Search Result
Results for "
diacetate ester prodrug
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-163849
-
|
|
Others
|
Inflammation/Immunology
|
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Mizoribine prodrug-1 (compound 18) is a oral active ester-based mizoribine (HY-17470) prodrug. Mizoribine prodrug-1 displays a inhibition of IL-2 production .
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-
-
- HY-163850
-
|
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Interleukin Related
|
Inflammation/Immunology
|
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Mizoribine prodrug-2 trifluoroacetate (compound 20) is a oral active mizoribine (HY-17470) prodrug (amino acid conjugate). Mizoribine prodrug-2 displays a prolonged inhibition of IL-2 production .
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-
-
- HY-161336
-
|
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Bacterial
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Cancer
|
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Alendronate prodrug-1(compound 2) is an inhibitor of farnesyl diphosphate synthase (FPPS). Alendronate prodrug-1 has an antiproliferative effect with an IC50 value of 34.0 μM .
|
-
-
- HY-172148
-
|
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Interleukin Related
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Inflammation/Immunology
|
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Itaconic acid prodrug-1 (Compound P2) is an orally active prodrug of Itaconic acid (HY-Y0520) that efficiently delivers the active ingredient Itaconic acid to skin tissue following oral administration. Itaconic acid prodrug-1 possesses immunomodulatory properties, significantly inhibiting Poly(I:C)/IFNγ-induced inflammatory cytokines in human epidermal keratinocytes. Itaconic acid prodrug-1 can be utilized for the research of alopecia areata and other inflammatory skin diseases .
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-
-
- HY-168928
-
|
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Bacterial
|
Infection
|
|
Antibiofilm agent prodrug 1 (Compound 5c) exhibits antibacterial activity through inhibition of biofilm formation and iron uptake. Antibiofilm agent prodrug 1 inhibits P. aeruginosa PAO1 with a MIC of 1.07 μM. Antibiofilm agent prodrug 1 exhibits anti-infectious efficacy in C. elegans with improved survival rate .
|
-
-
- HY-168875
-
|
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TrxR
Reactive Oxygen Species
|
Cancer
|
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TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1. TrxR1 prodrug-1 exhibits significant antitumor efficiency in nude mice and NSCLC organoids .
|
-
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- HY-168472
-
|
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SARS-CoV
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Infection
|
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13-TP prodrug (compound 15) is a potent and orally active anti-SARS-CoV-2 agent. 13-TP prodrug shows cytotoxicity. 13-TP prodrug decreases the SARS-CoV-2 N protein expression. 13-TP prodrug shows antiviral activity .
|
-
-
- HY-163544
-
|
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Others
|
Cancer
|
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δ-Tocotrienol prodrug-1 (compound 5b) is a prodrug of δ-tocotrienol (HY-122778). δ-Tocotrienol prodrug-1 shows radioprotective efficacy. δ-Tocotrienol prodrug-1 promotes the hematopoietic progenitor and stem cell regeneration in murine bone marrow and spleen .
|
-
-
- HY-173023
-
|
|
Apoptosis
Indoleamine 2,3-Dioxygenase (IDO)
Reactive Oxygen Species
|
Cancer
|
|
IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug. IDOi-Pt(IV) prodrug-1 inhibits IDO expression. IDOi-Pt(IV) prodrug-1 induces apoptosis, decreases the mitochondrial membrane potential, inhibits tumor cell migration and invasion. IDOi-Pt(IV) prodrug-1 induces reactive oxygen species-mediated endoplasmic reticulum stress and secretion of damage-associated molecular patterns (DAMPs), thereby presenting immunogenic cell death (ICD) effects. IDOi-Pt(IV) prodrug-1 has high-efficiency and low-toxicity antitumor effects compared to Cisplatin (HY-17394) .
|
-
-
- HY-161687
-
|
|
Src
|
Cancer
|
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Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
|
-
-
- HY-169131
-
|
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AMPK
|
Cancer
|
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ALKBH1-IN-4 prodrug (Compound 29E) is a prodrug of a DNA N6-methyladenine demethylase ALKBH1 inhibitor that significantly increases the abundance of 6mA in cells and upregulates the AMPK signaling pathway, thereby inhibiting the viability of gastric cancer cells. ALKBH1-IN-4 prodrug exhibits excellent cellular activity and favorable metabolic exposure in vivo, and holds promise for research in gastric cancer .
|
-
-
- HY-159921
-
|
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Microtubule/Tubulin
|
Cancer
|
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Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a palladium (Pd)-mediated tubulin polymerization inhibitor prodrug. Developed based on colchicine binding site inhibitors (CBSIs), it reduces toxicity and enhances targeted release properties. Compared to the parent compound, Tubulin Polymerization-IN-1 prodrug exhibited 68.3-fold lower cytotoxicity, which can be restored in situ in the presence of Pd resin. Mechanistic studies showed that its anticancer activity is consistent with CBSIs. In vivo, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth (63.2%) when activated by Pd resin. It holds promise for research in the field of anticancer therapy .
|
-
-
- HY-147015
-
|
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Orthopoxvirus
|
Infection
|
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HOE961, the diacetate ester proagent of S2242, is active against respiratory cowpox virus infections, is orally active in infection models. Anti-orthopoxvirus activity .
|
-
-
- HY-149025
-
|
P18
|
Phospholipase
|
Inflammation/Immunology
Cancer
|
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DPTIP-proagent 18 (P18) is a orally active and brain-penetrable proagent of DPTIP (HY-131002). DPTIP-proagent 18 is a potent nSMase2 inhibitor. DPTIP-proagent 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-proagent 18 can be used for brain injury research .
|
-
-
- HY-139995
-
|
|
Drug Intermediate
|
Others
|
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Spermine precursor-1 (Compound 1) is a redox-sensitive spermine precursor for the potential research of snyder robinson syndrome. Spermine precursor-1 inhibits wild-type (CMS-24949) and spermine synthase gene (SMS) mutant (CMS-26559, and CMS-6233) fibroblast cells with IC50s of 326.7, 198.5, and 244.1 μM, respectively .
|
-
-
- HY-145829
-
|
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JAK
Apoptosis
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Inflammation/Immunology
|
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Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
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-
-
- HY-145323
-
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Biochemical Assay Reagents
|
Cancer
|
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Mitochondria-Targeted Photoactivatable Proagent accumulates in the mitochondria and shows light-triggered temporally controlled cell death. Mitochondria-Targeted Photoactivatable Proagent can be used in a novel drug delivery platform that provides on-demand, real-time, organelle-specific agent release and monitoring upon photoactivation .
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-
-
- HY-168639
-
|
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Mitochondrial Metabolism
AMPK
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Metabolic Disease
|
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AP39 prodrug 1 (Compound M1) is a mitochondria-targeted H2S prodrug. AP39 prodrug 1 induces ROS-dependent mild mitochondrial uncoupling, activating mitochondria-associated AMPK to suppress Palmitic acid (PA) (HY-N0830)-induced lipid deposition in hepatocytes .
|
-
-
- HY-Z4483
-
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Drug Intermediate
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Others
|
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6-Deoxypenciclovir is an inactive metabolite of the antiviral prodrug Famciclovir. 6-Deoxypenciclovir is a good substrate for rabbit hepatic aldehyde oxidase and can be used to synthesize the prodrug form of penciclovir .
