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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
62 Results for "
apical
" in MedChemExpress (MCE) Product Catalog:
Products (62)
62 Results for "apical" in MCE Product Catalog:
13
Research Areas:
Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment .
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9 Cited Publications
Cat. No.: HY-104081
CAS No.: 11041-12-6
Synonyms: Cholestyramine resin; Colestyramine
Research Areas:
Cholestyramine (Cholestyramine resin) is an orally active bile acid sequestrant. Cholestyramine upregulates the expression of intestinal Apical sodium-dependent bile acid transporter and hepatic Cholesterol 7α-hydroxylase. Cholestyramine induces the expression of intestinal and hepatic cholesterol synthesis genes as well as hepatic lipogenesis genes, and promotes bile acid- and neutral sterol-mediated reverse cholesterol transport. Cholestyramine reduces intestinal cholesterol absorption and induces cholesterol efflux. Cholestyramine is applicable to research related to coronary artery disease, atherosclerotic cardiovascular disease and atherosclerosis .
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Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
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Erenapursta (E3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. Erenapursta is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. Erenapursta shows anticancer activities .
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2 Cited Publications
Cat. No.: HY-W014622
CAS No.: 6960-45-8
Target:
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CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds .
2
Hycanthone is an apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor, DNA intercalator and Antischistosomal agent, with an IC50 of 80 nM against APE1. Hycanthone irreversibly inhibits thymidine incorporation into DNA in adult sensitive *Schistosoma mansoni*, while exerts weak inhibitory effects on uridine and leucine incorporation. Hycanthone reduces influenza virus-induced interferon production. Hycanthone exhibits mutagenic effects in various organisms, shows teratogenicity in mice and rabbits, and induces neoplastic liver lesions in partially hepatectomized mice. Hycanthone can be used in research related to schistosomiasis and cancer .
1
1 Cited Publications
Cat. No.: HY-N7755
CAS No.: 14982-12-8
Research Areas:
Estradiol 3-glucuronide sodium is an estrogen metabolite, which is a glucuronide conjugate formed by the catalysis of uridine diphosphate glucuronosyltransferase in tissues such as the liver from Estradiol (HY-B0141). Estradiol 3-glucuronide sodium is a potent substrate of Mrp2, with an S50 of 55.7 μM. Estradiol 3-glucuronide sodium achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP .
1
1 Cited Publications
Cat. No.: HY-W585842
CAS No.: 15270-30-1
Research Areas:
Estradiol 3-glucuronide is an estrogen metabolite, which is a glucuronide conjugate formed from Estradiol (HY-B0141) via catalysis by uridine diphosphate glucuronosyltransferases in tissues such as the liver. Estradiol 3-glucuronide is a potent substrate of Mrp2, with an S50 value of 55.7 μM. Estradiol 3-glucuronide achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP .
1
1 Cited Publications
Target:
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APE-PLD (VU533) activator is a potent NAPE-PLD activator with an EC50 value of 0.30 µM. NAPE-PLD activator (VU533) can enhance NAPE-PLD activity and increase efferocytosis by macrophages. NAPE-PLD activator (VU533) can be used for cardiometabolic diseases research .
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APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells .
Cat. No.: HY-101190
CAS No.: 1025216-57-2
Synonyms: SHP626; LUM002
Research Areas:
Volixibat (SHP626) is a highly selective, minimally absorbed, and competitive apical sodium-dependent bile acid transporter (ASBT) inhibitor. Volixibat has potential for treatment for non-alcoholic steatohepatitis (NASH) .
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Bendroflumethiazide (Bendrofluazide) is an orally available diuretic. Bendroflumethiazide inhibits the electroneutral sodium-chloride symporter located in the apical membrane of the early segment of the distal convoluted tubule and can effectively lower blood pressure. Bendroflumethiazide is used in the study of hypertension and edema. Bendroflumethiazide has an antidiuretic effect in diabetes insipidus .
Research Areas:
eIF4A-IN-3, Silvestrol (HY-13251) analogue, is an eIF4A inhibitor. eIF4A-IN-3 blocks protein translation initiation by interfering with eIF4F complex assembly, preferentially inhibiting translation of mRNAs with long, highly structured 5'-untranslated regions. eIF4A-IN-3 inhibits proliferation of human breast cancer cells. eIF4A-IN-3 has moderate apical to basolateral permeability in intestinal cell monolayers and a low efflux ratio .
Research Areas:
Cat. No.: HY-130487
CAS No.: 304880-74-8
miR-21-IN-2 is a high-affinity miR-21 inhibitor. miR-21-IN-2 binds to the apical loop region of the pre-miR-21 hairpin, inhibits Dicer-mediated processing, and thereby blocks the biosynthesis of mature miR-21. miR-21-IN-2 can be used for the research of microRNA-related diseases .
Synonyms: TCBZ-SO
Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
Cat. No.: HY-120069
CAS No.: 1415030-15-7
APX2009 is a specific APE1/REF-1 redox inhibitor with anticancer activities which decreases the proliferative, migratory, and invasive properties of breast cancer cell and induces apoptosis in breast cancer cell .
Cat. No.: HY-119993
CAS No.: 510721-85-4
Synonyms: BMH-23
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AR03 (BMH-23) is an apurinic/apyrimidinic endonuclease 1 (Ape1) inhibitor with an IC50 of 2.1 µM. AR03 has low affinity for double-stranded DNA. AR03 potentiates the cytotoxicity of methyl methanesulfonate and temozolomide in SF767 cells .
Cat. No.: HY-148795
CAS No.: 2460667-52-9
Research Areas:
Ritivixibat is an apical sodium-dependent bile acid transporter (ASBT/IBAT) inhibitor. Ritivixibat blocks ASBT/IBAT function, thereby reducing bile acid reabsorption, regulating bile acid homeostasis and alleviating liver injury. Ritivixibat protects cholangiocytes from damage caused by cytotoxic bile acids. Ritivixibat is applicable to research related to primary sclerosing cholangitis .
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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
