1. Search Result
Search Result
Results for "

prodrug

" in MCE Product Catalog:

247

Inhibitors & Agonists

11

Natural
Products

9

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-B1323
    Dipivefrin hydrochloride

    Dipivefrine hydrochloride

    Others Neurological Disease
    Dipivefrin hydrochloride (Dipivefrine hydrochloride) is an antiglaucoma prodrug that is hydrolyzed to the active compound, epinephrine, by esterases in the cornea.
  • HY-141692
    IL-17 modulator 4

    Interleukin Related Inflammation/Immunology
    IL-17 modulator 4 is a prodrug of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator.
  • HY-U00046
    Apyramide

    COX Inflammation/Immunology
    Apyramide is an anti-inflammatory agent (NSAID) and behaves as a prodrug of indomethacin (HY-14397). Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2.
  • HY-132815
    Fostroxacitabine bralpamide

    MIV-818

    Nucleoside Antimetabolite/Analog Cancer
    Fostroxacitabine bralpamide (MIV-818) is an orally active Troxacitabine-based nucleotide prodrug. Fostroxacitabine bralpamide has anticancer effects.
  • HY-117606
    LY3027788

    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.
  • HY-117606A
    LY3027788 hydrochloride

    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.
  • HY-108060
    Valopicitabine

    NM283

    HIV Infection
    Valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2'-C-methylcytidine, acts as a promising antiviral agent for reasearch of chronic HCV infection.
  • HY-B0255
    Adefovir dipivoxil

    GS 0840

    HBV Reverse Transcriptase Infection Cancer
    Adefovir dipivoxil, an adenosine analogue, is an oral prodrug of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains.
  • HY-13598
    Valecobulin

    CKD-516

    Microtubule/Tubulin Cancer
    Valecobulin (CKD516) is a valine prodrug of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
  • HY-131336
    MGS0274

    mGluR Neurological Disease
    MGS0274, an ester-based lipophilic prodrug of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia.
  • HY-14737
    Ceftaroline fosamil

    TAK-599; PPI0903

    Bacterial Antibiotic Infection
    Ceftaroline fosamil (TAK-599), a cephalosporin derivative, is an N-phosphono prodrug of anti-methicillin-resistant Staphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil can be used for the research of MRSA infection.
  • HY-102032A
    (RS)-Butyryltimolol

    Adrenergic Receptor Others
    (RS)-Butyryltimolol is the racemate of Butyryltimolol. Butyryltimolol, an effective prodrug of Timolol, improves the corneal penetration of Timolol. Butyryltimolol is a β-adrenergic blocker.
  • HY-135655
    Fobrepodacin disodium

    SPR720 disodium; pVXc-486 disodium

    Bacterial Infection
    Fobrepodacin (SPR720) disodium is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). Fobrepodacin disodium has potent bactericidal activities in vivo.
  • HY-B0225B
    Methyldopa hydrate

    L-(-)-α-Methyldopa hydrate; MK-351 hydrate

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
  • HY-B0225A
    Methyldopa hydrochloride

    L-(-)-α-Methyldopa hydrochloride; MK-351 hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
  • HY-B0225
    Methyldopa

    L-(-)-α-Methyldopa; MK-351

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Methyldopa (L-(-)-α-Methyldopa), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
  • HY-116016
    Etilevodopa

    L-DOPA ethyl ester; Levodopa ethyl ester

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester), an ethyl-ester prodrug of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable prodrug as it facilitates CNS penetration and delivers dopamine.
  • HY-116016A
    Etilevodopa hydrochloride

    L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester prodrug of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa hydrochloride is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable prodrug as it facilitates CNS penetration and delivers dopamine.
  • HY-14738
    Ceftaroline fosamil inner salt

    TAK-599 free acid; PPI0903 free acid

    Bacterial Antibiotic Infection
    Ceftaroline fosamil (TAK-599) inner salt, a cephalosporin derivative, is an N-phosphono prodrug of anti-methicillin-resistant Staphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil inner salt can be used for the research of MRSA infection.
  • HY-13598A
    Valecobulin hydrochloride

    CKD-516 hydrochloride

    Microtubule/Tubulin Cancer
    Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
  • HY-14554
    Pomaglumetad methionil anhydrous

    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.
  • HY-100373
    Isavuconazonium sulfate

    BAL8557-002

    Fungal Infection
    Isavuconazonium sulfate (BAL8557-002), the prodrug of the active triazole Isavuconazole, is an orally active antifungal agent. Isavuconazonium sulfate is used for invasive aspergillosis and mucormycosis.
  • HY-138943
    5-Fluorouridine 5'-O-β-D-galactopyranoside

    5'-O-β-D-galactosyl-5-fluorouridine

    Others Cancer
    5-Fluorouridine 5'-O-β-D-galactopyranoside (5'-O-β-D-galactosyl-5-fluorouridine) is a 5-Fluorouridine prodrug. 5-Fluorouridine 5'-O-β-D-galactopyranoside can be converted by the enzyme β-D-galactosidase to the potent antineoplastic agent 5-Fluorouridine.
  • HY-14273S
    Isavuconazole D4

    BAL-4815 D4; RO-0094815 D4

    Fungal Cytochrome P450 Infection
    Isavuconazole D4 (BAL-4815 D4) is a deuterium labeled Isavuconazole (BAL-4815). Isavuconazole is a triazole prodrug with antifungal activity against yeasts, molds, and dimorphic fungi.
  • HY-105040
    Pomaglumetad methionil

    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.
  • HY-A0019A
    Paliperidone palmitate

    9-Hydroxyrisperidone palmitate

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia.
  • HY-14273
    Isavuconazole

    BAL-4815; RO-0094815

    Fungal Cytochrome P450 Antibiotic Infection
    Isavuconazole (BAL-4815) is a triazole prodrug with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4.
  • HY-10274
    Dabigatran etexilate

    BIBR 1048

    Others Cardiovascular Disease
    Dabigatran etexilate (BIBR 1048) is an orally active prodrug of Dabigatran. Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
  • HY-14532
    Brincidofovir

    CMX001; HDP-CDV

    CMV HSV 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.
  • HY-123875A
    Ralaniten triacetate

    EPI-506

    Androgen Receptor Cancer
    Ralaniten triacetate (EPI-506), the pro-drug of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7.
  • HY-10274A
    Dabigatran etexilate mesylate

    BIBR 1048MS; Dabigatran etexilate methanesulfonate

    Others Cardiovascular Disease
    Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
  • HY-A0035
    Faropenem