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- HY-W342471
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-
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- HY-A0032
-
|
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CMV
|
Infection
Cancer
|
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Valganciclovir, the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir.
|
-
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- HY-B1149A
-
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Bacterial
Antibiotic
|
Infection
|
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Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
|
-
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- HY-127122
-
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HBV
|
Infection
|
|
Valtorcitabine dihydrochloride is a prodrug of L-deoxycytidine and also is an HBV inhibitor .
|
-
-
- HY-109755
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-
-
- HY-B1149
-
-
-
- HY-162410
-
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MDM-2/p53
|
Cancer
|
|
Fluplatin is a prodrug composed of cisplatin and fluvastatin. Fluplatin has antitumor activity .
|
-
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- HY-118983
-
|
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Antibiotic
Bacterial
|
Infection
|
|
Pivampicillin hydrochloride is a penicillin antibiotic. Pivampicillin hydrochloride is a prodrug of Ampicillin (HY-B0522) .
|
-
-
- HY-169855
-
|
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Drug Intermediate
|
Others
|
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Apaziquone hydroquinone is a bioreductive prodrug and a derivative of Mitomycin C (HY-13316) .
|
-
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- HY-137238
-
|
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Drug Metabolite
|
Metabolic Disease
|
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Ethyl mycophenolate is a potential impurity found in commercial preparations of the mycophenolic acid prodrug mycophenolate mofetil.
|
-
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- HY-119011
-
-
-
- HY-162448
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-
-
- HY-12758
-
|
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BCRP
|
Cancer
|
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YHO-13351 is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
|
-
-
- HY-155371
-
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PROTACs
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Others
|
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BT-PROTAC is a bioorthogonally activatable prodrug. BT-PROTAC can accurately control the activity of PROTAC .
|
-
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- HY-105929
-
-
-
- HY-19495
-
-
-
- HY-B1079
-
-
-
- HY-157127
-
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COX
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Metabolic Disease
|
Ketoprofen L-thyroxine ester is a prodrug of Ketoprofen. Ketoprofen L-thyroxine ester reservoir and release ketoprofen slowly in the brain .
|
-
-
- HY-153260
-
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CDK
|
Cancer
|
|
TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor .
|
-
-
- HY-12758A
-
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BCRP
|
Cancer
|
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YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
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-
-
- HY-B0382
-
-
-
- HY-126719
-
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Drug Derivative
|
Neurological Disease
|
|
R-1 Methanandamide Phosphate is a water-soluble prodrug analog of arachidonylethanolamide (AEA). AEA is an endogenous cannabinoid compound .
|
-
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- HY-17422C
-
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Aciclovir alaninate; Acycloguanosine alaninate
|
HSV
|
Infection
|
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Acyclovir alaninate (Acyclovir alaninate) is a prodrug of Acyclovir (HY-17422) and can be used in antiviral (HSV) research .
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-
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- HY-107026
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HBV
|
Infection
|
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Lagociclovir valactate is a prodrug of Lagociclovir (HY-14844). Lagociclovir valactate is an orally active anti-HBV agent .
|
-
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- HY-164927
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-
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- HY-137362
-
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Drug Intermediate
|
Infection
|
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N2-Acetyl acyclovir is an Acyclovir prodrug. Acyclovir (Aciclovir) is a potent, orally active antiviral agent .
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-
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- HY-W099488
-
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Drug Intermediate
|
Cancer
|
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Capecitabine 2',3'-diacetate (Compound 10b) is the prodrug for the antitumor agent Capecitabine (HY-B0016) .
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-
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- HY-114840
-
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Ras
|
Cancer
|
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L 731734 is a prodrug of L-731735 (HY-129273), and inhibits Ras processing in cells transformed with v-ras .
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-
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- HY-162911
-
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Phosphodiesterase (PDE)
|
Cancer
|
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Enpp-1-IN-22 is an orally bioavailable prodrug of the potent ENPP1 inhibitor paraformaldehyde with antitumor activity .
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-
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- HY-135077
-
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Drug Intermediate
|
Others
|
|
Prostaglandin A1 ethyl ester is a prodrug form of Prostaglandin A1. Prostaglandin A1 inhibits the activation of platelets .
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-
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- HY-165164
-
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Others
|
Cancer
|
|
Methotrexate-alpha-alanine is a prodrug for activation by enzyme-monoclonal antibody conjugates. Methotrexate-alpha-alanine shows cytotoxicity .
|
-
- HY-112068
-
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HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
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DM-NOFD is a cell penetrant, prodrug of NOFD a potent and selective inhibitor of an asparaginyl hydroxylase FIH (factor-inhibiting HIF) .
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- HY-124584
-
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Apoptosis
|
Cancer
|
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Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis .
|
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- HY-129464
-
-
- HY-162926
-
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Bacterial
|
Infection
|
|
Antituberculosis agent-12 (compound 3408) is a narrow-spectrum antituberculosis prodrug phosphate that has the ability to inhibit drug-resistant tuberculosis infection .
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-
- HY-120639
-
|
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HIV
|
Others
|
|
BMS-663749 lysine is a prodrug of an HIV-1 attachment inhibitor with the potential to enhance the delivery of the parent compound following oral administration.
|
-
- HY-107074
-
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R1518
|
HCV
|
Infection
|
|
Levovirin valinate hydrochloride (R1518) is a prodrug of Levovirin (HY-119415) with oral activity, exhibiting antiviral activity against hepatitis C virus .
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-
- HY-200444
-
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Liposome
|
Others
|
|
Lipid catechol is a lipid that forms lipid prodrug nanoassemblies (LPNA) with boronic acid-containing compounds. Lipid catechol is promising for research of drug delivery .
|
-
- HY-157779
-
|
|
Reactive Oxygen Species
|
Metabolic Disease
|
|
TPA-NAC is a nonfluorogenic prodrug by introducing N-acetyl-L-cysteine (NAC) into a conjugated acceptor skeleton. TPA-NAC is capable of fluorogenic selective labeling of HSA .
|
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- HY-119960
-
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COX
|
Inflammation/Immunology
|
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AHR-10037 is a non-steroidal anti-inflammatory agent with low gastric toxicity. AHR-10037 is a prodrug converted in vivo to a cyclooxygenase inhibitor .
|
-
- HY-154842
-
-
- HY-125939
-
|
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Proteasome
|
Cancer
|
|
Bortezomib-pinanediol is a proteasome inhibitor and a prodrug of Bortezomib (HY-10227). Bortezomib-pinanediol inhibits cell growth and can be used for study of multiple myeloma .
|
-
- HY-16511
-
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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-W856812
-
|
|
Drug Intermediate
|
Others
|
|
Penicillanic acid (sodium) is a key drug intermediate. Penicillanic acid (sodium) can be used to synthesize β-lactamase inhibitors and prodrugs. Penicillanic acid (sodium) derivative Mecillinam has antibacterial activity .
|
-
- HY-123754
-
|
|
Proton Pump
|
Inflammation/Immunology
|
|
AGN-201904 is a proton pump inhibitor. AGN-201904 is an omeprazole prodrug that can delay aging and can be used to prevent and treat peptic ulcers .
|
-
- HY-16123
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Canfosfamide (hydrochloride) is a prodrug that upon activation by glutathione s-transferase P1-1 (GSTP1-1) yields an anticancer alkylating agent and a glutathione derivative.
