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prodrug

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-161336

    Bacterial Cancer
    Alendronate prodrug-1(compound 2) is an inhibitor of farnesyl diphosphate synthase (FPPS). Alendronate prodrug-1 has an antiproliferative effect with an IC50 value of 34.0 μM .
    Alendronate prodrug-1
  • HY-161687

    Src Cancer
    Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
    Cisplatin/Dasatinib prodrug-1
  • HY-163849

    Others Inflammation/Immunology
    Mizoribine prodrug-1 (compound 18) is a oral active ester-based mizoribine (HY-17470) prodrug. Mizoribine prodrug-1 displays a inhibition of IL-2 production .
    Mizoribine prodrug-1
  • HY-163850

    Interleukin Related Inflammation/Immunology
    Mizoribine prodrug-2 trifluoroacetate (compound 20) is a oral active mizoribine (HY-17470) prodrug (amino acid conjugate). Mizoribine prodrug-2 displays a prolonged inhibition of IL-2 production .
    Mizoribine prodrug-2 trifluoroacetate
  • HY-172148

    Interleukin Related Inflammation/Immunology
    Itaconic acid prodrug-1 (Compound P2) is an orally active prodrug of Itaconic acid (HY-Y0520) that efficiently delivers the active ingredient Itaconic acid to skin tissue following oral administration. Itaconic acid prodrug-1 possesses immunomodulatory properties, significantly inhibiting Poly(I:C)/IFNγ-induced inflammatory cytokines in human epidermal keratinocytes. Itaconic acid prodrug-1 can be utilized for the research of alopecia areata and other inflammatory skin diseases .
    Itaconic acid prodrug-1
  • HY-168928

    Bacterial Infection
    Antibiofilm agent prodrug 1 (Compound 5c) exhibits antibacterial activity through inhibition of biofilm formation and iron uptake. Antibiofilm agent prodrug 1 inhibits P. aeruginosa PAO1 with a MIC of 1.07 μM. Antibiofilm agent prodrug 1 exhibits anti-infectious efficacy in C. elegans with improved survival rate .
    Antibiofilm agent prodrug 1
  • HY-168875

    TrxR Reactive Oxygen Species Cancer
    TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1. TrxR1 prodrug-1 exhibits significant antitumor efficiency in nude mice and NSCLC organoids .
    TrxR1 prodrug-1
  • HY-168472

    SARS-CoV Infection
    13-TP prodrug (compound 15) is a potent and orally active anti-SARS-CoV-2 agent. 13-TP prodrug shows cytotoxicity. 13-TP prodrug decreases the SARS-CoV-2 N protein expression. 13-TP prodrug shows antiviral activity .
    13-TP prodrug
  • HY-163544

    Others Cancer
    δ-Tocotrienol prodrug-1 (compound 5b) is a prodrug of δ-tocotrienol (HY-122778). δ-Tocotrienol prodrug-1 shows radioprotective efficacy. δ-Tocotrienol prodrug-1 promotes the hematopoietic progenitor and stem cell regeneration in murine bone marrow and spleen .
    δ-Tocotrienol prodrug-1
  • HY-173023

    Apoptosis Indoleamine 2,3-Dioxygenase (IDO) Reactive Oxygen Species Cancer
    IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug. IDOi-Pt(IV) prodrug-1 inhibits IDO expression. IDOi-Pt(IV) prodrug-1 induces apoptosis, decreases the mitochondrial membrane potential, inhibits tumor cell migration and invasion. IDOi-Pt(IV) prodrug-1 induces reactive oxygen species-mediated endoplasmic reticulum stress and secretion of damage-associated molecular patterns (DAMPs), thereby presenting immunogenic cell death (ICD) effects. IDOi-Pt(IV) prodrug-1 has high-efficiency and low-toxicity antitumor effects compared to Cisplatin (HY-17394) .
    IDOi-Pt(IV) prodrug-1
  • HY-169131

    AMPK Cancer
    ALKBH1-IN-4 prodrug (Compound 29E) is a prodrug of a DNA N6-methyladenine demethylase ALKBH1 inhibitor that significantly increases the abundance of 6mA in cells and upregulates the AMPK signaling pathway, thereby inhibiting the viability of gastric cancer cells. ALKBH1-IN-4 prodrug exhibits excellent cellular activity and favorable metabolic exposure in vivo, and holds promise for research in gastric cancer .
    ALKBH1-IN-3 prodrug
  • HY-159921

    Microtubule/Tubulin Cancer
    Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a palladium (Pd)-mediated tubulin polymerization inhibitor prodrug. Developed based on colchicine binding site inhibitors (CBSIs), it reduces toxicity and enhances targeted release properties. Compared to the parent compound, Tubulin Polymerization-IN-1 prodrug exhibited 68.3-fold lower cytotoxicity, which can be restored in situ in the presence of Pd resin. Mechanistic studies showed that its anticancer activity is consistent with CBSIs. In vivo, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth (63.2%) when activated by Pd resin. It holds promise for research in the field of anticancer therapy .
    Tubulin Polymerization-IN-1 prodrug
  • HY-145829