    Antibiotic Infection
    Faropenem is a potent and orally active beta-lactam antibiotic. Faropenem demonstrates broad-spectrum in vitro antimicrobial activity against many gram-positive and -negative aerobes and anaerobes. Faropenem is resistant to hydrolysis by nearly all beta-lactamases, including extended-spectrum beta-lactamases and AmpC beta-lactamases. Faropenem is developed as an oral prodrug, faropenem medoxomil, for the research of respiratory tract infections.
  • HY-B0390
    Mestranol

    Estrogen Receptor/ERR Cancer Endocrinology
    Mestranol is an inactive prodrug and becomes biologically active on conversion to ethinyl estradiol (EE). Mestranol acts as an estrogen receptor agonist. Mestranol combines with a progestin in vivo and can be used for the research of menopausal hormone or menstrual disorders.
  • HY-13337
    BMS-986094

    INX-08189

    HCV Infection
    BMS-986094 (INX-08189) is a potent inhibitor of hepatitis C virus (HCV) replication, with an EC50 of 35 nM at 24 h in Huh-7 cells. BMS-986094 is a phosphoramidate prodrug of 6-O-methyl-2’-C-methyl guanosine. BMS-986094 can be used for the research of chronic HCV infection.
  • HY-133027
    Myristyl nicotinate

    Tetradecyl nicotinate

    Others Cancer
    Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug and a lipophilic derivative of Nicotinic acid. Myristyl nicotinate is being developed for delivery of Nicotinic acid into the skin for prevention of actinic keratosis and its progression to skin cancer. Myristyl nicotinate shows to stimulate epidermal differentiation in photodamaged skin, increasing skin NAD content and strengthening the skin barrier.
  • HY-13630
    Etoposide phosphate

    BMY-40481

    Topoisomerase Bacterial Autophagy Apoptosis Cancer Infection Neurological Disease
    Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
  • HY-122487
    Troriluzole

    BHV-4157

    Others Neurological Disease
    Troriluzole, a third-generation, tripeptide prodrug of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
  • HY-13630A
    Etoposide phosphate disodium

    BMY-40481 disodium

    Topoisomerase Autophagy Apoptosis Cancer Neurological Disease
    Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
  • HY-W011404
    Tributyrin

    Glyceryl tributyrate

    Apoptosis Metabolic Disease
    Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
  • HY-135124
    DC44SMe

    ADC Cytotoxin Cancer
    DC44SMe, a phosphate prodrug of cytotoxic DNA alkylator DC44, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC44SMe exhibits IC50s of 2.0 nM, 2.8 nM, and 1.9 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC44SMe can be used for the targeted treatment of cancer.
  • HY-135123
    DC4SMe

    ADC Cytotoxin Cancer
    DC4SMe, a phosphate prodrug of cytotoxic DNA alkylator DC4, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4SMe exhibits IC50s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer.
  • HY-18257
    Rolitetracycline

    Bacterial Antibiotic Infection
    Rolitetracycline, a derivative of tetracycline, is a broad-spectrum antibiotic. Rolitetracyclin has a role as a protein synthesis inhibitor, an antiprotozoal drug and a prodrug.
  • HY-B1152
    Piperacetazine

    Others Neurological Disease
    Piperacetazine is an antipsychotic prodrug, used forschizophrenia.
  • HY-14945
    Remogliflozin etabonate

    GSK189075

    SGLT Metabolic Disease
    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 prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.
  • HY-13061
    Daun02

    Topoisomerase ADC Cytotoxin Cancer
    Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin.
  • HY-101714
    Oxyphenisatin acetate

    Autophagy Cancer
    Oxyphenisatin acetate, the pro-drug of oxyphenisatin, is used to be a laxative.
  • HY-B1657A
    Fosphenytoin disodium

    Others Neurological Disease
    Fosphenytoin sodium is a phenytoin prodrug with similar anticonvulsant properties.
  • HY-100666
    Fosfluconazole

    Fungal Infection
    Fosfluconazole is a prodrug of Fluconazole that is widely used as an antifungal agent.
  • HY-A0032A
    Valganciclovir hydrochloride

    CMV Infection
    Valganciclovir (hydrochloride), the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir.
  • HY-B1149A
    Bacampicillin hydrochloride

    Bacterial Antibiotic Infection
    Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
  • HY-B1149
    Bacampicillin

    Bacterial Antibiotic Infection
    Bacampicillin is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
  • HY-B2102
    Oxyphenisatine

    Oxyphenisatin

    Others Cancer
    Oxyphenisatine (Oxyphenisatin) is a laxative. Oxyphenisatin acetate is the pro-drug of oxyphenisatin with anticancer activity.
  • HY-106349
    Fosteabine

    Cytarabine ocfosfate; YNK 01

    Nucleoside Antimetabolite/Analog Cancer
    Fosteabine is an oral and prodrug analogue of cytarabine which is resistant to deoxycytidine deaminase.
  • HY-101710
    GLN-1062

    Others Neurological Disease
    Memogain is a pro-drug of galantamine, used for the treatment for Alzheimer’s disease.
  • HY-16445
    Sapacitabine

    CS682; CYC682

    Nucleoside Antimetabolite/Analog Cancer
    Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.
  • HY-133145
    hDDAH-1-IN-2

    Others Neurological Disease Inflammation/Immunology
    hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability.
  • HY-115292
    Simvastatin hydroxy acid sodium

    Tenivastatin sodium; Simvastatin Impurity A sodium

    HMG-CoA Reductase (HMGCR) Cancer
    Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
  • HY-16216
    Gabapentin enacarbil

    XP-13512

    Calcium Channel Neurological Disease
    Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.
  • HY-N0666
    L-Aspartic acid

    Endogenous Metabolite Cardiovascular Disease
    L-Aspartic acid is is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly.
  • HY-B0810
    Pivmecillinam

    FL-1039

    Bacterial Antibiotic Infection
    Pivmecillinam (FL-1039) is an orally active prodrug of mecillinam, an extended-spectrum penicillin antibiotic.
  • HY-B0810A
    Pivmecillinam hydrochloride

    FL-1039 hydrochloride

    Bacterial Antibiotic Infection
    Pivmecillinam hydrochloride (FL-1039 hydrochloride) is an orally active prodrug of mecillinam, an extended-spectrum penicillin antibiotic.
  • HY-B0016
    Capecitabine

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Capecitabine is an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase.
  • HY-16363
    Omtriptolide

