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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
17 Results for "
MDCK-MDR1 cells
" in MedChemExpress (MCE) Product Catalog:
Products (17)
17 Results for "MDCK-MDR1 cells" in MCE Product Catalog:
Cat. No.: HY-167856
CAS No.: 3034664-39-3
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RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
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RTI-7470-44 is an orally active and blood-brain barrier-permeable antagonist of trace amine-associated receptor 1 (hTAAR1) with a Ki of 0.3 nM. RTI-7470-44 inhibits hTAAR1-mediated cAMP production and signal transduction (IC50 = 8.4 nM), and blocks hTAAR1-mediated GIRK current responses. RTI-7470-44 increases the spontaneous firing frequency of dopaminergic neurons and reduces collagen-induced platelet aggregation. RTI-7470-44 can be used in studies related to Parkinson's disease and gastric emptying .
Cat. No.: HY-143792
CAS No.: 2254502-89-9
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HTT-D3 is an orally active, blood-brain barrier penetrant splicing modulator of huntingtin (HTT). HTT-D3 promotes the inclusion of a pseudo-exon containing a premature termination codon into HTT pre-mRNA, triggers nonsense-mediated mRNA degradation and reduces HTT protein levels. HTT-D3 induces dose-dependent, comparable reductions in mutant HTT protein in both the brain and peripheral tissues of transgenic mouse models. HTT-D3 can be used for the research of Huntington's disease .
Cat. No.: HY-10486
CAS No.: 361444-66-8
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JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal .
Cat. No.: HY-155152
CAS No.: 3052839-42-3
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P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
Cat. No.: HY-116524
CAS No.: 1648726-56-0
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PF-04781340 is a potent and selective 5-HT2C receptor agonist, with an EC50 of 9 nM and a Ki of 3 nM, respectively. PF-04781340 exhibits weak partial agonist activity at the 5-HT2B receptor, with an EC50 of 1484 nM. PF-04781340 can be used in the research of obesity and psychiatric disorders .
Cat. No.: HY-156434
CAS No.: 3027607-92-4
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PDE11A4-IN-1 is a selective, cell-permeable inhibitor of phosphodiesterase 11A4 (PDE11A4) with an IC50 of 12 nM. PDE11A4-IN-1 inhibits PDE11A4-mediated hydrolysis of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) to the same extent. PDE11A4-IN-1 can be used in the research of age-related cognitive decline .
Cat. No.: HY-183247
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BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC50 19 nM, Ki 8.8 nM, Ka 1.6 nM, and BRDT-T IC50 56 nM, Ka 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma .
Cat. No.: HY-184573
CAS No.: 90471-34-4
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Dopamine D2 receptor modulator-1 is a positive allosteric modulator of hD2R. Dopamine D2 receptor modulator-1 enhances the potency of Dopamine (HY-B0451) on hD2R without intrinsic agonist activity. Dopamine D2 receptor modulator-1 protects dopaminergic differentiated cells from neurotoxic damage. Dopamine D2 receptor modulator-1 exhibits neuroprotective activity. Dopamine D2 receptor modulator-1 can be used in the research of Parkinson's disease .
Cat. No.: HY-116524A
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PF-04781340 TFA is a potent and selective 5-HT2C receptor agonist, with an EC50 of 9 nM and a Ki of 3 nM, respectively. PF-04781340 TFA exhibits weak partial agonist activity at the 5-HT2B receptor, with an EC50 of 1484 nM. PF-04781340 TFA can be used in the research of obesity and psychiatric disorders .
Cat. No.: HY-184206
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A-3190 is an orally active, blood-brain barrier permeable CD38 inhibitor, with an IC50 of 7.25 nM against human CD38 and 1.24 nM against mouse CD38. A-3190 is a derivative of A-8531 (HY-184021), and it forms covalent adducts with NAD + in the presence of CD38. A-3190 acts as an inducer of NAD + levels and an inhibitor of NAM and ADPR levels. A-3190 increases NAD + levels in the skin, lung, liver and brain of rodents, while reducing NAM and ADPR levels in brain tissues. A-3190 can be used in research related to multiple sclerosis, Parkinson's disease and Alzheimer's disease .
Cat. No.: HY-184021
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A-8531 is an orally active CD38 inhibitor with IC50 values of 1.10 nM against human CD38, IC50 values of 2.93 nM against mouse CD38, and a human Ka of 0.32 nM. A-8531 exerts its inhibitory activity via its 4-pyridine reactive warhead interacting with the CD38 substrate NAD +, and binds stably to CD38 only in the presence of NAD +, with a binding KD of 0.32 nM as detected by SPR. A-8531 dose-dependently increases NAD + levels in mouse skin, lung and liver tissues, while simultaneously reducing the contents of NAM and ADPR in these tissues. A-8531 derivative A-3190 (HY-184206) has blood-brain barrier penetration. A-8531 can be used in studies related to neurodegenerative diseases .
Cat. No.: HY-183203
CAS No.: 1451993-12-6
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VU0476406 is a blood-brain barrier-permeable and selective muscarinic acetylcholine receptor subtype 4 (M4) activator with human EC50 of 91.0 nM and human pEC50 of 7.04. VU0476406 potentiates endogenous acetylcholine activity at M4 receptors. VU0476406 can be used for the research of Parkinson's disease .
Cat. No.: HY-182697
CAS No.: 2130881-32-0
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RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([ 35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder .
Cat. No.: HY-184596
CAS No.: 3055537-47-5
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VU6066098 is a blood-brain barrier penetrant, orally active inhibitor of metabotropic glutamate receptor subtype 2 (mGlu2), with IC50 values of 77 nM and 111 nM against human and rat targets, respectively. VU6066098 induces antidepressant-like activity, inhibits psychosis-like hyperlocomotion, enhances recognition memory and associative learning, and reverses cognitive deficits caused by blast-related traumatic brain injury. VU6066098 can be used in research on major depressive disorder, schizophrenia, Alzheimer's disease, and traumatic brain injury .
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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
