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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
50 Results for "
substrate efflux
" in MedChemExpress (MCE) Product Catalog:
Products (50)
50 Results for "substrate efflux" in MCE Product Catalog:
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1
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Moxidectin (CL301423) is an orally active and brain-penetrant macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
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
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 .
Cat. No.: HY-D0180
CAS No.: 17455-13-9
Synonyms: 18C6; 1,4,7,10,13,16-Hexaoxacyclooctadecane
Cat. No.: HY-B0501
CAS No.: 119478-55-6
Synonyms: CP 76136-27
Target:
Research Areas:
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-W014118
CAS No.: 101-86-0
Target:
Cat. No.: HY-N0406
CAS No.: 861691-37-4
Category:
Flavonoids Plants Other Families Extract Disease Research Fields Inflammation/Immunology Isoflavones
Target:
Cat. No.: HY-B0777S
Synonyms: CL-301423-d3
Cat. No.: HY-173162
CAS No.: 86383-89-3
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Research Areas:
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .
Cat. No.: HY-B1751S
CAS No.: 1267657-68-0
Quinidine-d3 is the d3-labeled Quinidine (15% dihydroquinidine) (HY-B1751). Quinidine (15% dihydroquinidine) is an orally active antiarrhythmic agent. Quinidine (15% dihydroquinidine) reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine (15% dihydroquinidine) exerts sustained block and open-channel block effects on IK(f). Quinidine (15% dihydroquinidine) alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine (15% dihydroquinidine) can be used in studies related to uterine sarcoma and seizures .
Cat. No.: HY-128038
CAS No.: 66164-07-6
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Research Areas:
N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
Cat. No.: HY-161246
CAS No.: 2323525-19-3
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uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
Cat. No.: HY-185057
CAS No.: 41656-56-8
Synonyms: S-Lactylglutathione; (R)-S-Lactoylglutathione
Research Areas:
Cat. No.: HY-149812
CAS No.: 2890177-95-2
Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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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
