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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
69 Results for "
preclinical study
" in MedChemExpress (MCE) Product Catalog:
Products (69)
69 Results for "preclinical study" in MCE Product Catalog:
3
2
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Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M pro and 3CL pro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 .
Cat. No.: HY-P990083
CAS No.: 2628092-47-5
Synonyms: AT-1501
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Synonyms: (1R,9R)-DX8951f
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(1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
Synonyms: (1S,9R)-DX8951f
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(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia .
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
Synonyms: ZGN-1061
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Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells .
Cat. No.: HY-P10943
CAS No.: 3051946-11-0
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Cat. No.: HY-18060
CAS No.: 639489-84-2
Synonyms: TC-5619
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Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
Cat. No.: HY-W011168
CAS No.: 13389-03-2
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8-Bromo-2'-deoxyguanosine is an inflammation-related DNA halogenated adduct and an early biomarker of inflammation-induced oxidative tissue damage. The formation of 8-Bromo-2'-deoxyguanosine precedes that of oxidative and nitrative products, and it can be generated via the MPO-H2O2-Cl --Br - system. 8-Bromo-2'-deoxyguanosine serves as the immunogen for preparing the monoclonal antibody mAb8B3, which can be used to detect early DNA modifications in preclinical models; its urinary level also increases significantly in inflammatory disease models. 8-Bromo-2'-deoxyguanosine can also be produced in the dermis of UV-B irradiated mice, and the extract of Coprinus comatus significantly reduces its level. 8-Bromo-2'-deoxyguanosine finds applications in studies related to inflammatory diseases, diabetes, hepatocellular carcinoma, and UV-B induced skin inflammation .
Cat. No.: HY-16632
CAS No.: 1333990-84-3
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ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease .
Cat. No.: HY-164725
CAS No.: 3023869-94-2
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Cat. No.: HY-105998
CAS No.: 1173103-84-8
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AVN-211 (CD-008-0173) is a selective and orally active 5HT6R antagonist with an IC50 of 2.34 nM and a Ki of 1.09 nM. AVN-211 exhibits 5K-fold higher 5HT6R selectivity over other 65 receptors, enzymes, and ion channels. AVN-211 significantly improves cognitive and anxiety behaviors in various AD animal models, and has good safety profiles. AVN-211 can be used for the study of Alzheimer's dementia .
Cat. No.: HY-145285
CAS No.: 2135514-20-2
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APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease .
Cat. No.: HY-163683
CAS No.: 2375590-67-1
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EB-PSMA-617 is a modified form of PSMA-617 that has enhanced pharmacokinetic properties by conjugating it to Evans Blue (EB) to extend its circulation half-life to improve prostate tumor uptake and radiotherapy efficacy. In preclinical studies using PC3-PIP-loaded mice, EB-PSMA-617 demonstrated prolonged blood half-life, increased accumulation in PSMA-positive tumors, and successful tumor elimination with lower radioactivity .
Cat. No.: HY-117799
CAS No.: 228418-82-4
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LY426965 is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
Cat. No.: HY-117799A
CAS No.: 326821-27-6
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LY-426965 hydrochloride is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
Cat. No.: HY-123582
CAS No.: 519052-02-9
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CP-866,087 is a novel, potent and selective μ-opioid receptor antagonist with activity to inhibit opioid effects. CP-866,087 has shown promising preclinical efficacy data in disease models associated with alcohol consumption. CP-866,087 has also been used to study female sexual dysfunction .
Cat. No.: HY-145284
CAS No.: 2762567-70-2
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APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease .
Cat. No.: HY-18060A
CAS No.: 1111941-90-2
Synonyms: TC-5619 hydrochloride
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Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
Cat. No.: HY-16469
CAS No.: 637774-61-9
SR13668 is a potent indole analog derived from indole-3-carbinol (I3C), known for its natural anticancer properties but limited by poor metabolic characteristics. Developed to enhance I3C's anticancer efficacy, SR13668 effectively inhibits growth factor-stimulated Akt activation. It demonstrates strong oral anticancer activity across different cancer types in preclinical studies, showing promise in clinical development due to its favorable safety profile and potent therapeutic effects .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
