P-glycoprotein Substrate

P-glycoprotein Substrates (22):

Cat. No.	Product Name	Effect	Purity

HY-180935

Doxorubamine	Substrate
Doxorubamine is a Doxorubicin (HY-15142A) derivative. Doxorubamine is a poor substrate of P-glycoprotein. Doxorubamine efficiently kills agent-sensitive ovarian cancer.

HY-129987

Estradiol 17-(β-D-Glucuronide) sodium	Substrate	98.91%
Estradiol 17-(β-D-Glucuronide) sodium is a D-ring glucuronide metabolite of natural estrogen formed in the liver. Estradiol 17-(β-D-Glucuronide) sodium is a substrate of the organic anion-transporting polypeptide family (Oatp) and multidrug resistance-associated protein 2 (Mrp2). Estradiol 17-(β-D-Glucuronide) sodium regulates MRP8-mediated transport processes and inhibits MRP8-mediated transport of dehydroepiandrosterone 3-sulfate and taurocholic acid. Estradiol 17-(β-D-Glucuronide) sodium induces immediate, reversible reduction of bile flow and acute intrahepatic cholestasis in female rats without altering the bile acid composition in bile. Estradiol 17-(β-D-Glucuronide) sodium can be used in studies related to intrahepatic cholestasis.

HY-W353102

Estradiol 17-(β-D-Glucuronide)	Substrate	99.0%
Estradiol 17-(β-D-Glucuronide) is a D-ring glucuronide metabolite of natural estrogen formed in the liver. Estradiol 17-(β-D-Glucuronide) is a substrate of the organic anion-transporting polypeptide family (Oatp) and multidrug resistance-associated protein 2 (Mrp2). Estradiol 17-(β-D-Glucuronide) regulates MRP8-mediated transport processes and inhibits MRP8-mediated transport of dehydroepiandrosterone 3-sulfate and taurocholic acid. Estradiol 17-(β-D-Glucuronide) induces immediate, reversible reduction of bile flow and acute intrahepatic cholestasis in female rats without altering the bile acid composition in bile. Estradiol 17-(β-D-Glucuronide) can be used in studies related to intrahepatic cholestasis.

HY-D1078

5(6)-Carboxy-2',7'-dichlorofluorescein diacetate	Substrate
5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is a fluorescein-based reactive oxygen species (ROS) probe and also a MRP2 substrate. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate serves as a substrate for intracellular esterases, which cleave its acetate groups to generate a fluorescent product capable of detecting intracellular ROS. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is ATP-dependent and is transported via a single MRP2 binding site; it competes with LTC₄ for MRP2 binding sites and inhibits MRP2-mediated LTC₄ transport (Ex/Em = 496/525 nm).

HY-G0017

N-Desmethyl imatinib	Substrate	98.33%
N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.

HY-162495

IDOR-1117-2520	Substrate	99.94%
IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC₅₀ = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC₅₀ = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation.

HY-B0168B

Levomilnacipran hydrochloride	Substrate	99.95%
Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.

HY-G0017S

N-Desmethyl imatinib-d₈	Substrate	99.95%
N-Desmethyl imatinib-d₈ is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.

HY-142686A

SGK1-IN-3 hydrochloride	Substrate
SGK1-IN-3 hydrochloride (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC₅₀ of <1 nM against hSGK1. SGK1-IN-3 hydrochloride blocks the activity of CDK family members. SGK1-IN-3 hydrochloride serves as a P-glycoprotein substrate. SGK1-IN-3 can be used for the research of osteoarthritis.

HY-14895

Fabomotizole	Substrate	99.96%
Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects.

HY-162495A

(S)-IDOR-1117-2520	Substrate	99.47%
(S)-IDOR-1117-2520 is the S-isomer of IDOR-1117-2520 (HY-162495). IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC₅₀ = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC₅₀ = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation.

HY-170569

Cetagliptin	Substrate
Cetagliptin is an orally active inhibitor for dipeptidyl peptidase 4 (DPP-4) and CYP2D6 (IC₅₀ of 6 µM). Cetagliptin is a substrate for P-glycoprotein. Cetagliptin reduces the GLP-1 degradation, maintains the level of postprandial blood sugar, and can be used in type 2 diabetes mellitus research.

HY-14794A

Levomilnacipran	Substrate
Levomilnacipran ((1S,2R)-Milnacipran) is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.

HY-14794AS

Levomilnacipran-d₁₀ hydrochloride	Substrate
Levomilnacipran-d₁₀ ((1S,2R)-Milnacipran-d₁₀) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.

HY-G0017A

N-Desmethyl imatinib mesylate	Substrate
N-Desmethyl imatinib mesylate (Norimatinib mesylate) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib mesylate binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib mesylate induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib mesylate exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib mesylate can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.

HY-B0168BS

Levomilnacipran-d₅ hydrochloride	Substrate
Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.

HY-142686

SGK1-IN-3	Substrate
SGK1-IN-3 (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC₅₀ of <1 nM against hSGK1. SGK1-IN-3 blocks the activity of CDK family members. SGK1-IN-3 is a P-glycoprotein substrate. SGK1-IN-3 can be used for research on osteoarthritis.

HY-G0017S1

N-Desmethyl imatinib-d₄	Substrate
N-Desmethyl imatinib-d₄ is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.

HY-G0017R

N-Desmethyl imatinib (Standard)	Substrate
N‑Desmethyl imatinib (Standard) is the analytical standard of N‑Desmethyl imatinib (Norimatinib) (HY-G0017R). This product is intended for research and analytical applications. N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.

HY-129764

Prostaglandin F3α	Substrate
Prostaglandin F3α (PGF3α) is an eicosapentaenoic acid (EPA)-derived bioactive lipid mediator that has anti-cancer and anti-inflammatory effects. Prostaglandin F3α is a substrate of ABCC4 with a K_m of 12.1 μM. Prostaglandin F3α can be used for the research of diabetes.

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