    ERK Inflammation/Immunology
    Omtriptolide (PG490-88) is a derivative prodrug of triptolide purified from the Chinese herb.
  • HY-12758
    YHO-13351

    BCRP Cancer
    YHO-13351 is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-17357
    Nepafenac

    AHR 9434; AL 6515

    COX Inflammation/Immunology
    Nepafenac(AHR 9434; AL 6515; Nevanac) is a selective COX-2 inhibitor; is prodrug of Amfenac.
  • HY-B1079
    Suxibuzone

    Others Inflammation/Immunology
    Suxibuzone is a drug used for joint and muscular pain, is a prodrug of the non steroidal anti inflammatory drug Phenylbutazone.
  • HY-B0477
    Quinapril hydrochloride

    CI-906

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinapril (hydrochloride) (CI-906) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications.
  • HY-14932
    Pafuramidine

    DB289

    Parasite Antibiotic Infection
    Pafuramidine (DB289) is an orally bioavailable prodrug of furamidine, which has activity against Pneumocystis pneumonia.
  • HY-13239
    LY2979165

    mGluR Neurological Disease
    LY2979165 is the alanine prodrug of 2812223, a selective and potent orthosteric mGlu2 receptor agonist.
  • HY-U00148
    KY-556

    N556

    Others Inflammation/Immunology
    KY-556 is a promising and orally-active pro-drug of disodium cromoglycate (DSCG) against allergic diseases.
  • HY-19748
    LED209

    Bacterial Infection
    LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC.
  • HY-N0666C
    L-Aspartic aicd sodium

    Sodium L-aspartate

    Endogenous Metabolite Others
    L-Aspartic aicd sodium is is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly.
  • HY-111749
    JAK-IN-4

    JAK Inflammation/Immunology
    JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model.
  • HY-A0032
    Valganciclovir

    CMV Infection
    Valganciclovir, the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir. Valganciclovir is an antiviral medication used to treat cytomegalovirus infections.
  • HY-12758A
    YHO-13351 free base

    BCRP Cancer
    YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  • HY-109131
    Foscarbidopa

    Carbidopa 4′-monophosphate

    Dopamine Receptor Neurological Disease
    Foscarbidopa (Carbidopa 4′-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist.
  • HY-B0382
    Fosinopril sodium

    SQ28555

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.
  • HY-133105
    Oxothiazolidinecarboxylic acid

    Others Inflammation/Immunology
    Oxothiazolidinecarboxylic acid, an antioxidant, is a prodrug of cysteine that is inert until metabolized to cysteine intracellulary, thus stimulating glutathione synthesis.
  • HY-17615
    Fosnetupitant

    Pronetupitant

    Neurokinin Receptor Neurological Disease
    Fosnetupitant (Pronetupitant) a methylene phosphate prodrug of Netupitant. Fosnetupitant (Pronetupitant) exhibits a pKi of 9.5 for human NK1 receptor.
  • HY-17400
    Tegafur

    FT 207; NSC 148958

    Nucleoside Antimetabolite/Analog Cancer
    Tegafur (FT 207; NSC 148958) is a chemotherapeutic 5-FU prodrug used in the treatment of cancers; is a component of tegafur-uracil.
  • HY-13640
    Rabacfosadine

    GS-9219; VDC-1101

    Others Cancer
    Rabacfosadine (GS-9219), a novel prodrug of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells.
  • HY-A0169
    Methyl aminolevulinate

    Others Cancer Inflammation/Immunology
    Methyl aminolevulinate is an agent used as a sensitizer in photodynamic therapy (PDT). Methyl aminolevulinate is a prodrug that can be metabolized to Protoporphyrin IX.
  • HY-A0169A
    Methyl aminolevulinate hydrochloride

    Others Cancer Inflammation/Immunology
    Methyl aminolevulinate hydrochloride is an agent used as a sensitizer in photodynamic therapy (PDT). Methyl aminolevulinate is a prodrug that can be metabolized to Protoporphyrin IX.
  • HY-111494
    TRPA1 Antagonist 1

    TRP Channel Neurological Disease
    TRPA1 Antagonist 1 is a methylene phosphate prodrug which converts to its active parent drug, a TRPA1 antagonist with an IC50 of 8 nM.
  • HY-15232
    Tenofovir alafenamide

    GS-7340

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide (GS-7340) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-15232A
    Tenofovir alafenamide fumarate

    GS-7340 (fumarate)

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-B0806
    Proguanil

    Parasite Antifolate Infection
    Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
  • HY-A0273
    Propyphenazone

    4-Isopropylantipyrine; Isopropylphenazone

    COX Inflammation/Immunology
    Propyphenazone is a pyrazolone derivative with anti-inflammatory, analgesic and antipyretic activity, Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
  • HY-B0806A
    Proguanil hydrochloride

    Parasite Antifolate Infection
    Proguanil hydrochloride, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
  • HY-126253
    BI-4916

    Others Cancer
    BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD +-competitive PHGDH inhibitor.
  • HY-17501
    Bambuterol

    (±)-Bambuterol; KWD-2183

    Adrenergic Receptor Endocrinology
    Bambuterol ((±)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
  • HY-109754
    PF 03709270

    ulopenem etzadroxil

    Bacterial Infection
    PF 03709270 is an orally available ester prodrug form of sulopenem, with broad-spectrum antibacterial activity against most gram-positive and gram-negative bacteria.
  • HY-16261B
    MC-DOXHZN hydrochloride

    (E/Z)-Aldoxorubicin hydrochloride; Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride

    Topoisomerase Drug-Linker Conjugates for ADC Cancer
    MC-DOXHZN ((E/Z)-Aldoxorubicin) hydrochloride is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
  • HY-17501A
    Bambuterol hydrochloride

    (±)-Bambuterol hydrochloride; KWD-2183 hydrochloride

    Adrenergic Receptor Endocrinology
    Bambuterol hydrochloride ((±)-Bambuterol hydrochloride; KWD-2183 hydrochloride) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
  • HY-109105
    Tepilamide fumarate

    XP-23829

    Others Inflammation/Immunology
    Tepilamide fumarate (XP-23829) is an oral fumaric acid ester, acts as a prodrug of monomethyl fumarate, and is used in the research of moderate to severe chronic plaque psoriasis.
  • HY-16261A
    MC-DOXHZN

