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prodrug models

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46

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Inhibitory Antibodies

2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P99101
    Vobramitamab

    AEX-4089; MGC026 antibody

    		 ADC Antibody Cancer
    Vobramitamab is a humanized B7-H3 monoclonal antibody (mAb). Vobramitamab conjugated with prodrug seco-DUBA (HY-132180A) via a cleavable linker, to form antibody-drug conjugate (ADC), the MGC018. MGC018 displays potent antitumor activity in preclinical tumor models of breast, ovarian, and lung cancer, as well as melanoma .
    Vobramitamab
  • HY-108292
    Propacetamol hydrochloride

    		NF-κB Neurological Disease Cancer
    Propacetamol hydrochloride is an orally active prodrug of paracetamol and an inducer of acute liver injury models, with multiple properties including antinociception, antioxidation and gastroprotection. Propacetamol hydrochloride potentiates Tramadol and attenuates Aspirin (HY-14654)-induced gastric mucosal damage and lipid peroxidation. Under specific conditions, Propacetamol hydrochloride also acts as a hepatotoxic inducer, triggering acute liver injury, oxidative stress and apoptosis, with strain differences in toxicity sensitivity. Propacetamol hydrochloride can be used in the research of acute liver injury, drug-induced hepatotoxicity and gastric mucosal damage .
    Propacetamol hydrochloride
  • HY-118956
    Adrogolide hydrochloride

    ABT-431 hydrochloride; DAS-431 hydrochloride

    		 Dopamine Receptor Neurological Disease
    Adrogolide hydrochloride (ABT-431 hydrochloride) is a chemically stable prodrug that can convert to the dopamine D1 receptor agonist A-86929. Adrogolide hydrochloride ameliorates the MPTP (HY-15608)-induced Parkinson's Disease in marmoset model, reduces the dyskinesias tendency. Adrogolide hydrochloride reverses Risperidone (HY-11018)-induced cognitive deficits in monkey .
    Adrogolide hydrochloride
  • HY-178239
    DX-8951 Hydroxy-acid

    		Drug Metabolite AMPK Reactive Oxygen Species (ROS) Inflammation/Immunology
    DX-8951 Hydroxy-acid is a prodrug of phosphoramide. ProAX can effectively increase intracellular ATP levels. DX-8951 Hydroxy-acid activates the AMPK signaling pathway by increasing the AMP/ATP ratio. DX-8951 Hydroxy-acid can enhance mitochondrial function and antioxidant capacity while reducing reactive oxygen species (ROS) levels. DX-8951 Hydroxy-acid has shown significant anti-aging and longevity effects in both human fibroblast and nematode models .
    DX-8951 Hydroxy-acid
  • HY-17484
    Ampiroxicam
    2 Publications Verification

    CP 65703

    		 Drug Derivative Inflammation/Immunology
    Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases .
    Ampiroxicam
  • HY-134160
    5,6-Dihydro-5-Fluorouracil

    5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil

    		 Nucleoside Antimetabolite/Analog Cancer
    5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
    5,6-Dihydro-5-Fluorouracil
  • HY-176869
    EMC-AANL-DOX

    		Drug Derivative Cancer
    EMC-AANL-DOX is a legumain-activated prodrug conjugate of Doxorubicin (DOX) (HY-15142A). EMC-AANL-DOX shows antitumor activity in mouse models of neuroblastoma (NB), breast cancer (4T1), fibrosarcoma (HT1080), and colorectal cancer liver metastases (CT26). EMC-AANL-DOX can be used for cancer research .
    EMC-AANL-DOX
  • HY-P10759
    DTS-201 sodium

    		Peptide-Drug Conjugates (PDCs) Aminopeptidase Cancer
    DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
    DTS-201 sodium
  • HY-178239A
    DX-8951 Hydroxy-acid sodium

