC50 (half-maximal cytotoxic concentration) of 8.78 μM .
    HCV-IN-36
  • HY-144112
    HIV-1 inhibitor-13

    		HIV Infection
    HIV-1 inhibitor-13 (compound 16c) is a orally active and potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), with IC50 of 0.14 μM (HIV-1 RT). HIV-1 inhibitor-13 shows activity against a panel of HIV-1 resistant strains, with EC50 values of 2.85-18.0 nM .
    HIV-1 inhibitor-13
  • HY-143895
    FLT3-IN-12

    		FLT3 Cancer
    FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM) .
    FLT3-IN-12
  • HY-143244
    Monoamine Oxidase B inhibitor 1

    		Monoamine Oxidase Neurological Disease
    Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
    Monoamine Oxidase B inhibitor 1
  • HY-143245
    Monoamine Oxidase B inhibitor 2

    		Monoamine Oxidase Neurological Disease
    Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
    Monoamine Oxidase B inhibitor 2
  • HY-151261
    HDAC6-IN-13

    		HDAC Inflammation/Immunology
    HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity .
    HDAC6-IN-13
  • HY-101870B
    Uzansertib phosphate

    INCB053914 phosphate

    		 Pim Cancer
    Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
    Uzansertib phosphate

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