|
-
- HY-19690
-
|
KUC-7483 hydrochloride
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Ritobegron, a prodrug of the active compound, KUC-7322, is a selective β3 -adrenoceptor agonist. Ritobegron decreases intravesical pressure with minimal effects on the cardiovascular system.
|
-
- HY-120313
-
|
|
Drug Derivative
|
Cancer
|
|
SN23862 is a cancer prodrug with anti-cancer activity, and an analogue of CB-1954 (HY-13543). SN23862 can be used for cancer research .
|
-
- HY-108920
-
|
4-Cl-KYN; AV-101
|
iGluR
|
Neurological Disease
|
|
4-Chlorokynurenine is a prodrug of a NMDA receptor antagonist. 4-Chlorokynurenine has orally active and blood-brain permeability that can be used for the research of depression .
|
-
- HY-127125
-
|
|
COX
|
Inflammation/Immunology
|
|
Diclofenac ethyl ester is the prodrug of Diclofenac (HY-15036), that is encapsulated in polymer micelles in vitro, and released with prolonged circulation time and reduced drug concentrations in the heart and kidneys in vivo .
|
-
- HY-17501S
-
|
(±)-Bambuterol-d9 hydrochloride; KWD-2183-d9 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
|
Bambuterol-d9 (hydrochloride) is the deuterium labeled Bambuterol. Bambuterol ((±)-Bambuterol) hydrochloride is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
|
-
- HY-114635
-
|
Retorphan
|
Neprilysin
|
Metabolic Disease
|
|
Dexecadotril (Retorphan) is a powerful and selective neprilysin (NEP) inhibitor. Dexecadotril is a prodrug of the R-enantiomers of Thiorphan (HY-W013375). Dexecadotril shows intestinal antisecretatory action .
|
-
- HY-169993
-
|
|
HBV
|
Infection
|
|
ALG-000184, a prodrug of the potent Hhepatitis B virus (HBV) capsid assembly modulator ALG-001075, has the potential for the research of HBV infection research .
|
-
- HY-19167
-
|
AS 013; Lipo-pro-prostaglandin E1
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Ecraprost is a prodrug of prostaglandin E1. Ecraprost inhibits platelet adhesion, macrophage infiltration and proliferating cell nuclear antigen positive cell expression on the injured arterial walls .
|
-
- HY-160207
-
-
- HY-15406
-
-
- HY-129914
-
|
KY-109 free base
|
Bacterial
|
Infection
|
|
Cefcanel daloxate (KY-109 (free base)) is an orally active cephalosporin prodrug against Gram-positive bacteria and Haemophilus influenzae. Cefcanel daloxate is promising for research of uremia .
|
-
- HY-122278
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Melevodopa is an effervescent levodopa (HY-N0304) prodrug. Levodopa is an orally active metabolic precursor of neurotransmitters dopamine and has anti-allodynic effects and the potential for Parkinson's disease .
|
-
- HY-W011963
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Melevodopa hydrochloride is an effervescent Levodopa (HY-N0304) prodrug. Levodopa is an orally active metabolic precursor of neurotransmitters dopamine and has anti-allodynic effects and the potential for Parkinson's disease
|
-
- HY-108297
-
|
|
Others
|
Inflammation/Immunology
|
|
Piketoprofen is a non-steroidal anti-inflammatory reagent that can be used as a cream preparation for the study of soft tissue rheumatism. Piketoprofen-amide is a prodrug of COX-2 inhibitor .
|
-
- HY-169763
-
|
|
IRE1
Apoptosis
|
Cancer
|
|
D-F07 is a prodrug with an aldehyde shielding group and an IRE-1 inhibitor that induces Apoptosis. D-F07 has antitumor activity .
|
-
- HY-10213
-
|
PF-04929113
|
HSP
|
Cancer
|
|
SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
|
-
- HY-137453
-
|
HS-10234
|
HBV
|
Infection
|
|
Tenofovir amibufenamide (HS-10234), a Tenofovir prodrug, is an orally active antiviral agent. Tenofovir amibufenamide inhibits HBV, and can be used for chronic hepatitis B (CHB) study .
|
-
- HY-158329
-
-
- HY-B0021
-
|
Ro 21-9738; 5-Fluoro-5'-deoxyuridine; 5'-DFUR
|
Thymidylate Synthase
|
Cancer
|
|
Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs .
|
-
- HY-10213A
-
|
PF-04929113 mesylate
|
HSP
|
Cancer
|
|
SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
|
-
- HY-124584A
-
|
|
Apoptosis
|
Cancer
|
|
Minnelide free base is a prodrug of Triptolide (HY-32735) that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide free base promotes apoptosis .
|
-
- HY-135221A
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Cefcapene pivoxil, the pivalate ester prodrug form of Cefcapene, is an orally active third-generation cephalosporin with a wide spectrum of anti-bacterial activity. Cefcapene has the potential for the palmoplantar pustulosis (PPP) research .
|
-
- HY-105040C
-
|
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-B0382R
-
|
|
Angiotensin-converting Enzyme (ACE)
Apoptosis
|
Cardiovascular Disease
|
|
Fosinopril (sodium) (Standard) is the analytical standard of Fosinopril (sodium). This product is intended for research and analytical applications. 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-117630
-
|
|
Drug Intermediate
|
Cancer
|
|
RB-6145 is an orally active pro-drug of the hypoxic cell radiosensitizer RSU 1069. RB-6145 acts a hypoxic cell radiosensitizer and cytotoxin but reduces systemic toxicity in mice .
|
-
- HY-19288
-
|
ABT 606; MIV 606; A 174606.0
|
HSV
|
Infection
|
|
Valomaciclovir stearate (ABT 606), a nucleoside analog, is the Omaciclovir (HY-116174) prodrug. Valomaciclovir stearate has antiviral activity against HSV-1 and varicella zoster virus (VZV) .
|
-
- HY-157152
-
|
|
HDAC
|
Cancer
|
HDAC-IN-65 ( compound 6) is a selective histone deacetylase (HDAC) inhibitor with IC50 value of 2.5μM. HDAC-IN-65 is a prodrug with very good bioreductive properties .
|
-
- HY-108475
-
|
|
DYRK
|
Cancer
|
|
ProINDY, a prodrug of INDY (HY-108476), is a DYRK1A and DYRK1B inhibitor. ProINDY effectively recovers Xenopus embryos from head malformation induced by Dyrk1A overexpression .
|
-
- HY-117606
-
|
|
mGluR
|
Neurological Disease
|
|
LY3027788, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 has antidepressant efficacy .
|
-
- HY-117606A
-
|
|
mGluR
|
Neurological Disease
|
|
LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy .
|
-
- HY-135221
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cefcapene pivoxil hydrochloride, the pivalate ester prodrug form of Cefcapene, is an orally active third-generation cephalosporin with a wide spectrum of anti-bacterial activity. Cefcapene pivoxil hydrochloride has the potential for the palmoplantar pustulosis (PPP) research .
|
-
- HY-162039
-
|
|
MMP
|
Cancer
|
|
MMP-11-IN-1 (compound 9) is a new class of phosphinate prodrug. MMP-11-IN-1 is a glycosyl ester of RXP03 and improves blood–brain barrier (BBB) behavior .
|
-
- HY-14554
-
|
LY2140023
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research .
|
-
- HY-113929
-
|
R-58425
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Loperamide oxide (R-58425) is a orally active prodrug of the Loperamide (HY-156131). Loperamide oxide incubation with the contents of the intestinal lumen inhibits fluid secretion under aerobic conditions .