    (E/Z)-Aldoxorubicin; Doxorubicin(6-maleimidocaproyl)hydrazone

    Topoisomerase Drug-Linker Conjugates for ADC Cancer
    MC-DOXHZN ((E/Z)-Aldoxorubicin) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
  • HY-124584
    Minnelide

    Apoptosis Cancer
    Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis.
  • HY-13609
    Deflazacort

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Deflazacort, a glucocorticoid, is an inactive prodrug and is converted rapidly to the active metabolite 21-desacetyldeflazacort. Deflazacort is used as an anti-inflammatory and immunosuppressant.
  • HY-17431
    Fosamprenavir Calcium Salt

    GW433908G

    HIV Infection
    Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
  • HY-106574
    Ceftobiprole medocaril

    BAL5788

    Bacterial Infection
    Ceftobiprole medocaril is the parenteral prodrug of Ceftobiprole (HY-112579). Ceftobiprole is a broad-spectrum cephalosporin with activity against Methicillin-resistant staphylococcus aureus (MRSA).
  • HY-12045
    HMN-214

    IVX-214

    Polo-like Kinase (PLK) Cancer
    HMN-214, an orally bioavailable prodrug of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
  • HY-A0110A
    Cefotiam hexetil hydrochloride

    CTM-HE hydrochloride; SCE-2174 hydrochloride

    Bacterial Antibiotic Infection
    Cefotiam hexetil hydrochloride (CTM-HE) is an oral third-generation cephalosporin, which is a prodrug of cefotiam, but has no anti-bacterial property. Cefotiam is an antibiotic.
  • HY-101682
    SCH 42495

    Neprilysin Cardiovascular Disease
    SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • HY-78726
    Fosamprenavir

    Amprenavir phosphate; GW 433908

    HIV Infection
    Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
  • HY-75054
    Abiraterone acetate

    CB7630

    Cytochrome P450 Cancer
    Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a prodrug form of Abiraterone (CB7598).
  • HY-15232B
    Tenofovir alafenamide hemifumarate

    GS-7340 (hemifumarate)

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-B0559
    Nabumetone

    BRL14777

    COX Inflammation/Immunology Cancer
    Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA.
  • HY-10535
    Evofosfamide

    TH-302

    Apoptosis Cancer
    Evofosfamide (TH-302) is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
  • HY-19214
    Elisartan

    HN 65021

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    Elisartan is an orally active non-peptide pro-drug of angiotensin II AT1 receptor antagonist HN-12206, and shows anti-hypertension activities.
  • HY-16511
    Upamostat

    WX-671

    Ser/Thr Protease PAI-1 Cancer
    Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
  • HY-101873
    Atorvastatin lactone

    HMG-CoA Reductase (HMGCR) Metabolic Disease Inflammation/Immunology
    Atorvastatin lactone is a prodrug form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.
  • HY-115460
    AER-271

    Others Neurological Disease Cardiovascular Disease
    AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor for the research of acute ischemic stroke.
  • HY-B1582A
    Canrenoate potassium

    Aldadiene potassium; SC-14266

    Mineralocorticoid Receptor Cardiovascular Disease
    Canrenoate (Aldadiene) potassium, a prodrug that releases canrenone, is a potent, competitive mineralocorticoid receptor (aldosterone receptor) antagonist. Potassium canrenoate, as a diuretic, is used for the research of hypertension.
  • HY-B0069
    Fludarabine

    F-ara-A; NSC 118218

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis STAT Apoptosis Cancer
    Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which also inhibits phosphorylation of STAT1. Fludarabine, a pro-drug, is converted metabolically by dephosphorylation to the antimetabolite, F-ara-A.
  • HY-14844
    Lagociclovir

    MIV-210

    HBV Infection
    Lagociclovir(MIV-210) is a prodrug of 3'-fluoro-2',3'-dideoxyguanosine with high oral bioavailability in humans and potent activity against HBV.
  • HY-N7114A
    Chloramphenicol succinate sodium

    Bacterial Antibiotic Metabolic Disease Infection
    Chloramphenicol succinate sodium is a prodrug of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity.
  • HY-124955
    proTAME

    APC Cancer
    proTAME, a cell-permeable prodrug form of TAME, is an anaphase promoting complex/cyclosome (APC/C) inhibitor. proTAME causes cell cycle arrest in metaphase.
  • HY-B0016S
    Capecitabine-d11

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Capecitabine-d11 is the deuterium labeled Capecitabine. Capecitabine is an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase.
  • HY-12424A
    42-(2-Tetrazolyl)rapamycin

    Others Cancer
    42-(2-Tetrazolyl)rapamycin is a prodrug compound of a rapamycin analog extracted from patent US 20080171763 A1, Example 1. Rapamycin is a specific mTOR inhibitor.
  • HY-16779
    Fosravuconazole

    BMS-379224; E-1224

    Fungal Parasite Infection
    Fosravuconazole (BMS-379224), a prodrug of Ravuconazole, is an orally active broad spectrum antifungal agent. Fosravuconazole can be used for candidiasis, onychomycosis and parasitemia research.
  • HY-108715A
    RT-AM

    Others Neurological Disease
    RT-AM is a pro-drug real thiol. Real Thiol is a reversible reaction-based fluorescent probe which can quantitatively monitor the real-time glutathione dynamics in living cells.
  • HY-137459
    Vocacapsaicin

    CA-008

    TRP Channel Neurological Disease
    Vocacapsaicin (CA-008), a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief.
  • HY-108045
    Lodenafil carbonate

    Phosphodiesterase (PDE) Endocrinology
    Lodenafil carbonate, a dimer that acts as a prodrug delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
  • HY-135655A
    Fobrepodacin

    SPR720; pVXc-486

    Bacterial Infection
    Fobrepodacin (SPR720) is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). Fobrepodacin has potent bactericidal activities in vivo.
  • HY-101682A
    SCH 42495 racemate

    Neprilysin Cardiovascular Disease
    SCH 42495 racemate is the racemate of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • HY-19886
    F 16915

    Others Cardiovascular Disease
    F 16915, a Docosahexaenoic Acid (DHA, HY-B2167) derivative, is a potent pro-drug of DHA. F 16915 can prevent heart failure-induced atrial fibrillation.
  • HY-138181
    Contezolid phosphoramidic acid

    Others Others
    Contezolid phosphoramidic acid is an intermediate in the synthesis of prodrugs of antibacterial oxazolidinone agent MRX-I. Contezolid phosphoramidic acid is extracted from patent WO2015127316A1, Intermediate 3, Method I.
  • HY-B0329
    Isoniazid

