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BCRP substrates

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By Targets:	BCRP (5) 5-HT Receptor (2) Antibiotic (3) ATP-binding cassette (ABC) transporters (2) Drug Metabolite (2) Endogenous Metabolite (2) Isotope-Labeled Compounds (1) OAT (2) P-glycoprotein (3) Parasite (3) Reference Standards (1)
By Research Areas:	Cancer (2) Infection (3) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (3)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: BCRP

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0777

Moxidectin 1 Publications Verification CL301423	Antibiotic BCRP P-glycoprotein Parasite	Infection Neurological Disease
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 .

HY-N7755

Estradiol 3-glucuronide sodium	Endogenous Metabolite ATP-binding cassette (ABC) transporters OAT	Others
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* .

HY-W585842

Estradiol 3-glucuronide	Endogenous Metabolite ATP-binding cassette (ABC) transporters OAT	Others
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* .

HY-B0777S

Moxidectin-d3 CL-301423-d₃	Isotope-Labeled Compounds BCRP Parasite Antibiotic P-glycoprotein	Infection
Moxidectin-d₃ (CL-301423-d₃) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active 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 .

HY-161246

uPSEM792	5-HT Receptor	Neurological Disease
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM ⁴-GlyR, with an affinity of K_i 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 .

HY-120464

PF-05212377 SAM-760	5-HT Receptor	Neurological Disease
PF-05212377 (SAM-760) is an inhibitor for serotonin receptor 5-HT6. PF-05212377 is a substrate for P-gp/non-BCRP human transporter. PF-05212377 exhibits blood brain barrier permeability in non-human primates. PF-05212377 can be used for Alzheimer’s Disease research .

HY-172233

INCB-056868	BCRP Drug Metabolite	Metabolic Disease
INCB-056868 is the metabolite M11 of Epacadostat (HY-15689). INCB-056868 can also serve as a substrate for *BCRP*. INCB-056868 is promising for research of metabolic diseases .

HY-B0777R

Moxidectin (Standard) CL301423 (Standard)	Antibiotic BCRP P-glycoprotein Parasite Reference Standards	Infection
Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active 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 .

HY-N9440

7-Hydroxycoumarin glucuronide	Drug Metabolite	Inflammation/Immunology Cancer
7-Hydroxycoumarin glucuronide is a transport substrate and main human coumarin metabolite. 7-Hydroxycoumarin glucuronide undergoes ATP-dependent efflux transport via MRP3 and MRP4. 7-Hydroxycoumarin glucuronide undergoes active transport processes for urinary excretion and is primarily excreted into urine in humans.

HY-118083

Pentamethoxymorin MRS923	BCRP	Cancer
Pentamethoxymorin (MRS923) is a selective breast cancer resistance protein (BCRP/ABCG2) inhibitor. Pentamethoxymorin shows selectivity for BCRP over P-gp and MRP1. Pentamethoxymorin inhibits MDCK BCRP cells with IC₅₀ vaues of 5.98 μM and 5.94 μM in Hoechst 33342 (HY-15559) assay and Pheophorbide A (HY-125665) assay, respectively. Pentamethoxymorin can be used for the study of ccancer .

Cat. No.	Product Name	Chemical Structure

HY-B0777S

Moxidectin-d3
Moxidectin-d₃ (CL-301423-d₃) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active 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 .

Moxidectin-d3

Moxidectin-d₃ (CL-301423-d₃) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active 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 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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