|
-
- HY-W040022
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cefcapene pivoxil hydrochloride hydrate, the pivalate ester prodrug form of Cefcapene, is an orally active third-generation cephalosporin with a wide spectrum of anti-bacterial activity. Cefcapene pivoxil hydrochloride hydrate has the potential for the palmoplantar pustulosis (PPP) research .
|
-
- HY-169832
-
|
|
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 .
|
-
- HY-132180A
-
|
|
ADC Cytotoxin
|
Inflammation/Immunology
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-14408
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
Lu AA47070 is a phosphonooxymethylene prodrug of a potent and selective Adenosine A2A receptor antagonist. Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade .
|
-
- HY-106155
-
|
DAPD
|
HIV
Reverse Transcriptase
|
Infection
|
|
Amdoxovir (DAPD) is an orally active nucleoside reverse transcriptase inhibitor. Amdoxovir is active against wild-type and NRTl-resistant viruses. Amdoxovir is the prodrug of dioxolane guanosine. Amdoxovir can be used for research of HIV/AIDS .
|
-
- HY-16309
-
|
|
Phosphatase
|
Metabolic Disease
|
|
MB07803 is an orally available prodrug of a potent, noncompetitive inhibitor (MB07729) of fructose 1,6-bisphosphatase (FBPase), with EC50 of 140 nM and t1/2 of 7.6±2.9 h.
|
-
- HY-133206A
-
|
Pronetupitant chloride monohydrochloride
|
Neurokinin Receptor
|
Cancer
|
|
Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant .
|
-
- HY-10127A
-
|
AZD1152 dihydrochloride
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Barasertib (AZD1152 dihydrochloride), 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 dihydrochloride) induces growth arrest and apoptosis in cancer cells .
|
-
- HY-162929
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
TP-DEA2, a predictable-release Triptolide (HY-32735) prodrug, block Bleomycin-induced pulmonary fibrosis and inflammation. TP-DEA2 significantly inhibits α-SMA production .
|
-
- HY-17549
-
|
CRL 40028
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Adrafinil (CRL-40028, Olmifon), prodrug of modafinil, is a mild central nervous system stimulant drug used to relieve excessive sleepiness and inattention, Adrafinil is believed to serve as an alpha-1 adrenoceptor agonist.
|
-
- HY-132987
-
|
ARX-1796; AV-006
|
Beta-lactamase
Bacterial
Drug Intermediate
|
Infection
|
|
Avibactam tomilopil (ARX-1796, AV-006) is an orally active prodrug of Avibactam and a β-lactamase inhibitor. Avibactam tomilopil can be used in the study of diseases such as urinary tract infections .
|
-
- HY-10127
-
Barasertib
Maximum Cited Publications
18 Publications Verification
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-19916A
-
|
BAL-101553 dihydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin dihydrochloride exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1 .
|
-
- HY-137453C
-
|
(R,1R)-HS-10234
|
Drug Intermediate
|
Others
|
|
(R,1R)-Tenofovir amibufenamide ((R,1R)-HS-10234) can be used for the purifying a tenofovir prodrug. Tynofovir (tenofovir) is a nucleoside acids reverse transcriptase inhibitors .
|
-
- HY-19916
-
|
BAL-101553
|
Microtubule/Tubulin
|
Cancer
|
|
Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1 .
|
-
- HY-19748
-
|
|
Bacterial
|
Infection
|
|
LED209 is a potent and orally active small molecule inhibitor of the bacterial receptor QseC and a potent prodrug with high selectivity for QseC. LED209 inhibits the binding of signaling molecules to QseC. LED209 has antibacterial activity .
|
-
- HY-144876
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
RIDR-PI-103 is a reactive oxygen species (ROS)-induced drug release prodrug with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103).
|
-
- HY-111288
-
-
- HY-15440A
-
|
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-128920
-
|
|
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-159924
-
|
|
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 .
|
-
- HY-139355
-
|
|
SARS-CoV
|
Infection
|
|
(S)-GS-621763 is the S-enantiomer of GS-621763 (HY-145119). GS-621763 is an orally active prodrug form of GS-443902 (HY-126303) that inhibits SARS-CoV-2 .
|
-
- HY-168143
-
|
|
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. .
|
-
- HY-124060
-
|
|
PDK-1
|
Cancer
|
|
PS423 is a prodrug of PS210, acting as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K. PS210 is a potent and selective PDK1 activator targeting the PIF binding pocket of PDK1 .
|
-
- HY-161089
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-45 (compound 9) is a prodrug. Antiproliferative agent-45 exhibits significant anti-proliferative effects for human pancreatic cells in hypoxia but fewer effects in normoxia. Antiproliferative agent-45 can be used for cancer research .
|
-
- HY-157222
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
Antitumor agent-125 (compound 17A) is a novel platinum(IV) prodrug. Antitumor agent-125 can activate the mitochondrion-dependent apoptosis pathway. Antitumor agent-125 induces ferroptosis in HCT-116/OXA .
|
-
- HY-15284S
-
|
PCR 4099-d5
|
Isotope-Labeled Compounds
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel-d5 is deuterium labeled Prasugrel. 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[1].
|
-
- HY-W048545
-
|
β-D-Glucopyranuronic acid, methyl ester, 2,3,4-triacetate
|
Drug Intermediate
|
Infection
|
|
2,3,4-Tri-O-acetyl-β-D-glucuronide methyl ester (β-D-Glucopyranuronic acid, methyl ester, 2,3,4-triacetate) is a synthetic intermediate in the synthesis of prodrug forms of the antitumor antibiotic Daunomycin (HY-13062A).
|
-
- HY-A0267
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Bitolterol is a β2-adrenergic agonist with bronchodilator activity. Bitolterol is classified as a prodrug and is primarily used for the suppression of respiratory diseases. Bitolterol is considered safe for use during breastfeeding, as the amount that can enter breast milk is very limited .
|
-
- HY-105040
-
|
LY2140023 hydrate
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia .
|
-
- HY-114206
-
|
|
Histone Methyltransferase
|
Cancer
|
|
SKI-73 is a chemical probe for CARM1 with prodrug properties. SKI-73 can rapidly penetrate cell membranes and be processed into active inhibitors. SKI-73 inhibits the invasion of breast cancer cells and can be used in the study of cancer .
|
-
- HY-14818C
-
|
CS-8958 hydrate
|
Influenza Virus
|
Infection
|
|
Laninamivir octanoate hydrate (CS-8958 hydrate), a prodrug of Laninamivir, is a long-acting neuraminidase (NA) inhibitor with anti-influenza virus activity. Laninamivir octanoate hydrate shows anti-influenza activity against Oseltamivir-resistant viruses, and also against the pandemic influenza viruses .
|
-
- HY-14922
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
Fosalvudine tidoxil is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Fosalvudine tidoxil is a prodrug derived from Alovudine (HY-B1516). Fosalvudine tidoxil is less toxic than Alovudine and can be used for the research of HIV-1 infection .
|
-
- HY-125309
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Others
|
|
ABT-299 is a prodrug of a platelet-activating factor (PAF) antagonist that exhibits significant inhibitory activity on PAF-induced β-platelet globulin release in vitro after in vivo administration in humans, an effect that may be partially attributed to the pyridine-N-oxide metabolite.