    INH; Isonicotinic acid hydrazide; Isonicotinic hydrazide

    Bacterial Autophagy Mitophagy Infection
    Isoniazid (INH) is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity.
  • HY-B1147
    Diloxanide furoate

    Parasite Infection
    Diloxanide furoate is the prodrug of Diloxanide. Diloxanide furoate is a potent and orally active anti-protozoal agent and can be used for the research of amebiasis, mild intestinal amebiasis or asymptomatic cyst carriers.
  • HY-13571A
    Beclometasone dipropionate

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Betamethasone dipropionate, the prodrug of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release.
  • HY-115499
    MPC-0767

    HSP Cancer
    MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester prodrug of MPC-3100 with improved chemical stability.
  • HY-B0584
    Travoprost

    Fluprostenol isopropyl ester; AL6221; Flu-Ipr

    Prostaglandin Receptor Endocrinology
    Travoprost (Fluprostenol isopropyl ester), an isopropyl ester prodrug, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension.
  • HY-15284
    Prasugrel

    PCR 4099

    P2Y Receptor Cardiovascular Disease
    Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-14407
    Fosaprepitant

    L-758298

    Neurokinin Receptor Neurological Disease Endocrinology
    Fosaprepitant (L-785298) is a prodrug of Aprepitant (HY-10052). Fosaprepitant is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
  • HY-15284A
    Prasugrel hydrochloride

    PCR 4099 hydrochloride

    P2Y Receptor Cardiovascular Disease
    Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and prodrug, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-105040C
    Pomaglumetad methionil hydrochloride

    LY2140023 hydrochloride

    mGluR Neurological Disease
    Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.
  • HY-B1192
    Estradiol benzoate

    β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate

    Estrogen Receptor/ERR Endocrinology Cancer
    Estradiol Benzoate (β-Estradiol 3-benzoate), a prodrug of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.
  • HY-10309
    Sibrafiban

    RO 48-3657

    Integrin Cardiovascular Disease
    Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
  • HY-101076
    L-690488

    Phosphatase Metabolic Disease
    L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor. L-690488 has more effective cell penetration than L-690330.
  • HY-13569A
    Beraprost sodium

    Prostaglandin Receptor Inflammation/Immunology Cardiovascular Disease
    Beraprost sodium, a prostacyclin analog, is a stable and orally active prodrug of PGI2. Beraprost sodium is a potent vasodilator, has the potential for pulmonary arterial hypertension treatment through expanding renal vessels, improving microcirculation.
  • HY-15284B
    Prasugrel (Maleic acid)

    PCR 4099 (Maleic acid)

    P2Y Receptor Cardiovascular Disease
    Prasugrel (PCR 4099) Maleic acid is a thienopyridine and prodrug, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-W127442
    Etzadroxil

    Ethyl 2-Ethylbutyrate

    Others Others
    Etzadroxil (Ethyl 2-Ethylbutyrate) is a volatile ester compound. Sulopenem Etzadroxil is an orally available ester prodrug form of Sulopenem, an antibiotic with broad-spectrum activities against Gram-positive and Gram-negative bacteria.
  • HY-14407A
    Fosaprepitant dimeglumine

    MK-0517; L785298

    Neurokinin Receptor Neurological Disease Endocrinology Cancer
    Fosaprepitant dimeglumine (MK-0517) is a prodrug of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
  • HY-101682B
    (R)-SCH 42495

    Others Others
    (R)-SCH 42495 is the less active enantiomer of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • HY-109000
    Afabicin

    Debio 1450; AFN-1720

    Bacterial Infection
    Afabicin (Debio 1450) is the prodrug of Debio1452, specifically targeting staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 is an inhibitor FabI, an enzyme critical to fatty acid biosynthesis in staphylococci.
  • HY-B1325
    Cefuroxime axetil

    Bacterial Antibiotic Infection
    Cefuroxime Axetil, a prodrug of the cephalosporin cefuroxime and an oarl broad spectrum antibiotic, inhibits several gram-positive and gram-negative organisms, including those most frequently associated with various common community-acquired infections.
  • HY-B0271
    Pyrazinamide

    Pyrazinecarboxamide; Pyrazinoic acid amide

    Bacterial Autophagy Antibiotic Infection
    Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a prodrug that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
  • HY-132180A
    Seco-DUBA

    ADC Cytotoxin Cancer
    Seco-DUBA is a duocarmycin (DUBA) prodrug containing two hydroxyl groups, which can each be used for coupling to an antibody via a linker. Seco-DUBA can be used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-135470
    Nifurpirinol

    P-7138

    Antibiotic Bacterial Infection
    Nifurpirinol (P-7138) is a nitroaromatic antibiotic and acts as a novel substrate for the bacterial nitroreductase (NTR) enzyme. Nifurpirinol is a more potent prodrug compared to Metronidazole to trigger cell-ablation in nitroreductase expressing transgenic models.
  • HY-U00193
    Ro18-5362

    Others Metabolic Disease
    Ro18-5362 is the less active prodrug of Ro 18-5364. Even at concentrations as high as 0.1 mM Ro 18-5362 fails to affect significantly (H ++K +)-ATPase activity and associated proton translocation.
  • HY-107774
    BMS-986163

    iGluR Neurological Disease
    BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
  • HY-128922
    Dexamethasone palmitate

    DXP

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent.
  • HY-105019A
    Melflufen hydrochloride

    Melphalan flufenamide hydrochloride

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-108582
    Y-27152

    Potassium Channel Cardiovascular Disease
    Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.
  • HY-105019
    Melflufen

    Melphalan flufenamide

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-10127
    Barasertib

    AZD1152

    Aurora Kinase Apoptosis Cancer
    Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.
  • HY-15440A
    Fostemsavir

    BMS-663068

    HIV Infection
    Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
  • HY-B0477AS1
    Quinapril-d5 hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinapril-d5 hydrochloride (CI-906-d5) is the deuterium labeled Quinapril hydrochloride. Quinapril hydrochloride (CI-906) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications.
  • HY-19856
    FV-100

    Others Infection
    FV-100 is a potent, selective and orally active anti-varicella zoster virus agent. FV-100 is a prodrug of CF-1743. FV-100 exhibits very low toxicity in vivo.
  • HY-111950
    (-)-Ibuprofenamide

    (R)-Ibuprofenamide

    Others Inflammation/Immunology
    (-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-79369
    Succinic anhydride