    		Drug Metabolite AMPK Reactive Oxygen Species (ROS) Inflammation/Immunology
    DX-8951 Hydroxy-acid sodium is a prodrug of phosphoramide. DX-8951 Hydroxy-acid sodium can effectively increase intracellular ATP levels. DX-8951 Hydroxy-acid sodium activates the AMPK signaling pathway by increasing the AMP/ATP ratio. DX-8951 Hydroxy-acid sodium can enhance mitochondrial function and antioxidant capacity while reducing reactive oxygen species (ROS) levels. DX-8951 Hydroxy-acid sodium has shown significant anti-aging and longevity effects in both human fibroblast and nematode models .
    DX-8951 Hydroxy-acid sodium
  • HY-159925
    QKY-613

    		Cyclic GMP-AMP Synthase Infection Inflammation/Immunology
    QKY-613 is a prodrug that enhances immune surveillance by targeting nucleic acid modification pathways. QKY-613 promotes the selective incorporation of 6mdA (N6-methyldeoxyadenosine) into viral DNA, enhancing the phase separation potential of DNA, thereby increasing the activation of cGAS and strengthening host immune surveillance. In virus-infected mouse models, QKY-613 significantly reduced mortality in aged mice. QKY-613 holds promise for research on nucleic acid modification-based immune surveillance mechanisms .
    QKY-613
  • HY-125356
    ETX0282

    		Beta-lactamase Infection
    ETX0282 is an orally active prodrug, with its active form being ETX1317. ETX0282 and ETX1317 are β-lactamase inhibitors of the dioxolane-dibenzo-p-heptane (DBO) type. ETX0282 exhibits high stability during intestinal absorption and can be efficiently converted into ETX1317 in the liver. ETX0282 alone has no bactericidal activity, but in a mouse model of neutropenic thigh infection, it can significantly reduce bacterial load when used in combination with Cefpodoxime Proxetil (HY-N7101). ETX0282 can be used for the study of infections caused by drug-resistant Gram-negative bacteria .
    ETX0282
  • HY-178819
    NM-001

    		Integrin Drug Intermediate Cancer
    NM-001 is a theranostic prodrug that targets ανβ3 integrin. NM-001 consists of cRGD and GFLG peptides, a DCM fluorophore and Chlorambucil (HY-13593). NM-001 internalizes into lysosomes of tumor cells via the cRGD peptide, and generates NM-002 (HY-178820) and Chlorambucil through intracellular cleavage at the GFLG peptide by overexpressed Cathepsin B (CTSB). NM-001 exhibits green fluorescence under physiological conditions, and converts to NIR fluorescence by CTSB activation. NM-001 has significant antitumor activity with low toxicity in HeLa cell xenografts mouse models. NM-001 can be used for real-time drug release monitoring research .
    NM-001
  • HY-179221
    HIV-1-IN-89

    		HIV Infection
    HIV-1-IN-89 (Compound 20a-D) is a prodrug of 20a (an HIV-1 protease inhibitor). HIV-1-IN-89 has better pharmacokinetic properties. HIV-1-IN-89 can be used for studying the resistance to HIV-1 .
    HIV-1-IN-89
  • HY-176771
    Tapinarof prodrug-1

    		Drug Intermediate Inflammation/Immunology
    Tapinarof prodrug-1 (Compound 31) is an orally active prodrug of Tapinarof (HY-109044). Tapinarof is an AhR agonist. Tapinarof prodrug-1 has an improving effect in the TNBS-induced mouse model of inflammatory bowel disease. Tapinarof prodrug-1 can be used in the research of inflammatory diseases .
    Tapinarof prodrug-1
  • HY-175257
    Theophylline-platinum(IV) prodrug-1

    		PARP Reactive Oxygen Species (ROS) Apoptosis NF-κB ERK Bcl-2 Family TGF-β Receptor EGFR Cadherin Cancer
    Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer .
    Theophylline-platinum(IV) prodrug-1
  • HY-134521
    Diclofenac amide

    		COX Inflammation/Immunology
    Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
    Diclofenac amide
  • HY-161838
    ICT10336

    		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-179418
    Ceritinib-platinum(IV)-4-phenylbutyrate