|
-
- HY-B0667
-
|
|
Interleukin Related
STAT
|
Inflammation/Immunology
Cancer
|
|
Balsalazide is a prodrug of amino salicylic acid that releases mesalamine (HY-15027) in the colon, offering various anti-inflammatory effects in areas of colitis, and it also exerts related anticancer effects by regulating the IL-6/STAT3 pathway .
|
-
- HY-B0667A
-
|
Balsalazide disodium dihydrate
|
Interleukin Related
STAT
|
Inflammation/Immunology
Cancer
|
|
Balsalazide sodium hydrate is a prodrug of amino salicylic acid that releases mesalamine (HY-15027) in the colon, offering various anti-inflammatory effects in areas of colitis, and it also exerts related anticancer effects by regulating the IL-6/STAT3 pathway .
|
-
- HY-100085
-
|
21-desDFZ
|
Drug Metabolite
|
Inflammation/Immunology
|
|
21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
|
-
- HY-B0021R
-
|
Ro 21-9738 (Standard); 5-Fluoro-5'-deoxyuridine (Standard); 5'-DFUR (Standard)
|
Thymidylate Synthase
|
Cancer
|
|
Doxifluridine (Standard) is the analytical standard of Doxifluridine. This product is intended for research and analytical applications. Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs .
|
-
- HY-108244
-
|
|
Interleukin Related
STAT
|
Inflammation/Immunology
Cancer
|
|
Balsalazide disodium is a prodrug of amino salicylic acid that releases mesalamine (HY-15027) in the colon, offering various anti-inflammatory effects in areas of colitis, and it also exerts related anticancer effects by regulating the IL-6/STAT3 pathway .
|
-
- HY-W811579
-
|
|
Bacterial
|
Infection
|
|
Bensuldazic acid (compound 4f) is a lipophilic 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivative that can be used as a prodrug model. Bensuldazic acid has antifungal activity .
|
-
- HY-114623
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
Prostaglandin D2 methyl ester is a prodrug form of Prostaglandin D2. Prostaglandin D2 methyl ester binds to the human and mouse PGD2 receptors (DP and CRTH2) with Ki values of 160 nM, 175 nM, 460 nM, and 270 nM for mCRTH2, mDP, hCRTH2, and hDP, respectively .
|
-
- HY-W811579A
-
|
|
Bacterial
|
Infection
|
|
Bensuldazic acid sodium (compound 4f) is a lipophilic 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivative that can be used as a prodrug model. Bensuldazic acid has antifungal activity .
|
-
- HY-B0021S1
-
|
Ro 21-9738-d3; 5-Fluoro-5'-deoxyuridine-d3; 5'-DFUR-d3
|
Thymidylate Synthase
Isotope-Labeled Compounds
|
Cancer
|
|
Doxifluridine-d3 is deuterated labeled Doxifluridine (HY-B0021). Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs .
|
-
- HY-78726A
-
|
Amprenavir phosphate sodium; GW 433908 sodium
|
HIV
Endogenous Metabolite
|
Infection
|
|
Fosamprenavir sodium (Amprenavir phosphate sodium) is an anti-HIV drug with antiviral activity. Fosamprenavir sodium is a water-soluble prodrug of amprenavir. Fosamprenavir sodium can help achieve and maintain viral suppression during antiretroviral suppression, thereby reducing the risk of HIV transmission through breast milk. Fosamprenavir sodium is not recommended for use during breastfeeding .
|
-
- HY-137362R
-
|
|
Drug Intermediate
|
Infection
|
|
N2-Acetyl acyclovir (Standard) is the analytical standard of N2-Acetyl acyclovir. This product is intended for research and analytical applications. N2-Acetyl acyclovir is an Acyclovir prodrug. Acyclovir (Aciclovir) is a potent, orally active antiviral agent .
|
-
- HY-157220
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Tolvaptan phosphate ester sodium, a prodrug of Tolvaptan (HY-17000), can be used in the study of cardiac edema. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation .
|
-
- HY-P10909
-
|
MBX 2109
|
Thyroid Hormone Receptor
|
Endocrinology
|
|
Canvuparatide (MBX 2109) is a prodrug for parathyroid hormone (PTH) peptide that releases the bioactive PTH[1-32] peptide agonist that retains a fatty acylated lysine (Lys33) at the C-terminus, thereby extending the halflife of Canvuparatide. Canvuparatide can be used for the symptoms of hypoparathyroidism such as hypocalcemia and hyperphosphatemia .
|
-
- HY-W778423
-
|
Dihydroxy Oxaliplatin-Pt(IV)
|
Drug Intermediate
|
Cancer
|
|
[Pt(DACH)(OH)2(ox)] is a Oxaliplatin (HY-17371)-based Pt(IV) scaffold. [Pt(DACH)(OH)2(ox)] reacts with N-hydroxysuccinimide (NHS) ester of PPA to yield phorbiplatin. Phorbiplatin is a highly potent Pt(IV) antitumor prodrug .
|
-
![[Pt(DACH)(OH)2(ox)]](//file.medchemexpress.eu/product_pic/hy-w778423.gif)
- HY-118520
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
16-Phenoxy tetranor Prostaglandin F2α methyl ester is a metabolically stable form of Prostaglandin F2α that can binds to FP receptor. 16-Phenoxy tetranor Prostaglandin F2α methyl ester serves as prodrug that can be hydrolyzed to generate bioactive free acid .
|
-
- HY-P10782
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
|
Pt(IV)-M13 is a BBB-penatrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma .
|
-
- HY-137807
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Thymidine 5′-monophosphate p-nitrophenyl ester sodium (Compound 2a) is the derivative of thymidine 5'-phosphate (TMP). Thymidine 5′-monophosphate p-nitrophenyl ester sodium penetrates mammalian cells, releases intracellular antimetabolite 5' nucleotides. Thymidine 5′-monophosphate p-nitrophenyl ester sodium is potential as an antitumor prodrug .
|
-
- HY-113929R
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Loperamide oxide (Standard) is the analytical standard of Loperamide oxide. This product is intended for research and analytical applications. Loperamide oxide (R-58425) is a orally active prodrug of the Loperamide (HY-156131). Loperamide oxide incubation with the contents of the intestinal lumen inhibits fluid secretion under aerobic conditions .
|
-
- HY-W040022R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cefcapene pivoxil (hydrochloride hydrate) (Standard) is the analytical standard of Cefcapene pivoxil (hydrochloride hydrate). This product is intended for research and analytical applications. Cefcapene pivoxil hydrochloride hydrate, the pivalate ester prodrug form of Cefcapene, is an orally active third-generation cephalosporin with a wide spectrum of anti-bacterial activity. Cefcapene pivoxil hydrochloride hydrate has the potential for the palmoplantar pustulosis (PPP) research .
|
-
- HY-157529
-
|
|
Microtubule/Tubulin
Fluorescent Dye
|
Cancer
|
|
IR820-PTX, an IR-820 (HY-136886)-Paclitaxel (HY-B0015) conjugate, is an amphipathic small molecule prodrug. IR820-PTX effectively inhibits tumor growth via combined photothermal therapy (PTT) and chemotherapy .
|
-
- HY-15440AR
-
|
|
HIV
|
Infection
|
|
Fostemsavir (Standard) is the analytical standard of Fostemsavir. This product is intended for research and analytical applications. 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-161062
-
|
|
EAAT
|
Neurological Disease
|
|
TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death .