    ADC Linker Cancer
    Succinic anhydride is a cyclic anhydride and a nonclaevable ADC linker extracted from patent WO2009064913A1. Succinic anhydride can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide.
  • HY-W040022
    Cefcapene pivoxil hydrochloride hydrate

    Bacterial Antibiotic Infection
    Cefcapene pivoxil hydrochloride hydrate is a prodrug and an orally active 3rd-generation cephalosporin with broad-spectrum of anti-bacterial activity. Cefcapene pivoxil hydrochloride hydrate is used for the study of palmoplantar pustulosis (PPP) and other infectious diseases.
  • HY-10443A
    Balapiravir hydrochloride

    Ro 4588161 hydrochloride; R1626 hydrochloride

    HCV DNA/RNA Synthesis Infection
    Balapiravir hydrochloride (Ro 4588161 hydrochloride; R1626 hydrochloride) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir hydrochloride has anti-HCV activity.
  • HY-10443
    Balapiravir

    Ro 4588161; R1626

    HCV DNA/RNA Synthesis Infection
    Balapiravir (Ro 4588161; R1626) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity.
  • HY-19915A
    Contezolid acefosamil

    MRX-4

    Bacterial Antibiotic Infection Inflammation/Immunology
    Contezolid acefosamil (MRX-4) is the orally active prodrug of the active antimicrobial metabolite Contezolid (MRX-I), an oxazolidinone which shows potent in vitro activity against various multidrug-resistant Gram-positive bacteria, including MRSA.
  • HY-13672
    LY2334737

    Nucleoside Antimetabolite/Analog Enterovirus Cancer Infection
    LY2334737 is an nucleoside analog and is an orally active prodrug of Gemcitabine. LY2334737 exhibits inhibitory activity against enterovirus A71 (EV-A71) infection. LY2334737 has antiviral and anticancer effects.
  • HY-128920
    Phortress free base

    Cytochrome P450 Cancer
    Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
  • HY-13458
    Droxidopa

    L-DOPS; DOPS; SM5688

    Others Neurological Disease
    Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood–brain barrier.
  • HY-B0382S
    Fosinopril-d5 sodium

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Fosinopril-d5 sodium (SQ28555-d5 sodium) is the deuterium labeled Fosinopril sodium. Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.
  • HY-16779B
    Fosravuconazole L-lysine ethanolate

    BMS-379224 L-lysine ethanolate; E-1224 L-lysine ethanolate

    Fungal Parasite Infection
    Fosravuconazole L-lysine ethanolate (BMS-379224 L-lysine ethanolate), a prodrug of Ravuconazole, is an orally active broad spectrum antifungal agent. Fosravuconazole L-lysine ethanolate can be used for candidiasis, onychomycosis and parasitemia research.
  • HY-101873S
    Atorvastatin lactone D5

    HMG-CoA Reductase (HMGCR) Metabolic Disease Inflammation/Immunology
    Atorvastatin lactone D5 is a deuterated form of Atorvastatin lactone (HY-101873). Atorvastatin lactone is a prodrug form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.
  • HY-B0592
    Trandolapril

    RU44570

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Trandolapril (RU44570) is a nonsulfhydryl prodrug that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI).
  • HY-10080
    Teglarinad chloride

    GMX1777; EB-1627

    NAMPT Cancer
    Teglarinad chloride (GMX1777) is a prodrug of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis.
  • HY-138936
    SSK1

    Apoptosis Inflammation/Immunology
    SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted prodrug attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation of p38 MAPK and induction of apoptosis.
  • HY-108751
    Aripiprazole Lauroxil

    Others Neurological Disease
    Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity.
  • HY-131233
    Anti-virus agent 1

    Others Infection
    Anti-virus agent 1 (compound 4i), a phosphoramidate prodrug of GS-5734 (HY-104077; Remdesivir), has potent antiviral activity. Anti-virus agent 1 is used for the research of coronavirus and Ebola virus (EBOV).
  • HY-15440B
    Fostemsavir Tris

    BMS-663068 Tris

    HIV Infection
    Fostemsavir Tris (BMS-663068 (Tris)) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir Tris (BMS-663068 (Tris)) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
  • HY-17425
    Valacyclovir

    Valaciclovir

    HSV Antibiotic Infection
    Valacyclovir (Valaciclovir) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir is a prodrug of Aciclovir (HY-17422) .
  • HY-19675
    Naproxen etemesil

    LT-NS 001; MX 1094

    COX Inflammation/Immunology
    Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  • HY-N7115
    Sultamicillin

    Bacterial Antibiotic Infection
    Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic beta-lactamase inhibitor which, in combination with Ampicillin, extends the antibacterial activity of the latter to include some beta-lactamase-producing strains of bacteria that would otherwise be resistant.
  • HY-17425A
    Valacyclovir hydrochloride

    Valaciclovir hydrochloride

    HSV Antibiotic Infection
    Valacyclovir hydrochloride (Valaciclovir hydrochloride) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir hydrochloride inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir hydrochloride is a prodrug of Aciclovir (HY-17422) .
  • HY-16261
    Aldoxorubicin

    INNO-206; DOXO-EMCH

    Topoisomerase ADC Cytotoxin Cancer
    Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
  • HY-B1039
    Ambroxol

    NA-872

    Glucosidase Autophagy Metabolic Disease Neurological Disease
    Ambroxol (NA-872), an active metabolite of the prodrug Bromhexine, has potent expectorant effects. Ambroxol is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.
  • HY-B1039A
    Ambroxol hydrochloride

    NA-872 hydrochloride

    Glucosidase Autophagy Metabolic Disease Neurological Disease
    Ambroxol hydrochloride (NA-872 hydrochloride), an active metabolite of the prodrug Bromhexine, has potent expectorant effects. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.
  • HY-14818A
    Laninamivir octanoate

    CS-8958

    Influenza Virus Infection
    Laninamivir octanoate (CS-8958), a prodrug of Laninamivir, is a long-acting neuraminidase (NA) inhibitor with anti-influenza virus activity. Laninamivir octanoate shows anti-influenza activity against Oseltamivir-resistant viruses, and also against the pandemic influenza viruses.
  • HY-119972
    Diloxanide

    Parasite Infection
    Diloxanide is an anti-protozoal agent and can be used for the research of asymptomatic-intestinal amebiasis caused by Entamoeba histolytica or some other protozoal infections. Diloxanide is an active luminal amebicide and hydrolyzed in the gastrointestinal tract from its prodrug Diloxanide furoate (HY-B1147).
  • HY-19447A
    Besifovir Dipivoxil maleate

