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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
336 Results for "
Rb efflux
" in MedChemExpress (MCE) Product Catalog:
Products (336)
336 Results for "Rb efflux" in MCE Product Catalog:
1
1 Cited Publications
Cat. No.: HY-D0194
CAS No.: 111843-78-8
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5 (6)-Carboxy-2',7'-dichlorofluorescein is a fluorescent probe substrate that acts on MRP1 and MRP3/Mrp3, passively diffuses across cell membranes, and is actively effluxed by MRP1 in MRP1-positive cells. 5 (6)-Carboxy-2',7'-dichlorofluorescein is transported across membranes in an ATP-dependent manner, but does not stimulate ATPase activity .
1
1 Cited Publications
Cat. No.: HY-N7755
CAS No.: 14982-12-8
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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
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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 .
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1 Cited Publications
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Finafloxacin is an orally active fourth-generation fluoroquinolone broad-spectrum antibiotic. Finafloxacin exhibits stronger antibacterial activity in acidic pH environments and is not easily affected by bacterial multidrug efflux transporters. Finafloxacin is effective against a variety of extracellular pathogenic bacteria, and can also accumulate in macrophages, showing excellent antibacterial activity against intracellular Staphylococcus aureus, Listeria monocytogenes, Legionella pneumophila, Burkholderia pseudomallei, and other pathogens. Finafloxacin has been approved by the U.S. FDA for research on acute otitis externa mediated by Pseudomonas aeruginosa. Finafloxacin is also used in studies related to diseases such as melioidosis, inhalational tularemia, and inhalational plague .
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Rapastinel (GLYX-13) is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel is applicable to the research of major depressive disorder and hepatocellular carcinoma .
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Rapastinel (GLYX-13) Trifluoroacetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel Trifluoroacetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel Trifluoroacetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel Trifluoroacetate is applicable to the research of major depressive disorder and hepatocellular carcinoma .
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1 Cited Publications
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DPO-1 is a potent Kv1.5 and Kv1.3 (EC50 = 3.1 μM) channels inhibitor with potential immunomodulatory and anti-inflammatory effects. DPO-1 reduces Kv1.3 current density, blunts Ca 2+ influx in Ca 2+-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. DPO-1 inhibits Uric acid sodium (HY-B2130A) (MSU)-induced NLRP3 inflammasome activation by blocking Kv1.5-mediated K + efflux. DPO-1 can be used for the study of immunologic disorders and atrial fibrillation .
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1 Cited Publications
Synonyms: Hexahydroadiphenine hydrochloride
Target:
Cholinesterase (ChE) Potassium Channel Amyloid-β TRP Channel Tau Protein NOD-like Receptor (NLR) JNK NF-κB IKK
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Drofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
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1 Cited Publications
Cat. No.: HY-N0468
CAS No.: 63279-13-0
Category:
Terpenoids Metabolic Disease Diterpenoids Plants Other Families Extract Disease Research Fields Sweeteners Food Research
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Cat. No.: HY-B0501
CAS No.: 119478-55-6
Synonyms: CP 76136-27
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Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .
Cat. No.: HY-W040150
CAS No.: 77058-74-3
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24S,25-Epoxycholesterol is an agonist for Liver X Receptor (LXR). 24S,25-Epoxycholesterol exhibits properties in regulating the cholesterol efflux , inhibiting tumor growth against gastric cancer and glioblastoma and inducing apoptosis in BMMC cells .
Cat. No.: HY-124819
CAS No.: 957471-96-4
D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively . D13-9001 exhibits antibiotic activities .
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2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization .
Cat. No.: HY-N2947
CAS No.: 114567-34-9
Category:
Natural Products Phenols Polyphenols Plants Other Families Extract Disease Research Fields Inflammation/Immunology
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Cat. No.: HY-N0406
CAS No.: 861691-37-4
Category:
Flavonoids Plants Other Families Extract Disease Research Fields Inflammation/Immunology Isoflavones
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Cat. No.: HY-50879R
CAS No.: 143664-11-3
Synonyms: GF120918 (Standard); GW0918 (Standard); GG918 (Standard); GW120918 (Standard)
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Elacridar (Standard) is the analytical standard of Elacridar. This product is intended for research and analytical applications. Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .
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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