|
-
- HY-168913
-
|
|
PSMA
|
Cancer
|
|
CTT2274 is a prodrug of MMAE (HY-15162). CTT2274 is composed of a prostate-specific membrane antigen (PSMA)-binding scaffold, a biphenyl motif, a pH-sensitive phosphoramidate linker, and MMAE payload. CTT2274 shows selective binding to PSMA and delivers MMAE. CTT2274 inhibits prostate cancer .
|
-
- HY-P10765
-
|
|
Peptide-Drug Conjugates (PDCs)
Topoisomerase
|
Cancer
|
|
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
|
-
- HY-168903
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-41 (Compound 16) is a prodrug of compound 1. STAT3-IN-41 slowly releases compound 1 inhibiting STAT3 signaling pathway. STAT3-IN-41 shows antitumor activity against lung cancer, hepatocellular carcinoma and pancreatic cancer .
|
-
- HY-171030
-
|
|
Ferroptosis
|
Cancer
|
|
Pro-GA is a γ-Glutamylcyclotransferase (GGCT) inhibitor and a cell-permeable diester-type pro-drug with anticancer activity, GGCT is a key enzyme in glutathione metabolism and is involved in the ferroptosis pathway. Pro-GA exhibits an IC50 of 57 μM against the bladder cancer cell line T24 and can be utilized in cancer research .
|
-
- HY-U00085
-
|
RU 47213
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Itameline (RU 47213) is a prodrug with oral and long-lasting cholinergic activity. Itameline is a novel tetrahydropyridine-oxime that is cleaved in vivo to form an active metabolite, RU 35963. RU 35963 is a muscarinic receptor agonist that is nonselective with respect to receptor subtypes. Itameline possesses the capacity to reduce memory deficits induced by an impairment of cholinergic transmission in the rat .
|
-
- HY-136506
-
|
|
Drug Derivative
|
Cancer
|
|
NUC-7738, an aryloxy phosphoramidate of 3′-Deoxyadenosine, is a 5′-aryloxy phosphoramidate prodrug of 3′-Deoxyadenosine (3′-dA). NUC-7738 has potent cytotoxic activity against a panel of hematological cancer cell lines. NUC-7738 can be used in research of cancer .
|
-
- HY-P10667
-
|
|
Integrin
|
Cancer
|
|
Ac-MRGDH-NH2 is a pentapeptide containing the RGD sequence. Ac-MRGDH-NH2 can be used to synthesize the diastereoisomeric prodrugs Λ- and Δ-[Ru(Ph2phen)2(κS,κN-(Ac-MRGDH-NH2))]Cl2. In these prodrugs, Ac-MRGDH-NH2 serves as a photolabile protecting group for the cytotoxic bis-aqua ruthenium warhead [Ru(Ph2phen)2(OH2)2]2+, and Ac-MRGDH-NH2 possesses integrin targeting ability and photosubstitution properties. Therefore, Ac-MRGDH-NH2 can be utilized in research on tumor-targeted photodynamic activation chemotherapy (PACT) .
|
-
- HY-W209628
-
|
Methyl acetylsalicylate
|
Drug Intermediate
|
Inflammation/Immunology
|
|
Methyl 2-acetoxybenzoate (Methyl acetylsalicylate) is a safe and simple anti-inflammatory aspirin prodrug. Methyl 2-acetoxybenzoate (Methyl acetylsalicylate) can be chemical or enzymatically hydrolysed to methyl 2-hydroxy benzoate. Methyl 2-acetoxybenzoate (Methyl acetylsalicylate) can be used as analgesic agent in liniments and also inflammatory diseases research .
|
-
- HY-163483
-
|
|
Parasite
|
Others
|
|
ELQ-598, as a prodrug, is converted into the active drug ELQ-596 upon oral administration. ELQ-598 demonstrates potent parasitic growth inhibition capabilities (IC50= 37 nM). ELQ-598 also shows low toxicity towards human cells (IC50= 19 μM). ELQ-598 can be used for research into babesiosis .
|
-
- HY-118956
-
|
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 .
|
-
- HY-137492
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
16,16-Dimethyl-PGE2-4-(4-acetamidobenzamido)phenyl ester is a derivative of 16,16-Dimethyl-PGE2 (HY-106420). 16,16-Dimethyl-PGE2-4-(4-acetamidobenzamido)phenyl ester is a prodrug for 16,16-Dimethyl-PGE2 .
|
-
- HY-119151
-
|
|
Apoptosis
HPV
DNA/RNA Synthesis
|
Infection
|
|
GS-9191 is the prodrug of the nucleotide analog PMEG. GS-9191 is a topical agent to permeate skin and be metabolized to the active nucleoside triphosphate analog in the epithelial layer. GS-9191 inhibits NA synthesis, arrests cell in S phase, and induces cell apoptosis. GS-9191 can be used for research of human papillomaviruses (HPV) infection .
|
-
- HY-134521
-
|
|
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) .
|
-
- HY-149065
-
|
|
α-synuclein
|
Neurological Disease
|
|
D-685, a prodrug of D-520, exhibits higher in vivo anti-Parkinsonian efficacy in a reserpinized Parkinson's disease (PD) animal model than the parent D-520. D-685 reduces accumulation of human α-synuclein (α-syn) protein. D-685 exhibits facile brain penetration .
|
-
- HY-161821
-
|
|
Interleukin Related
TNF Receptor
MMP
|
Cancer
|
|
Antitumor agent-173 (Compound 4b) is a prodrug of Cycloicaritin (HY-N1940). Antitumor agent-173 is a substrate for OATP2B1. Antitumor agent-173 selectively inhibits the growth of tumor Antitumor agent-173 significantly increases the oral bioavailability of Cycloicaritin and exerts good antitumor activity and safety .
|
-
- HY-124200
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AL 8810 (Item No. 16735) is an 11β-fluoro analog of prostaglandin F2α which acts as a potent and selective antagonist at the FP receptor. AL 8810 isopropyl ester is a lipid soluble, esterified prodrug form of AL 8810 analogous to the commonly used therapeutic intraocular prostaglandin compounds such as Latanoprost (HY-B0577) and Travoprost (HY-B0584).
|
-
- HY-107345
-
|
Ombolan
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Droxicam (Ombolan) is a non-steroidal anti-inflammatory agent, with strong analgesic activity. Droxicam acts by inhibiting PGE2 varies, and is characterised by being a pro-drug of Piroxicam (HY-B0253). Droxicam is well tolerated with slight side effects in the said mucosa. Droxicam does not show cardiovascular or respiratory effects in cats, and inhibits peritoneal capillary permeability in mouse .
|
-
- HY-P10759
-
|
|
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 .
|
-
- HY-P10760
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
PhAc-ALGP-Dox, a peptide-drug conjugate, is a novel anticancer prodrug, with IC50 values ranged from 311 nM to 34.25 μM for TNBC (E0771), normal murine epithelium (HC-11), human TNBC (MDA-MB-231 and MDA-MB-468), human CrC (LS 174T), normal human epithelium (HME-1) cells .
|
-
- HY-16124
-
|
TLK-286; TER286
|
DNA-PK
Apoptosis
|
Cancer
|
|
Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies .
|
-
- HY-P99101
-
|
AEX-4089
|
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 .