    LB80380 maleate

    HBV Infection
    Besifovir Dipivoxil maleate (LB80380 maleate) is an oral prodrug of LB80317. Besifovir Dipivoxil maleate (LB80380 maleate) is effective in hepatitis B virus (HBV) DNA suppression for both treatment-naive and lamivudine-resistant chronic hepatitis B (CHB) patients in preliminary studies[2]
  • HY-100435
    Oxaquin

    MCB-3837; DNV3837

    Bacterial Infection
    Oxaquin (MCB-3837) is a injectable prodrug that is rapidly converted to the active substance MCB3681 in vivo following intravenous (i.v.) administration, active against Gram-positive bacterial species. Oxaquin (MCB-3837) itself has no antimicrobial effects.
  • HY-17449
    Fosbretabulin disodium

    CA 4DP; CA 4P; Combretastatin A4 disodium phosphate

    Microtubule/Tubulin Apoptosis Cancer
    Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent. Fosbretabulin disodium is the Combretastatin A4 prodrug that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis.
  • HY-A0230A
    Spirapril hydrochloride

    SCH 33844 hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active prodrug of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
  • HY-16405
    PR-104

    DNA Alkylator/Crosslinker Cancer
    PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.
  • HY-109025A
    Baloxavir

    Baloxavir acid; S-033447

    Influenza Virus Infection
    Baloxavir (Baloxavir acid), derived from the prodrug Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity.
  • HY-14833
    Atiratecan

    TP300

    Others Cancer
    Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models.
  • HY-16406
    PR-104 sodium

    DNA Alkylator/Crosslinker Cancer
    PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.
  • HY-100375
    Diroximel fumarate

    ALKS 8700; BIIB098

    Others Others
    Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) prodrug in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS).
  • HY-75385
    Zaurategrast ethyl ester

    CDP323; UCB1184197

    Integrin Inflammation/Immunology
    Zaurategrast ethyl ester (CDP323), the ethyl ester prodrug of CT7758, is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders.
  • HY-B0199
    Mycophenolate Mofetil

    RS 61443; TM-MMF

    Drug Metabolite Apoptosis Cancer
    Mycophenolate mofetil (RS 61443) is the morpholinoethylester prodrug of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation.
  • HY-128775
    JHU395

    Others Cancer
    JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) prodrug. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST.
  • HY-19304
    Amelubant

    BIIL 284

    Leukotriene Receptor Inflammation/Immunology
    Amelubant (BIIL 284) is a potent, oral and long acting LTB4 receptor antagonist, negligibly binds to LTB4 receptor, with Kis of 221 nM and 230 nM in vital cells and membranes. Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity.
  • HY-19851
    Rovafovir etalafenamide

    GS-9131

    Reverse Transcriptase HIV Cancer
    Rovafovir etalafenamide (GS-9131), a prodrug of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity.
  • HY-B1696A
    Methyldopate hydrochloride

    Adrenergic Receptor Cardiovascular Disease
    Methyldopate hydrochloride is an ethyl ester hydrochloride prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research.
  • HY-109058
    Firibastat

    QGC001; RB150

    Aminopeptidase Cardiovascular Disease
    Firibastat (QGC001), an orally active brain penetrating prodrug of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.
  • HY-B0024
    Prulifloxacin

    NM441

    Bacterial Antibiotic Infection
    Prulifloxacin (NM441) is an orally active fluoroquinolone antibiotic with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is a prodrug of a thiazeto-quinoline carboxylic acid derivative Ulifloxacin (NM394). Prulifloxacin has the potential for lower urinary tract infections and exacerbations of chronic bronchitis.
  • HY-116217
    5-Fluoro-2'-deoxycytidine

    DNA Methyltransferase Cancer
    5-Fluoro-2'-deoxycytidine, a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective prodrug of the potent thymidylate synthase inhibitor 5-fluoro-2′-dUMP.
  • HY-75385A
    Zaurategrast ethyl ester sulfate

    CDP323 sulfate; UCB1184197 sulfate

    Integrin Inflammation/Immunology
    Zaurategrast ethyl ester sulfate (CDP323 sulfate), the ethyl ester prodrug of CT7758, is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders.
  • HY-100500
    Lenampicillin hydrochloride

    KBT 1585 hydrochloride

    Bacterial Cancer
    Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active prodrug of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection .
  • HY-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one

    DHED

    Estrogen Receptor/ERR Metabolic Disease
    10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.
  • HY-13629
    Etoposide

    VP-16; VP-16-213

    Topoisomerase Autophagy Mitophagy Bacterial Apoptosis Antibiotic Cancer Infection
    Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
  • HY-124573
    OBI-3424

    TH-3424

    DNA Alkylator/Crosslinker Cancer
    OBI-3424 (TH-3424) is a prodrug that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research.
  • HY-17425AS1
    Valacyclovir-d4 hydrochloride

    HSV Antibiotic Infection
    Valacyclovir-d4 hydrochloride is the deuterium labeled Valacyclovir hydrochloride. Valacyclovir hydrochloride (Valaciclovir hydrochloride) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir hydrochloride inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir hydrochloride is a prodrug of Aciclovir (HY-17422).
  • HY-10545
    Taribavirin

    HBV HCV Infection
    Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin, is a ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
  • HY-10545A
    Taribavirin hydrochloride

    HBV HCV Infection
    Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
  • HY-117433
    4-Hydroperoxy cyclophosphamide

    DNA Alkylator/Crosslinker Apoptosis Reactive Oxygen Species Drug Metabolite Inflammation/Immunology
    4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide has the potential for lymphomas and autoimmune disorders.
  • HY-122218
    JHU-083

    Glutaminase Neurological Disease
    JHU-083, a prodrug of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b + cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
  • HY-17474A
    Parecoxib Sodium

    SC 69124A

    COX Inflammation/Immunology Cancer
    Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
  • HY-B1562
    Bopindolol

    (±)-Bopindolol

    Adrenergic Receptor Cardiovascular Disease
    Bopindolol is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol is a prodrug of pindolol and can be used for essential and renovascular hypertension research.
  • HY-13038A
    Fostamatinib

    R788

    Syk FLT3 Inflammation/Immunology Cancer
    Fostamatinib (R788) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-17474
    Parecoxib

    SC 69124

    COX Cancer Inflammation/Immunology
    Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
  • HY-111274
    Indomethacin farnesil