    		Apoptosis Cancer
    Ceritinib-platinum(IV)-4-phenylbutyrate (complex 7) is a Ceritinib (HY-15656)-conjugated Platinum(IV) prodrug with anticancer activity. Ceritinib-platinum(IV)-4-phenylbutyrate induces S-phase arrest, DNA damage responses, and apoptosis. Ceritinib-platinum(IV)-4-phenylbutyrate combines cytotoxicity with immune and anti-invasive activation in cancer cell models. Ceritinib-platinum(IV)-4-phenylbutyrate can be used for cancer research, such as non-small cell lung cancer (NSCLC) .
    Ceritinib-platinum(IV)-4-phenylbutyrate
  • 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-134160S
    5,6-Dihydro-5-Fluorouracil-13C,15N2

    5-DHFU-13C,15N2; 5-Fluorodihydropyrimidine-2,4-dione-13C,15N2; 5-Fluorodihydrouracil-13C,15N2

    		 Isotope-Labeled Compounds Nucleoside Antimetabolite/Analog Cancer
    5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
    5,6-Dihydro-5-Fluorouracil-13C,15N2
  • HY-W811579
    Bensuldazic acid

    		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-W811579A
    Bensuldazic acid sodium

    		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-176149
    Fluoxetine-Conjugated Platinum(IV) prodrug-1

    		CaMK MMP AMPK Apoptosis Autophagy Cancer
    Fluoxetine-Conjugated Platinum(IV) prodrug-1 (Compound 8) is an eEF2K inhibitor. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits cancer cell proliferation, induces DNA damage, cell cycle arrest at S phase and apoptosis. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces ROS accumulation and mitochondrial dysfunction. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits TNBC cell migration and invasion by inhibiting MMP-2 activity. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces autophagy in TNBC cells by activating AMPK. Fluoxetine-Conjugated Platinum(IV) prodrug-1 has antitumor activity and activates immunosuppression in the 4T1-Luc mouse model. Fluoxetine-Conjugated Platinum(IV) prodrug-1 can be used in triple-negative breast cancer (TNBC) research .
    Fluoxetine-Conjugated Platinum(IV) prodrug-1
  • HY-175201
    pro-FTY

    		LPL Receptor STAT Cancer
    pro-FTY, a FTY720 (HY-12005) anticancer prodrug, is a sphingosine-1-phosphate (S1P) (HY-108496) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel (HY-B0015) or Doxorubicin (HY-15142A). pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia .
    pro-FTY
  • HY-178451
    NQO1-responsive prodrug

    		Apoptosis Cancer
    NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research .
    NQO1-responsive prodrug
  • HY-169832
    Sulfanegen

    		Drug Intermediate Others
    Sulfanegen is a 3-mercaptopyruvate prodrug and cyanide antidote. Sulfanegen converts toxic cyanide into a relatively non-toxic substance. Sulfanegen, alone or in combination with Cobinamide, has detoxification effect in mouse models of cyanide poisoning .
    Sulfanegen
  • HY-159924
    DBPR116

    		Opioid Receptor Neurological Disease
    DBPR116 is a prodrug of BPRMU191 (HY-159923) with blood-brain barrier penetration capability. DBPR116 significantly improves the delivery of centrally targeted drugs. In combination with the antagonist Naltrexone (HY-76711), DBPR116 demonstrated superior safety and analgesic efficacy compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a prodrug strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing potential as a safer opioid analgesic .
    DBPR116
  • HY-168143
    YD1342

    		Histone Methyltransferase Cancer
    YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors. .
    YD1342
  • HY-174433
    PAN endonuclease-IN-4

    		Influenza Virus Infection
    PAN endonuclease-IN-4 (Compound 41) is an inhibitor of PAN endonuclease with antiviral properties. PAN endonuclease-IN-4 is the prodrug of 39-(S). PAN endonuclease-IN-4 can significantly suppress viral replication in an A/WSN/33 infected mouse model .
    PAN endonuclease-IN-4
  • HY-149065
    D-685

    		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-106154
    DTS-201

    		Peptide-Drug Conjugates (PDCs) Aminopeptidase Cancer
    DTS-201 (CPI-0004) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
    DTS-201
  • HY-168927
    Apoptosis inducer 36

