2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. OY-101

OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764).

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OY-101 Chemical Structure

OY-101 Chemical Structure

CAS No. : 41183-02-2

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OY-101 Related Antibodies

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Description

OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764)[1].

In Vitro

OY-101 shows excellent synergistic anti-cancer effect with Vincristine (HY-N0488A) against drug-resistant cells Eca109/VCR, with an IC50 of 9.9 ± 1.3 nM[1].
OY-101 (0-5 μM) is not significantly toxic to Eca109/VCR cells, and exhibits significantly increased Vincristine (HY-N0488A) sensitization in Eca109/VCR cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

OY-101 Related Antibodies

Cell Viability Assay[1]

Cell Line: Eca109/VCR cells
Concentration: 1.0, 2.5, and 5.0 μM
Incubation Time: 48 h
Result: Exhibited significantly increased Vincristine sensitization in Eca109/VCR cells, achieving around 3.7, 103.4, and 690.6-fold reversal activity, respectively.
In Vivo

OY-101 (30 mg/kg/2 days, IG, for 3 weeks) increases Vincristine (HY-N0488A) sensitization in vivo without obvious toxicity[1].
OY-101 (Intravenous (3 mg/kg) and oral administration (30 mg/kg); once) shows good pharmacokinetics[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (4-5 weeks old, xenograft model bearing P-gp-overexpressing Eca109/VCR cells)[1]
Dosage: 30 mg/kg
Administration: IG, once every 2 days, for 3 weeks, 1 h before tail vein injection of Vincristine (HY-N0488A)
Result: Only co-administration OY-101 with Vincristine can effectively inhibit tumor proliferation in vivo (P < 0.001) and significantly reduce tumor weight. After 3 weeks of treatment, the tumor growth inhibition rate of the OY-101/Vincristine combination was 79.13%, which was significantly lower than that of the single-treatment group and the vehicle group.
Animal Model: SD rats (8 week-old, male, 300-400 g)[1]
Dosage: 3 mg/kg (IV), 30 mg/kg (PO)
Administration: Intravenous and oral administration, once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of OY-101 in male Sprague-Dawley rats[1].
IV (3 mg/kg) PO (30 mg/kg)
Tmax (h) 0.17 ± 0.12 0.38 ± 0.18
Cmax (ng/mL) 1573.20 ± 143.97 636.55 ± 355.60
AUC0-t (ng/mL∗h) 2688.45 ± 180.10 2665.45 ± 450.92
t1/2 (h) 8.43 ± 7.83 7.37 ± 4.92
CL/F (L/kg/h) 1.10 ± 0.08 11.16 ± 2.10
Vz/F (L/kg) 12.84 ± 11.33 111.27 ± 56.82
F (%) 7.65 ± 2.15
Molecular Weight

433.54

Formula

C27H31NO4
CAS No.
SMILES

CN1C(CC2=CC=C(OC)C(OCC3=CC=CC=C3)=C2)C4=C(C=C(OC)C(OC)=C4)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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OY-101 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OY-10141183-02-2OY101OY 101P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243LX-2HK-2HEK293TGES-1Eca109/VCRefflux functionmultidrug resistanceInhibitorinhibitorinhibit

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