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Art. -Nr.: HY-149053

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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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CAS. Nr.: 41183-02-2
Formel: C₂₇H₃₁NO₄
Molecular Weight:433.54

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

OY-101 Chemical Structure

CAS. Nr.: 41183-02-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
ECa-109 cell line	IC₅₀	>100 μM Compound: 39; OY-101	Cytotoxicity against human Eca-109 cells incubated for 48 hrs by CCK-8 method Cytotoxicity against human Eca-109 cells incubated for 48 hrs by CCK-8 method	[PMID: 36892076]
ECa-109 cell line	IC₅₀	1872 nM Compound: 39; OY-101	Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 1 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM) Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 1 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)	[PMID: 36892076]
ECa-109 cell line	IC₅₀	66.1 nM Compound: 39; OY-101	Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 2.5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM) Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 2.5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)	[PMID: 36892076]
ECa-109 cell line	IC₅₀	9.9 nM Compound: 39; OY-101	Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM) Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)	[PMID: 36892076]
GES1	IC₅₀	>50 μM Compound: 39; OY-101	Cytotoxicity against human GES1 cells incubated for 48 hrs by CCK-8 method Cytotoxicity against human GES1 cells incubated for 48 hrs by CCK-8 method	[PMID: 36892076]
HEK-293T	IC₅₀	>50 μM Compound: 39; OY-101	Cytotoxicity against HEK293T cells incubated for 48 hrs by CCK-8 method Cytotoxicity against HEK293T cells incubated for 48 hrs by CCK-8 method	[PMID: 36892076]
HK-2	IC₅₀	>50 μM Compound: 39; OY-101	Cytotoxicity against human HK-2 cells incubated for 48 hrs by CCK-8 method Cytotoxicity against human HK-2 cells incubated for 48 hrs by CCK-8 method	[PMID: 36892076]
LX-2	IC₅₀	>50 μM Compound: 39; OY-101	Cytotoxicity against human LX2 cells incubated for 48 hrs by CCK-8 method Cytotoxicity against human LX2 cells incubated for 48 hrs by CCK-8 method	[PMID: 36892076]

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.

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)
T_max (h)	0.17 ± 0.12	0.38 ± 0.18
C_max (ng/mL)	1573.20 ± 143.97	636.55 ± 355.60
AUC_0-t (ng/mL∗h)	2688.45 ± 180.10	2665.45 ± 450.92
t_1/2 (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

Chemical Information

CAS. Nr. 41183-02-2
Molecular Weight 433.54
Formel C₂₇H₃₁NO₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zeng R, et al. Simplified Derivatives of Tetrandrine as Potent and Specific P-gp Inhibitors to Reverse Multidrug Resistance in Cancer Chemotherapy. J Med Chem. 2023 Mar 23;66(6):4086-4105. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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