|
-
- HY-149257
-
|
|
JAK
STAT
|
Cancer
|
|
HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor with antitumor effects. HAT-SIL-TG-1&AT is the hypoxia-activated prodrug, witch inhibits JAK-STAT signaling in tumor tissue. And HAT-SIL-TG-1&AT inhibits HEL cells proliferation and downregulated phosphorylated STAT3/5 under hypoxic conditions .
|
-
- HY-170956
-
|
|
Drug Intermediate
|
Inflammation/Immunology
|
|
BTN3A1 ligand-1 (Compound 26b) is a triazole-containing aryl/acyloxyalkyl phosphonate prodrug. BTN3A1 ligand-1 can stimulate T cell proliferation (EC50: 0.49 nM) and interferon γ secretion. BTN3A1 ligand-1 has certain plasma stability and can be used in related immunotherapy research .
|
-
- HY-100085R
-
|
|
Drug Metabolite
|
Inflammation/Immunology
|
|
21-Desacetyldeflazacort (Standard) is the analytical standard of 21-Desacetyldeflazacort. This product is intended for research and analytical applications. 21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
|
-
- HY-168927
-
|
|
Apoptosis
Pyroptosis
|
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 .
|
-
- HY-162470
-
|
|
Aurora Kinase
|
Cancer
|
|
DBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465 .
|
-
- HY-169951
-
|
|
iGluR
|
Neurological Disease
|
|
Lu AF90103 (Compound 42e) is a methyl ester prodrug of compound 42d capable of penetrating the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1/GluN2B complex, exhibiting 24% efficacy, and has an EC50 value of 78 nM. Lu AF90103 plays an important role in neuropsychiatric diseases research .
|
-
- HY-123330
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
GW695634 is an orally active prodrug of GW678248. GW695634 undergoes amidolysis in vivo to release the active ingredient GW678248, thereby inhibiting viral replication. GW678248 is a non-nucleoside reverse transcriptase inhibitor (NNRTi) with potent antiviral activity against Efavirenz (HY-10572)-resistant and Nevirapine (HY-10570)-resistant HIV and AIDS viruses .
|
-
- HY-135853S
-
|
EIDD-2801-d7; MK-4482-d7
|
SARS-CoV
Influenza Virus
|
Inflammation/Immunology
|
|
Molnupiravir-d7 is the deuterium labeled Molnupiravir. 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[1][2].
|
-
- HY-167840
-
|
|
PD-1/PD-L1
|
Neurological Disease
Cancer
|
|
IMMH-010 maleate is a prodrug that serves as a novel PD-L1 inhibitor, exhibiting potential antitumor activity for the treatment of neurological disorders and advanced malignant solid tumors. IMMH-010 maleate is rapidly converted to its active form, YPD-29B, following oral administration. IMMH-010 maleate is poised for advancing research in the field of PD-L1 inhibitors and related therapeutic applications.
|
-
- HY-169434
-
|
Lon-TK-BMS-1
|
PD-1/PD-L1
|
Cancer
|
|
LTB is a prodrug formed by coupling glycolysis inhibitor (Lonidamine (HY-B0486)) with PD1/PDL1 blocker (BMS-1 (HY-19991)) by thioketal linkage. LTB can further encapsulate photosensitizer chlorine e6 (Ce6) (HY-13594) to construct a co-delivery photodynamic nanoplatform (LTB-6 NPs) by self-assembly .
|
-
- HY-134345
-
|
8-(4-Chlorophenylthio)-cGMP-AM
|
PKG
|
Neurological Disease
|
|
8-pCPT-cGMP-AM (8-(4-Chlorophenylthio)-cGMP-AM) is a highly membrane permeable prodrug of the PKG agonist 8-pCPT-cGMP, which increases the membrane permeability of cGMP and is converted to its active form by esterase hydrolysis within the cell, thereby activating PKG. 8-pCPT-cGMP-AM can be used to explore the role of cGMP signaling in neural plasticity and memory formation .
|
-
- HY-159515
-
|
|
Apoptosis
DNA/RNA Synthesis
Reactive Oxygen Species
|
Cancer
|
|
PBE-AMF is a prodrug that activates H2O2 with anticancer activity. PBE-AMF impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing apoptosis, and arresting the cell cycle. PBE-AMF potently and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells .
|
-
- HY-121629
-
|
|
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-162074
-
|
|
HIV
|
Infection
|
|
Nipamovir is a nitroimidazole prodrug. Nipamovir shows comparable antiviral activity to SAMT-247 (HY-102077) and NS-1040 in both cellular assays and a human ex vivo model of HIV infection, along with low toxicity. Nipamovir has EC50 values of 3.64±3.28 and 3.23±2.81 μM for CEM-SS/HIV-1RF and hPBMC/HIV-192HT599, respectively .
|
-
- HY-134123
-
|
LXB4 methyl ester
|
Drug Intermediate
Leukotriene Receptor
|
Metabolic Disease
|
|
Lipoxin B4 (LXB4) methyl ester is a lipid soluble prodrug form of the transcellular metabolite LXB4. LXB4 is a positional isomer of LXA4 produced by the metabolism of 15-HETE or 15-HpETE by human leukocytes. At a concentration of 100 nM, LXB4 inhibits polymorphonuclear leukocyte (PMN) migration stimulated by leukotriene B4 (LTB4; Item No. 20110) and inhibits LTB4-induced adhesion of PMNs with an IC50 value of 0.3 nM.
|
-
- HY-A0114
-
|
RS 10029
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Moexiprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC50=2.1 nM) and an active metabolite of the prodrug Moexipril (HY-117281). It is formed from moexipril in vivo by side chain ester hydrolysis. Moexiprilat (10 nM) prevents the estrone- or angiotensin II-stimulated proliferation of primary neonatal rat cardiac fibroblasts. It reduces mean arterial blood pressure and increases the levels of atrial natriuretic peptide, a marker of hypertension, in ovariectomized mice when administered at a dose of 50 mg/kg per day.
|
-
- HY-168635
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SJ46420, a SJ46421 (HY-168634) pro-drug variant, is a potent and selective BRD3 PROTAC degrader. SJ46420 degrads BRD3 in a KLHDC2-dependent manner, thereby partially reducing the levels of BRD2 or BRD4 (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-159973)) .
|
-
- HY-169986S
-
|
|
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 .
|
-
- HY-158331
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
Gal-ARV-771, PROTAC prodrug, is a gal modified ARV-771 (HY-100972). Gal-ARV-771 can be activated in SA-β-Gal-expressed cancer senescent cells to release ARV-771. Gal-ARV-771 induces selective degradation of BRD4 protein by the ubiquitin-proteasome pathway in senescent cells. Gal-ARV-771 promotes apoptosis of senescent cancer cells .
|
-
- HY-161838
-
|
|
ATM/ATR
|
Cancer
|
|
ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
|
-
- HY-14532
-
|
CMX001; HDP-CDV
|
CMV
HSV
Orthopoxvirus
|
Infection
|
|
Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections. Brincidofovir, an oral antiviral in late stage development, has proven effective against orthopoxviruses in vitro and in vivo. .
|
-
- HY-169436
-
|
|
PD-1/PD-L1
|
|
|
Lon-TK is a glycolysis inhibitor + linker conjugate of LTB (HY-169434). LTB is an intelligent responsive prodrug that connects Lonidamine (Lon) (HY-B0486) and a PD-L1 inhibitor (BMS-1, HY-19991) through a thioketal linker. It significantly inhibits the glycolytic metabolism of tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK shows potential for application in photodynamic-enhanced immunotherapy research .