    		Apoptosis Pyroptosis PANoptosis Cancer
    Apoptosis inducer 36 (Compound 42) exhibits anti-leukemic activity through reduction of leukemia stem cells (LSCs) and induction of differentiation. Apoptosis inducer 36 inhibits the proliferation of AML cells, arrests cell cycle at G1 phase, and induces PANoptosis including apoptosis, pyroptosis and necrosis. Prodrug of apoptosis inducer 36 exhibits orally active antitumor efficacy in mouse model .
    Apoptosis inducer 36
  • HY-W747879
    Diclofenac Amide-13C6

    		Isotope-Labeled Compounds COX Inflammation/Immunology
    Diclofenac Amide- 13C6 is the 13C-labeled Diclofenac amide (HY-134521). Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
    Diclofenac Amide-13C6
  • HY-169986S
    TyK2-IN-21-d3

    		JAK Inflammation/Immunology
    TyK2-IN-21-d3 (Compound 3c) is the orally active prodrug of the tyrosine kinase 2. TyK2-IN-21-d3 exhibits good chemical stability in aqueous system under different pHs. TyK2-IN-21-d3 alleviates the effect of gastric acid changes on drug absorption and improve the drug bioavailability in rat model .
    TyK2-IN-21-d3
  • HY-176712
    GSNOR-IN-1

    		GSNOR Apoptosis Neurological Disease
    GSNOR-IN-1, a prodrug of GSNOR-IN-2 (HY-176275), is a BBB-penetrable S-nitrosoglutathione reductase (GSNOR) inhibitor. GSNOR-IN-1 has significant protective activity against OGD/R-induced injury. GSNOR-IN-1 regulates calcium signaling and synaptic function via Clstn1 S-nitrosation and inhibits neuronal apoptosis. GSNOR-IN-1 significantly reduces infarct volume while improving neurological deficits in ischemic stroke rat models. GSNOR-IN-1 has neuroprotective activity, promising for ischemic stroke research .
    GSNOR-IN-1
  • HY-17484R
    Ampiroxicam (Standard)

    CP 65703 (Standard)

    		 Reference Standards Inflammation/Immunology
    Ampiroxicam (Standard) is the analytical standard of Ampiroxicam. This product is intended for research and analytical applications. Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases.
    Ampiroxicam (Standard)
  • HY-15334
    CEP-5214

    		VEGFR Cancer
    CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
    CEP-5214
  • HY-182360
    Cytisine-platinum(IV) prodrug-1

    		PERK Eukaryotic Initiation Factor (eIF) Bcl-2 Family Apoptosis Reactive Oxygen Species (ROS) STING DNA/RNA Synthesis PD-1/PD-L1 Cancer
    Cytisine-Platinum(IV) Prodrug-1 is a Pt(IV) prodrug incorporating the natural compound Cytisine (HY-N0175) with antiproliferative activity against tumor cells. Cytisine-Platinum(IV) Prodrug-1 promotes calcium transfer across the IP3R1-GRP75-VDAC1 axis to drive mitochondrial calcium overload. Cytisine-Platinum(IV) Prodrug-1 initiates unfolded protein response via PERK, eIF2α, ATF4, and CHOP to modulate Bcl-2 and Bax, triggering apoptosis. Cytisine-Platinum(IV) Prodrug-1 induces mitochondrial dysfunction, ROS production, reduced ATP synthesis, DNA damage, and S-phase cell cycle arrest. Cytisine-Platinum(IV) Prodrug-1 activates the cGAS-STING pathway, reduces PD-L1 expression, drives immunogenic cell death. Cytisine-Platinum(IV) Prodrug-1 exhibits high physiological stability, efficient cellular accumulation, and enhanced platinum-DNA binding, and inhibits tumor growth in mouse models with reduced systemic toxicity. Cytisine-Platinum(IV) Prodrug-1 can be used for the research of lung cancer .
    Cytisine-platinum(IV) prodrug-1
  • HY-185585
    JNJ-27548547

    		Drug Intermediate Cancer
    JNJ-27548547, Mitomycin C (HY-13316) prodrug, is a Mitomycin C and lipophilic group conjugate. JNJ-27548547 undergoes thiolytic cleavage of its dithiobenzyl linker in the presence of reducing agents to release active substance Mitomycin C. JNJ-27548547 is formulated into pegylated liposomes (PL-MLP) with high antitumor activity in mice models .
    JNJ-27548547
  • HY-179719
    Anti-MRSA agent 41

