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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
25 Results for "
Clinical efficacy
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "Clinical efficacy" in MCE Product Catalog:
2
2 Cited Publications
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(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
Synonyms: UK-453061
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Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC50=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains .
Cat. No.: HY-B0755
CAS No.: 362045-44-1
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Etimicin (sulfate), a fourth-generation aminoglycoside antibiotic, is now widely clinically used due to its high efficacy and low toxicity.
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-106614
CAS No.: 105149-00-6
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Osaterone acetate is an orally active steroid anti-androgen agent, mainly used for benign prostatic hyperplasia (BPH) in dogs. Osaterone acetate competitively antagonizes androgen receptor and inhibits 5α-reductase, reducing the concentration of dihydrotestosterone (DHT) while blocking the growth-stimulating effects of testosterone and DHT on prostate cells. Osaterone acetate can rapidly alleviate the symptoms of BPH in dogs without affecting the fertility of breeding dogs .
Cat. No.: HY-16525
CAS No.: 701909-57-1
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Cat. No.: HY-16622A
CAS No.: 1005407-76-0
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GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
Cat. No.: HY-12629
CAS No.: 1539296-45-1
Synonyms: PF-06297470
PF470 (PF-06297470) is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with significant efficacy in Parkinson's disease models, but clinical development was halted due to potential issues found in toxicology studies.
Cat. No.: HY-14915
CAS No.: 194785-19-8
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Bedoradrine is a highly selective β2-adrenergic agonist with activity in suppressing asthma and chronic obstructive pulmonary disease (COPD). Bedoradrine is administered by intravenous infusion and is specifically indicated for the suppression of acute asthma attacks. Bedoradrine has shown good safety and preliminary efficacy in clinical trials, especially in patients with stable moderate to severe asthma. The results of Bedoradrine studies have shown that it can provide clinical benefits without increasing clinical risks, especially for patients who are unable to use inhalation or nebulization suppression .
Cat. No.: HY-118557A
CAS No.: 210350-29-1
Synonyms: S-MPEC hydrochloride
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Iferanserin hydrochloride (S-MPEC hydrochloride) is a selective serotonin receptor antagonist with the potential to inhibit internal hemorrhoids. Iferanserin hydrochloride demonstrated efficacy and tolerability in ongoing Phase IIb clinical trials, with the ability to significantly reduce patient-reported symptoms of bleeding and pruritus .
Cat. No.: HY-116149
CAS No.: 1335145-56-6
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
Cat. No.: HY-B0357B
CAS No.: 112209-99-1
Synonyms: R-64433 sodium
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Diclazuril sodium (R-64433 sodium) is an anticoccidial agent active in preventing parasitic contamination of livestock and poultry feed. Evaluation of the efficacy of Diclazuril sodium in the treatment of Eimeria infection showed poor performance in sustained levels of oocyst excretion compared with controls. Diclazuril sodium has a significant impact on the pathological effects of young animals in clinical applications .
Cat. No.: HY-119467
CAS No.: 1366240-73-4
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MDK0734 is a selective inhibitor that inhibits feline hepsin B endopeptidase and exopeptidase activities. MDK0734 demonstrated efficacy in a cell-based in vitro tumor invasion model, significantly attenuating the invasive ability of MCF-10A neoT cells. MDK0734 provides new potential inhibitors for the development of clinically useful compounds targeting the deleterious effects of feline hepsin B in cancer progression .
Cat. No.: HY-13736
CAS No.: 87056-78-8
Synonyms: CV205-502
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Quinagolide (CV205-502) is a non-ergot dopamine D(2) receptor agonist that promotes dopamine activity. Quinagolide has shown effectiveness in modulating endocrine function, particularly in inhibiting disorders associated with dopamine deficiency. Quinagolide is used to suppress hyperprolactinemia and corresponding clinical symptoms, showing good efficacy. Quinagolide's biological activity enables its use as an important research compound in drug isolation and analysis .
Cat. No.: HY-167950
CAS No.: 849150-59-0
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PPARα/γ agonist 5 is a dual PPARα/γ agonist with significant biological activity exhibited at low concentrations. The EC50 of PPARα/γ agonist 5 are 0.358μM and 1.21μM respectively, showing its potential in inhibiting type 2 diabetes and lipid metabolism disorders. PPARα/γ agonist 5 was selected for clinical development due to its high efficacy .
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 .
Cat. No.: HY-16633
CAS No.: 1444006-79-4
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ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease .
Cat. No.: HY-12193
CAS No.: 556835-30-4
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A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
Cat. No.: HY-116184
CAS No.: 1604034-71-0
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PF-05387252 is a potent and selective IRAK4 inhibitor with the activity of inhibiting endogenous TLR signaling pathways. PF-05387252 has shown anti-inflammatory activity in experimental models and may have potential clinical application value in inhibiting psoriasis. Although PF-05387252 and its related compounds have shown anti-inflammatory effects in animal models, their efficacy in inhibiting psoriasis has not yet been verified .
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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
