Search Result
Results for "
ester prodrug
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-163849
-
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Others
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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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-
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- HY-163850
-
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Interleukin Related
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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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Others
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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 .
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-
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- HY-163544
-
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Others
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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 .
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-
-
- HY-161687
-
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Src
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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 .
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-
-
- HY-169131
-
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AMPK
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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 .
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-
-
- HY-149025
-
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P18
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Phospholipase
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Inflammation/Immunology
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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 .
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-
-
- HY-139995
-
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Others
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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 .
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-
-
- 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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Others
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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 .
|
-
-
- HY-131336
-
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mGluR
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Neurological Disease
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MGS0274, an ester-based lipophilic proagent of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia .
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-
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- HY-A0019A
-
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9-Hydroxyrisperidone palmitate
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Dopamine Receptor
5-HT Receptor
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Neurological Disease
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Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester proagent of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia .
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-
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- HY-145774
-
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester proagent of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice .
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-
-
- HY-B1152
-
-
-
- HY-A0032
-
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CMV
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Infection
|
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Valganciclovir, the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir.
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-
-
- HY-127122
-
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HBV
|
Infection
|
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Valtorcitabine dihydrochloride is a prodrug of L-deoxycytidine and also is an HBV inhibitor .
|
-
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- HY-B1149
-
-
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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.
|
-
-
- HY-109755
-
-
-
- HY-162410
-
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Others
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Cancer
|
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Fluplatin is a prodrug composed of cisplatin and fluvastatin. Fluplatin has antitumor activity .
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-
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- HY-137238
-
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Others
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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
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-
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- HY-17422C
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Aciclovir alaninate; Acycloguanosine alaninate
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Others
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Infection
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Acyclovir alaninate (Aciclovir alaninate) is a pro-drug of Acyclovir (HY-17422)
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- HY-118983
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Antibiotic
Bacterial
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Infection
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Pivampicillin hydrochloride is a penicillin antibiotic. Pivampicillin hydrochloride is a prodrug of Ampicillin (HY-B0522) .
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- HY-12758
-
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BCRP
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Cancer
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YHO-13351 is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
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-
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- HY-162448
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-
-
- HY-133027
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Tetradecyl nicotinate
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Others
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Cancer
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Myristyl nicotinate (Tetradecyl nicotinate) is an ester proagent 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 .
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- HY-B1079
-
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Others
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Inflammation/Immunology
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Suxibuzone is a drug used for joint and muscular pain, is a prodrug of the non steroidal anti inflammatory drug Phenylbutazone.
|
-
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- 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
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-
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- HY-19495
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Others
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Others
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OT-730 is an innovative selective beta-blocker prodrug designed for research into ocular diseases.
|
-
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- 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-153260
-
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CDK
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Cancer
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TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor .
|
-
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- HY-157127
-
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Others
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Metabolic Disease
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Ketoprofen L-thyroxine ester is a prodrug of Ketoprofen. Ketoprofen L-thyroxine ester reservoir and release ketoprofen slowly in the brain .
|
-
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- HY-B0382
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-
-
- HY-107026
-
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HBV
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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-126719
-
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Others
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Neurological Disease
|
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R-1 Methanandamide Phosphate is a water-soluble prodrug analog of arachidonylethanolamide (AEA). AEA is an endogenous cannabinoid compound .
|
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- HY-137362
-
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Others
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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-135077
-
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Others
|
Others
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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
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Cancer
|
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Methotrexate-alpha-alanine is a prodrug for activation by enzyme-monoclonal antibody conjugates. Methotrexate-alpha-alanine shows cytotoxicity .
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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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- 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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-
-
- HY-B1064
-
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Clindamycin 2-phosphate; U-28508
|
Bacterial
Antibiotic
Parasite
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Infection
|
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Clindamycin phosphate (Clindamycin 2-phosphate) is a broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin phosphate is the proagent of Clindamycin (HY-B1455) with no antimicrobial activity in vitro but can be rapidly converted in vivo to the active parent agent, Clindamycin, by phosphatase ester hydrolysis. Clindamycin phosphate can be used for researching acne and bacterial vaginosis .Clindamycin phosphate has no cytotoxicity。 Combined with platelet rich fibrin (PRF), PRF-Clindamycin phosphate enhances antimicrobial properties .
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- HY-B1064A
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Clindamycin 2-phosphate hydrochloride; U-28508 hydrochloride
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Bacterial
Antibiotic
Parasite
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Infection
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Clindamycin phosphate (Clindamycin 2-phosphate) hydrochloride is a broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin phosphate hydrochloride is the proagent of Clindamycin (HY-B1455) with no antimicrobial activity in vitro but can be rapidly converted in vivo to the active parent agent, Clindamycin, by phosphatase ester hydrolysis. Clindamycin phosphate hydrochloride can be used for researching acne and bacterial vaginosis .