    		Bacterial Drug Intermediate Infection
    Anti-MRSA agent 41 (Compound 3d) is a prodrug of Mupirocin (HY-B0958), being a cholesterol disulfide conjugate of Mupirocin. Anti-MRSA agent 41 shows no antibacterial activity or cytotoxicity in vitro. Anti-MRSA agent 41 demonstrates strong anti-MRSA infection efficacy in systemic bacteremia and pneumonia mouse models. Anti-MRSA agent 41 can be used in antibiotic resistance research .
    Anti-MRSA agent 41
  • HY-181777
    Mal-Pip-ValCit-PAB-AZ7550

    		EGFR Cancer
    Mal-Pip-ValCit-PAB-AZ7550 is a prodrug of EGFR inhibitor. Mal-Pip-ValCit-PAB-AZ7550 selectively binds covalently to albumin via its maleimide moiety. Mal-Pip-ValCit-PAB-AZ7550 exhibits potent in vivo anticancer activity in non-small cell lung cancer xenograft models. Mal-Pip-ValCit-PAB-AZ7550 can be used in research related to non-small cell lung cancer .
    Mal-Pip-ValCit-PAB-AZ7550
  • HY-181865
    BuChE-IN-22

    		Cholinesterase (ChE) Drug Intermediate Neurological Disease
    BuChE-IN-22 is a pseudo-irreversible butyrylcholinesterase (BuChE) inhibitor, with IC50 values of 4 nM and 157 nM against hBuChE and hAChE, respectively. It also acts as a prodrug of 7-hydroxysertraline. BuChE-IN-22 releases 7-hydroxysertraline during BuChE inhibition. BuChE-IN-22 completely reverses Aβ25-35-induced short-term and long-term memory impairments in a mouse model of Alzheimer's disease. BuChE-IN-22 can be used in research related to Alzheimer's disease .
    BuChE-IN-22
  • HY-182268
    Antibiofilm agent-21

    		Bacterial Interleukin Related TNF Receptor Infection Inflammation/Immunology
    Antibiofilm agent-21 is an orally active prodrug of Antibiofilm agent-20 (HY-182268) with glucuronidation. Antibiofilm agent-21 avoids absorption in the small intestine via reduced membrane permeability, improving colon delivery rate, and converts to its active form in the colon. Antibiofilm agent-21 increases colon length and reduces IL-17 and TNF-α levels in a murine DSS (HY-116282C)-induced colitis model. Antibiofilm agent-21 can be used for the research of inflammatory bowel disease .
    Antibiofilm agent-21
  • HY-185150
    PMEG

    9-(2-Phosphonylmethoxy)ethylguanine

    		 DNA/RNA Synthesis CMV Infection Inflammation/Immunology Cancer
    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].
    PMEG
  • HY-111103A
    CZh226 hydrochloride

    		PAK Cancer
    CZh226 hydrochloride is a potent and selective PAK4 inhibitor with an IC50 of 18 nM, and its selectivity for PAK1 is 346 times. The oral bioavailability of CZh226 hydrochloride is poor, and it requires the use of the prodrug PAK4-IN-1 (HY-130628) to improve absorption and metabolic stability. CZh226 hydrochloride can be used for research on colorectal cancer and melanoma .
    CZh226 hydrochloride
  • HY-179379
    EP4 receptor agonist 3 prodrug

    		Drug Derivative Inflammation/Immunology
    EP4 receptor agonist 3 prodrug (Compound 9) is a prodrug of EP4 receptor agonist (Compound 1a). EP4 receptor agonist 3 prodrug itself has no agonistic activity on the EP4 receptor and needs to be specifically hydrolyzed by intestinal alkaline phosphatase (IAP) in the intestine to release the active molecule, which then exerts the EP4 receptor agonistic effect locally in the intestine. EP4 receptor agonist 3 prodrug has colonic targeting properties and significantly alleviates colitis in mice .
    EP4 receptor agonist 3 prodrug

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