|
-
- HY-131605
-
|
GCV-TP
|
Endogenous Metabolite
|
Cancer
|
|
Ganciclovir triphosphate (GCV-TP) is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate has an IC50 of 0.01 μM and has good antiviral effects against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
|
-
- HY-116161A
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
17-phenyl trinor PGF2α N-ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost.1 The N-ethyl amide prostaglandin prodrugs are converted to the active free acid more slowly than the analogous prostaglandin ester prodrugs such as latanoprost.2 This product is the isopropyl ester of the free acid prostaglandin which corresponds to Bimatoprost. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist.3 In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity. The 17-phenyl trinor PGF2α isopropyl ester derivative is examined for IOP-lowering activity during the development of latanoprost.4 At the dose of 3 μg/eye in the monkey, 17-phenyl trinor PGF2α isopropyl ester is the most potent analog tested in reducing IOP, lowering the IOP 1.3 mm Hg below the level achieved by latanoprost. However, this derivative is also significantly more irritating to the eye than latanoprost.
|
-
- HY-P10783
-
|
|
Peptide-Drug Conjugates (PDCs)
Integrin
|
Cancer
|
|
BGC0222 is a novel prodrug of Irinotecan (HY-16562). BGC0222, as a PEG-cRGD-conjugated Irinotecan (HY-16562) derivative, could slowly and steadily release Irinotecan (HY-16562). BGC0222 binds to αVβ3 with IC50 values of 4.25 μM (αVβ3) and 58.7 μM (αVβ5). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors .
|
-
- HY-159925
-
|
|
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 .
|
-
- HY-168497
-
|
|
Histone Methyltransferase
|
Cancer
|
|
C-MS023 is a photo-activatable MS023 (HY-19615) prodrug, achieving spatiotemporal inhibition of Histone Arginine Asymmetric Dimethylation. C-MS023 inhibits PRMT6 mediated asymmetric dimethylation of H3 arginine 2 (H3R2me2a), with an estimate IC50 of 0.2224 μM. The photolysis of C-MS023 could be triggered by visible light irradiation at 420 nm, thereby liberating MS023 for effective downregulation of histone arginine asymmetric dimethylation and DNA replication-related transcriptomic activities .
|
-
- HY-134160
-
|
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.
|
-
- HY-139124
-
|
15(R)-Carboprost; 15(R)-15-methyl PGF2α
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
15(R)-15-Methyl Prostaglandin F2α (15(R)-Carboprost; 15(R)-15-methyl PGF2α) is a metabolically stable analog of PGF2α. 15(R)-15-Methyl Prostaglandin F2α is an inactive, prodrug PGF agonist designed for activation by gastric acid after oral administration. Acid-catalyzed epimerization of 15(R)-15-Methyl Prostaglandin F2α converts it into the active 15(S)-isomer. The 15(S)-isomer induces luteolysis when injected in rhesus monkeys at a dose of about 12 mg/animal, while the 15(R)-isomer does not.
|
-
- HY-129934
-
|
Lat-NEt
|
Prostaglandin Receptor
|
Endocrinology
|
|
Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides.
|
-
- HY-15334
-
|
|
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 .
|
-
- HY-129934S
-
|
Lat-NEt-d4
|
Isotope-Labeled Compounds
Prostaglandin Receptor
|
Endocrinology
|
|
Latanoprost ethyl amide-d4 (Lat-NEt-d4) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10909
-
|
MBX 2109
|
Thyroid Hormone Receptor
|
Endocrinology
|
|
Canvuparatide (MBX 2109) is a prodrug for parathyroid hormone (PTH) peptide that releases the bioactive PTH[1-32] peptide agonist that retains a fatty acylated lysine (Lys33) at the C-terminus, thereby extending the halflife of Canvuparatide. Canvuparatide can be used for the symptoms of hypoparathyroidism such as hypocalcemia and hyperphosphatemia .
|
-
- HY-P10782
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
|
Pt(IV)-M13 is a BBB-penatrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma .
|
-
- HY-P10765
-
|
|
Peptide-Drug Conjugates (PDCs)
Topoisomerase
|
Cancer
|
|
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
|
-
- HY-P10667
-
|
|
Integrin
|
Cancer
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Ac-MRGDH-NH2 is a pentapeptide containing the RGD sequence. Ac-MRGDH-NH2 can be used to synthesize the diastereoisomeric prodrugs Λ- and Δ-[Ru(Ph2phen)2(κS,κN-(Ac-MRGDH-NH2))]Cl2. In these prodrugs, Ac-MRGDH-NH2 serves as a photolabile protecting group for the cytotoxic bis-aqua ruthenium warhead [Ru(Ph2phen)2(OH2)2]2+, and Ac-MRGDH-NH2 possesses integrin targeting ability and photosubstitution properties. Therefore, Ac-MRGDH-NH2 can be utilized in research on tumor-targeted photodynamic activation chemotherapy (PACT) .
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- HY-P10759
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Peptide-Drug Conjugates (PDCs)
Aminopeptidase
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Cancer
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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 .
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- HY-P10760
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Peptide-Drug Conjugates (PDCs)
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Cancer
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PhAc-ALGP-Dox, a peptide-drug conjugate, is a novel anticancer prodrug, with IC50 values ranged from 311 nM to 34.25 μM for TNBC (E0771), normal murine epithelium (HC-11), human TNBC (MDA-MB-231 and MDA-MB-468), human CrC (LS 174T), normal human epithelium (HME-1) cells .
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- HY-P10783
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Peptide-Drug Conjugates (PDCs)
Integrin
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Cancer
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BGC0222 is a novel prodrug of Irinotecan (HY-16562). BGC0222, as a PEG-cRGD-conjugated Irinotecan (HY-16562) derivative, could slowly and steadily release Irinotecan (HY-16562). BGC0222 binds to αVβ3 with IC50 values of 4.25 μM (αVβ3) and 58.7 μM (αVβ5). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99101
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AEX-4089
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ADC Antibody
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Cancer
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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 .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-17501S
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Bambuterol-d9 (hydrochloride) is the deuterium labeled Bambuterol. Bambuterol ((±)-Bambuterol) hydrochloride is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
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- HY-135853S
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Molnupiravir-d7 is the deuterium labeled Molnupiravir. 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[1][2].
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- HY-15284S
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Prasugrel-d5 is deuterium labeled Prasugrel. 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[1].
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- HY-B0021S1
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Doxifluridine-d3 is deuterated labeled Doxifluridine (HY-B0021). Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs .
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- HY-129934S
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Latanoprost ethyl amide-d4 (Lat-NEt-d4) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .
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| Cat. No. |
Product Name |
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Classification |
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- HY-159921
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Alkynes
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Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a palladium (Pd)-mediated tubulin polymerization inhibitor prodrug. Developed based on colchicine binding site inhibitors (CBSIs), it reduces toxicity and enhances targeted release properties. Compared to the parent compound, Tubulin Polymerization-IN-1 prodrug exhibited 68.3-fold lower cytotoxicity, which can be restored in situ in the presence of Pd resin. Mechanistic studies showed that its anticancer activity is consistent with CBSIs. In vivo, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth (63.2%) when activated by Pd resin. It holds promise for research in the field of anticancer therapy .
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