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- HY-124584
-
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Apoptosis
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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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-
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- HY-129464
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-
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- HY-162926
-
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Bacterial
|
Infection
|
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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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-
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- HY-120639
-
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Others
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Others
|
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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.
|
-
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- 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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-
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- HY-125939
-
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Proteasome
|
Cancer
|
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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 .
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- HY-154842
-
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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 .
|
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- HY-157779
-
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Reactive Oxygen Species
|
Metabolic Disease
|
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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-162038
-
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MMP
|
Others
|
|
RXP03 is a MMPs inhibitor with the Ki of 20 nM, 2.5 nM, 10 nM, 5nM and 105 nM for MMP-2, MMP-8, MMP-9, MMP-11, MMP-14, respectively .
|
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- HY-123754
-
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Proton Pump
|
Inflammation/Immunology
|
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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-16511
-
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WX-671
|
Ser/Thr Protease
PAI-1
|
Cancer
|
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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.
|
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- HY-120313
-
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Others
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Cancer
|
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SN23862 is a cancer prodrug with anti-cancer activity, and an analogue of CB-1954 (HY-13543). SN23862 can be used for cancer research .
|
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- HY-16123
-
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DNA Alkylator/Crosslinker
|
Cancer
|
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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
-
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KUC-7483 hydrochloride
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
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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-17501S
-
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(±)-Bambuterol-d9 hydrochloride; KWD-2183-d9 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
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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.
|
-
- HY-108920
-
|
4-Cl-KYN; AV-101
|
Others
|
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-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-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-15406
-
-
- HY-129914
-
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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-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-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-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-160207
-
-
- 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-10213A
-
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PF-04929113 mesylate
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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.
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-
- 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-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-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-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
-
|
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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-117630
-
|
|
Others
|
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 .
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-
- HY-108475
-
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DYRK
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Cancer
|
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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-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-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-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-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-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-113929
-
|
R-58425
|
Others
|
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-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-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-147015
-
|
|
Orthopoxvirus
|
Infection
|
|
HOE961, the diacetate ester proagent of S2242, is active against respiratory cowpox virus infections, is orally active in infection models. Anti-orthopoxvirus activity .
|
-
- 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-10127
-
Barasertib
Maximum Cited Publications
16 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-137453C
-
|
(R,1R)-HS-10234
|
Others
|
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-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-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-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-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-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-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-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-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-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-157222
-
|
|
Others
|
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-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-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. .
|
-
- 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-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-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-125309
-
|
|
Others
|
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-A0267
-
|
|
Others
|
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-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-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-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-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-137362R
-
|
|
Others
|
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-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-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-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-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-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-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-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-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
-
|
|
Others
|
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-W209628
-
|
Methyl acetylsalicylate
|
Others
|
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-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-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-137492
-
|
|
Others
|
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-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-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-161821
-
|
|
Others
|
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
|
Others
|
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-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-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-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-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-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-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-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-167840
-
|
|
Others
|
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-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-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-134123
-
|
LXB4 methyl ester
|
Others
|
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-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-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-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-161838
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ATM/ATR
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Cancer
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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.
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- HY-131605
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GCV-TP
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Others
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Cancer
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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 .
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- HY-116161A
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Prostaglandin Receptor
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Endocrinology
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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.
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- HY-163525
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HSV
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Infection
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LAVR-289 is a [(Z)-3-(acetoxymethyl)-4-(2,4-diaminopyrimidin-6-yl)oxy-but-2-enyl]phosphonic acid prodrug with broad-spectrum anti-DNA virus activity. LAVR-289 can inhibit the activity of the wild-type (TK+) of varicella-zoster virus (VZV), thymidine kinase VZV-defective strain, human cytomegalovirus (HCMV), vaccinia virus (VV), and human herpesvirus 1 (HSV-1) (TK-) with EC50 values of 3.5 nM, 18 nM, 21 nM, 50 nM, and 8.5 nM, respectively .
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- HY-134160
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5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil
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Others
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Cancer
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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.
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- HY-139124
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15(R)-Carboprost; 15(R)-15-methyl PGF2α
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Others
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Metabolic Disease
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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.
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- HY-129934
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Lat-NEt
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Prostaglandin Receptor
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Endocrinology
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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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- HY-15334
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VEGFR
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Cancer
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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 .
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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. .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| 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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