    JAK Apoptosis Inflammation/Immunology
    Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
    Tofacitinib Prodrug-1
  • HY-109755

    Bacterial Antibiotic Others
    PF-04064900 is a prodrug of sulopenem penem antibiotic .
    PF-04064900
  • HY-118983

    Antibiotic Bacterial Infection
    Pivampicillin hydrochloride is a penicillin antibiotic. Pivampicillin hydrochloride is a prodrug of Ampicillin (HY-B0522) .
    Pivampicillin hydrochloride
  • HY-119011

    Antibiotic Bacterial Infection
    Pivampicillin is a penicillin antibiotic. Pivampicillin is a prodrug of Ampicillin (HY-B0522) .
    Pivampicillin
  • HY-157127

    COX Metabolic Disease
    Ketoprofen L-thyroxine ester is a prodrug of Ketoprofen. Ketoprofen L-thyroxine ester reservoir and release ketoprofen slowly in the brain .
    Ketoprofen L-thyroxine ester
  • HY-114840

    Ras Cancer
    L 731734 is a prodrug of L-731735 (HY-129273), and inhibits Ras processing in cells transformed with v-ras .
    L 731734
  • HY-135077

    Drug Intermediate Others
    Prostaglandin A1 ethyl ester is a prodrug form of Prostaglandin A1. Prostaglandin A1 inhibits the activation of platelets .
    Prostaglandin A1 ethyl ester
  • HY-162039

    MMP Cancer
    MMP-11-IN-1 (compound 9) is a new class of phosphinate prodrug. MMP-11-IN-1 is a glycosyl ester of RXP03 and improves blood–brain barrier (BBB) behavior .
    MMP-11-IN-1
  • HY-162410

    MDM-2/p53 Cancer
    Fluplatin is a prodrug composed of cisplatin and fluvastatin. Fluplatin has antitumor activity .
    Fluplatin
  • HY-126719

    Drug Derivative Neurological Disease
    R-1 Methanandamide Phosphate is a water-soluble prodrug analog of arachidonylethanolamide (AEA). AEA is an endogenous cannabinoid compound .
    R-1 Methanandamide Phosphate
  • HY-162911

    Phosphodiesterase (PDE) Cancer
    Enpp-1-IN-22 is an orally bioavailable prodrug of the potent ENPP1 inhibitor paraformaldehyde with antitumor activity .
    Enpp-1-IN-22
  • HY-165164

    Others Cancer
    Methotrexate-alpha-alanine is a prodrug for activation by enzyme-monoclonal antibody conjugates. Methotrexate-alpha-alanine shows cytotoxicity .
    Methotrexate-alpha-alanine
  • HY-168639

    Mitochondrial Metabolism AMPK Metabolic Disease
    AP39 prodrug 1 (Compound M1) is a mitochondria-targeted H2S prodrug. AP39 prodrug 1 induces ROS-dependent mild mitochondrial uncoupling, activating mitochondria-associated AMPK to suppress Palmitic acid (PA) (HY-N0830)-induced lipid deposition in hepatocytes .
    AMPK activator 15
  • HY-129464

    GABA Receptor Neurological Disease
    NO-711ME is a prodrug of NO-711. NO-711 is a potent and selective GABA uptake inhibitor .
    NO-711ME
  • HY-158329

    N-Alloc doxorubicin

    Apoptosis Topoisomerase Antibiotic AMPK Bacterial Autophagy Mitophagy HIV HBV Cancer
    Alloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth .
    Alloc-DOX
  • HY-107074

    R1518

    HCV Infection
    Levovirin valinate hydrochloride (R1518) is a prodrug of Levovirin (HY-119415) with oral activity, exhibiting antiviral activity against hepatitis C virus .
    Levovirin valinate hydrochloride
  • HY-117606

    mGluR Neurological Disease
    LY3027788, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 has antidepressant efficacy .
    LY3027788
  • HY-117606A

    mGluR Neurological Disease
    LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy .
    LY3027788 hydrochloride
  • HY-120313

    Drug Derivative Cancer
    SN23862 is a cancer prodrug with anti-cancer activity, and an analogue of CB-1954 (HY-13543). SN23862 can be used for cancer research .
    SN23862
  • HY-155371

    PROTACs Others
    BT-PROTAC is a bioorthogonally activatable prodrug. BT-PROTAC can accurately control the activity of PROTAC .
    BT-PROTAC
  • HY-W811579

    Bacterial Infection
    Bensuldazic acid (compound 4f) is a lipophilic 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivative that can be used as a prodrug model. Bensuldazic acid has antifungal activity .
    Bensuldazic acid
  • HY-114623

    Prostaglandin Receptor Endocrinology
    Prostaglandin D2 methyl ester is a prodrug form of Prostaglandin D2. Prostaglandin D2 methyl ester binds to the human and mouse PGD2 receptors (DP and CRTH2) with Ki values of 160 nM, 175 nM, 460 nM, and 270 nM for mCRTH2, mDP, hCRTH2, and hDP, respectively .
    Prostaglandin D2 methyl ester
  • HY-W811579A

