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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
93 Results for "
first-generation
" in MedChemExpress (MCE) Product Catalog:
Products (93)
93 Results for "first-generation" in MCE Product Catalog:
91
91 Publications Verification
Synonyms: (±)-Verapamil; CP-16533-1
Research Areas:
Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
91
91 Publications Verification
Synonyms: (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride
Research Areas:
Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
17
Target:
Adrenergic Receptor ERK JNK p38 MAPK NF-κB AP-1 Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism TNF Receptor
Research Areas:
Desipramine hydrochloride is a first-generation tricyclic antidepressant. Desipramine hydrochloride selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine hydrochloride activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine hydrochloride also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine hydrochloride can be used for the research of hepatocellular cancer, inflammation, and neurological diseases .
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Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Cefazolin (Cephazolin) is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
13
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Cefazolin sodium is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin sodium has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
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9
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Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 μg/ml .
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6 Cited Publications
Research Areas:
CX546 is a first-generation and selective benzamide-type positive AMPAR modulator. CX546 is a prototypical ampakine agent and has antipsychotic effects .
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Target:
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Clodronic acid (Clodronate) disodium salt is an orally active bisphosphonate. Clodronic acid disodium salt inhibits osteoclast-mediated bone resorption. Clodronic acid disodium salt reduces skeletal event risk in malignant bone disease, impairs malignant osteolysis, blocks bone matrix growth-factor release, induces apoptosis in osteoclasts and macrophages. Clodronic acid disodium salt is effective in the maintenance or improvement of bone mineral density. Clodronic acid disodium salt can be used for the research of multiple myeloma and postmenopausal osteoporosis .
5
5 Cited Publications
Synonyms: Disodium clodronate tetrahydrate
Target:
Research Areas:
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .
2
Target:
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Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.
2
Target:
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Vebicorvir (ABI-H0731) is a first-generation hepatitis B virus (HBV) core protein inhibitor. Vebicorvir (ABI-H0731) suppresses covalently closed circular DNA (cccDNA) formation in two de novo infection models with EC50s from 1.84 μM to 7.3 μM .
2
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Acetohexamide is an orally active first-generation sulfonylurea agent used in research related to type 2 diabetes and cancer. Acetohexamide exerts reductase activity in human erythrocytes. Acetohexamide stimulates the pancreas to secrete insulin. Acetohexamide inhibits ATP-sensitive potassium channels in the β cells of the pancreas. Acetohexamide can inhibit the formation of circular chemorepellent induced defects (CCIDs) in lymphendothelial cell (LEC) monolayers. Acetohexamide inhibits markers of epithelial-to-mesenchymal-transition and migration. Acetohexamide suppresses the synthesis of 12(S)-HETE. Acetohexamide can potentiate hypoglycaemic action .
1
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Promethazine is an orally active histamine receptor antagonist . Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects .
1
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Dinitolmide (Zoalene) is an orally active anticoccidial agent used as a fodder additive. Dinitolmide has a wide anticoccidial spectrum with no effect on host immunity. Dinitolmide mainly acts on the first generation merozoite stage of coccidia and also has an inhibitory effect on the sporulation process of oocysts. Dinitolmide has anti-Toxoplasma gondii effect in vitro with an EC50 of 3.625 μg/mL. Dinitolmide can be used to inhibits infections caused by Eimeria tenella .
Cat. No.: HY-D1458
CAS No.: 817170-66-4
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Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis . Pericyazine is a selective D2-dopamine receptor antagonist . Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects .
Cat. No.: HY-W011651
CAS No.: 339-43-5
Synonyms: BZ-55
Target:
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Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity .
Target:
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Triprolidine hydrochloride monohydrate, a first-generation antihistamine, is an oral active histamine H1 antagonist. Triprolidine hydrochloride monohydrate can be used for the research of allergic rhinitis. Triprolidine hydrochloride monohydrate exhibits spinal motor and sensory block in rats .
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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