    Indometacin farnesil

    COX Autophagy Inflammation/Immunology
    Indomethacin farnesil is an orally active prodrug of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
  • HY-117259
    ALZ-801

    Amyloid-β Neurological Disease
    ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.
  • HY-N6263
    EGCG Octaacetate

    Bacterial Infection Cardiovascular Disease
    EGCG Octaacetate is a prodrug of Green tea epigallocatechin-3-gallate (EGCG), utilized to enhance the stability and bioavailability of EGCG in vivo. EGCG Octaacetate has high efficacy, bioavailability, anti-oxidation and anti-angiogenesis capacities. EGCG octaacetate is the potential antibacterial compound for gram-positive bacteria (GPB) and gram-negative bacteria (GNB) .
  • HY-135853
    Molnupiravir

    EIDD-2801; MK-4482

    SARS-CoV Influenza Virus Infection
    Molnupiravir (EIDD-2801) is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza.
  • HY-136588
    trans-R-138727MP

    Prasugrel metabolite R-138727MP

    P2Y Receptor Cardiovascular Disease
    trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-13038B
    Fostamatinib disodium hexahydrate

    R788 disodium hexahydrate

    Syk FLT3 Cancer Inflammation/Immunology
    Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-10220
    SF1126

    PI3K Apoptosis Cancer
    SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis.
  • HY-13038
    Fostamatinib Disodium

    R788(Disodium)

    Syk FLT3 Inflammation/Immunology Cancer
    Fostamatinib Disodium (R788 Disodium) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-109016
    Valnivudine

    FV-100 free base

    Antibiotic Bacterial Infection
    Valnivudine (FV-100 free base), a prodrug of CF-1743, is an orally active anti-herpes zoster (HZ) nucleoside analogue. CF-1743, a bicyclic nucleoside analog (BCNA), has highly specific antiviral activity against varicella-zoster virus (VZV). Valnivudine is rapidly and extensively converted to CF-1743 in vivo.
  • HY-131904
    POMHEX

    Enolase Apoptosis Cancer Metabolic Disease
    POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor.
  • HY-103370
    Talniflumate

    BA 7602-06

    Chloride Channel Inflammation/Immunology
    Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase. Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.
  • HY-137958
    Bemnifosbuvir hemisulfate

    AT-527

    HCV SARS-CoV Infection
    Bemnifosbuvir hemisulfate (AT-527), a hemisulfate salt of AT-511, a guanosine nucleotide prodrug, is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir hemisulfate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC90=0.47 μM). Bemnifosbuvir hemisulfate has pangenotypic antiviral activity.
  • HY-119726
    Fosmanogepix

    APX001; E1211

    Fungal Infection
    Fosmanogepix (APX001) is a first-in-class and orally available broad-spectrum antifungal agent, which targets the highly conserved Gwt1 fungal enzyme. Fosmanogepix (APX001) is an N-phosphonooxymethyl prodrug which is rapidly and completely metabolized by systemic alkaline phosphatases to the active moiety, APX001A. Fosmanogepix (APX001) can be used in development for the treatment of invasive fungal infections.
  • HY-B0024S
    Prulifloxacin-d8

    Bacterial Antibiotic Infection
    Prulifloxacin-d8 (NM441-d8) is the deuterium labeled Prulifloxacin. Prulifloxacin (NM441) is an orally active fluoroquinolone antibiotic with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is a prodrug of a thiazeto-quinoline carboxylic acid derivative Ulifloxacin (NM394). Prulifloxacin has the potential for lower urinary tract infections and exacerbations of chronic bronchitis.
  • HY-13543
    Tretazicar

    CB 1954

    DNA Alkylator/Crosslinker Cancer
    Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).
  • HY-131296
    5-A-RU-PABC-Val-Cit-Fmoc

    Others Inflammation/Immunology
    5-A-RU-PABC-Val-Cit-Fmoc is the prodrug of 5-A-RU. 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
  • HY-100500S
    Lenampicillin-d5 hydrochloride

    Bacterial Cancer
    Lenampicillin-d5 (KBT 1585-d5) hydrochloride is the deuterium labeled Lenampicillin hydrochloride. Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active prodrug of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection.
  • HY-16146
    Combretastatin A-1 phosphate tetrasodium

    OXi-4503 tetrasodium

    Microtubule/Tubulin Cancer
    Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects.
  • HY-138078
    Lufotrelvir

    PF-07304814

    SARS-CoV Infection
    Lufotrelvir (PF-07304814), a phosphate prodrug of PF-00835231, acts as a potent 3CL pro protease (M pro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-2 3CL pro activity with a Ki of 174nM. Lufotrelvir is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle.
  • HY-117433S
    4-Hydroperoxy Cyclophosphamide-d4

    DNA Alkylator/Crosslinker Apoptosis Reactive Oxygen Species Drug Metabolite Inflammation/Immunology
    4-Hydroperoxy Cyclophosphamide-d4 is the deuterium labeled 4-Hydroperoxy cyclophosphamide. 4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide has the potential for lymphomas and autoimmune disorders.
  • HY-121629
    PS210

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
  • HY-13205
    Belnacasan

    VX-765

    Caspase Inflammation/Immunology
    Belnacasan (VX-765) is an orally bioactive prodrug of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM.
  • HY-14905
    Uridine triacetate

    Tri-O-acetyl uridine

    Others Neurological Disease
    Uridine triacetate (Tri-O-acetyl uridine) is an orally active prodrug of Uridine. Uridine triacetate (Tri-O-acetyl uridine) is quickly absorbed in the gut, and is rapidly deacetylated in the circulation to yield free uridine. Uridine triacetate (Tri-O-acetyl uridine) is uesd for the prevention and treatment of life-threatening 5-fluorouracil and capecitabine toxicity. Uridine triacetate (Tri-O-acetyl uridine) delivers high concentrations of uridine, which competes with toxic 5-FU metabolites.
  • HY-14572
    PR-104A

    SN 27858

    DNA Alkylator/Crosslinker Cancer
    PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL).
  • HY-10187
    TG 100801 Hydrochloride

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 Hydrochloride is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-10186
    TG 100801

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-15648F
    GSK-J4 hydrochloride

    Histone Demethylase Cancer
    GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.
  • HY-135125
    DC4

    ADC Cytotoxin Cancer
    DC4, an ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4 can be used for the targeted treatment of cancer.
  • HY-15648B
    GSK-J4

    Histone Demethylase Apoptosis Cancer
    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.