    Bacterial Infection
    Bensuldazic acid sodium (compound 4f) is a lipophilic 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivative that can be used as a prodrug model. Bensuldazic acid has antifungal activity .
    Bensuldazic acid sodium
  • HY-14554

    LY2140023

    mGluR Neurological Disease
    Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research .
    Pomaglumetad methionil anhydrous
  • HY-149025

    P18

    Phospholipase Inflammation/Immunology Cancer
    DPTIP-proagent 18 (P18) is a orally active and brain-penetrable proagent of DPTIP (HY-131002). DPTIP-proagent 18 is a potent nSMase2 inhibitor. DPTIP-proagent 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-proagent 18 can be used for brain injury research .
    DPTIP-prodrug 18
  • HY-122278

    Dopamine Receptor Neurological Disease
    Melevodopa is an effervescent levodopa (HY-N0304) prodrug. Levodopa is an orally active metabolic precursor of neurotransmitters dopamine and has anti-allodynic effects and the potential for Parkinson's disease .
    Melevodopa
  • HY-W011963

    Dopamine Receptor Neurological Disease
    Melevodopa hydrochloride is an effervescent Levodopa (HY-N0304) prodrug. Levodopa is an orally active metabolic precursor of neurotransmitters dopamine and has anti-allodynic effects and the potential for Parkinson's disease
    Melevodopa hydrochloride
  • HY-105040

    LY2140023 hydrate

    mGluR Neurological Disease
    Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia .
    Pomaglumetad methionil
  • HY-139995

    Drug Intermediate Others
    Spermine precursor-1 (Compound 1) is a redox-sensitive spermine precursor for the potential research of snyder robinson syndrome. Spermine precursor-1 inhibits wild-type (CMS-24949) and spermine synthase gene (SMS) mutant (CMS-26559, and CMS-6233) fibroblast cells with IC50s of 326.7, 198.5, and 244.1 μM, respectively .
    Spermine Prodrug-1
  • HY-123330

    HIV Reverse Transcriptase Infection
    GW695634 is an orally active prodrug of GW678248. GW695634 undergoes amidolysis in vivo to release the active ingredient GW678248, thereby inhibiting viral replication. GW678248 is a non-nucleoside reverse transcriptase inhibitor (NNRTi) with potent antiviral activity against Efavirenz (HY-10572)-resistant and Nevirapine (HY-10570)-resistant HIV and AIDS viruses .
    GW695634
  • HY-145323

    Biochemical Assay Reagents Cancer
    Mitochondria-Targeted Photoactivatable Proagent accumulates in the mitochondria and shows light-triggered temporally controlled cell death. Mitochondria-Targeted Photoactivatable Proagent can be used in a novel drug delivery platform that provides on-demand, real-time, organelle-specific agent release and monitoring upon photoactivation .
    Mitochondria-Targeted Photoactivatable Prodrug
  • HY-108244

    Interleukin Related STAT Inflammation/Immunology Cancer
    Balsalazide disodium is a prodrug of amino salicylic acid that releases mesalamine (HY-15027) in the colon, offering various anti-inflammatory effects in areas of colitis, and it also exerts related anticancer effects by regulating the IL-6/STAT3 pathway .
    Balsalazide disodium
  • HY-144876

    Reactive Oxygen Species Cancer
    RIDR-PI-103 is a reactive oxygen species (ROS)-induced drug release prodrug with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103).
    RIDR-PI-103
  • HY-161062

    EAAT Neurological Disease
    TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death .
    TAOA AM Ester trimethyl lock
  • HY-161838

    ATM/ATR Cancer
    ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
    ICT10336
  • HY-14532
    Brincidofovir
    2 Publications Verification

    CMX001; HDP-CDV

    CMV HSV Orthopoxvirus Infection
    Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections. Brincidofovir, an oral antiviral in late stage development, has proven effective against orthopoxviruses in vitro and in vivo. .
    Brincidofovir
  • HY-149065

    α-synuclein Neurological Disease
    D-685, a prodrug of D-520, exhibits higher in vivo anti-Parkinsonian efficacy in a reserpinized Parkinson's disease (PD) animal model than the parent D-520. D-685 reduces accumulation of human α-synuclein (α-syn) protein. D-685 exhibits facile brain penetration .
    D-685
  • HY-U00085

    RU 47213

    Cholinesterase (ChE) Neurological Disease
    Itameline (RU 47213) is a prodrug with oral and long-lasting cholinergic activity. Itameline is a novel tetrahydropyridine-oxime that is cleaved in vivo to form an active metabolite, RU 35963. RU 35963 is a muscarinic receptor agonist that is nonselective with respect to receptor subtypes. Itameline possesses the capacity to reduce memory deficits induced by an impairment of cholinergic transmission in the rat .
    Itameline

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