P-gp inhibitor 1

Name: P-gp inhibitor 1
Brand: MedChemExpress
SKU: HY-101791
Rating: 4.5 (0 reviews)

Art. -Nr.: HY-101791 Reinheit: 98.79%: Data Sheet
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Handling Instructions
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P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

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P-gp inhibitor 1 Chemische Struktur

CAS. Nr. : 2050747-49-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
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•Related Small Molecules:

•Related Proteins:

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Beschreibung

P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

IC₅₀ & Target

P-glycoprotein^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	73.58 μM Compound: 12k	Cytotoxicity against HUVEC assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against HUVEC assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 28355069]
K562	IC₅₀	4 μM Compound: 12k	Cytotoxicity against human K562 cells assessed as suppression of cell viability after 48 hrs by MTT assay Cytotoxicity against human K562 cells assessed as suppression of cell viability after 48 hrs by MTT assay	[PMID: 28355069]
K562/A02	IC₅₀	12.78 μM Compound: 12k	Cytotoxicity against human K562/A02 cells assessed as suppression of cell viability after 48 hrs by MTT assay Cytotoxicity against human K562/A02 cells assessed as suppression of cell viability after 48 hrs by MTT assay	[PMID: 28355069]

In Vitro

P-gp inhibitor 1 (12k) possesses high potency (EC₅₀=57.9±3.5 nM), low cytotoxicity, and long duration of activity in reversing doxorubicin (DOX) resistance in K562/A02 cells (1 μM, 80 minutes)^[1].

P-gp inhibitor 1 also boosts the potency of other MDR-related cytotoxic agents with different structures, increases accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity in K562/A02 MDR cells (0.1, 1, 5 μM, 1 hour)^[1].

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

Western Blot Analysis^[1]

Cell Line:	K562/A02 cell
Concentration:	0.1, 0.5, or 2.0 μM
Incubation Time:	72 hours
Result:	MDR reversal by 12k was not caused by a decreased protein expression but instead most likely due to direct inhibition of P-gp efflux^[1].

Molekulargewicht

517.62

Formel

C₃₂H₃₁N₅O₂

CAS. Nr.

2050747-49-2

Appearance

Solid

Color

Light yellow to brown

SMILES

COC(C(OC)=C1)=CC2=C1CCN(C2)CCC3=CC=C(NC4=NC(C5=CC=NC=C5)=NC6=CC=CC=C46)C=C3

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 16.67 mg/mL (32.21 mM; ultrasonic and warming and heat to 70°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9319 mL	9.6596 mL	19.3192 mL
5 mM	0.3864 mL	1.9319 mL	3.8638 mL
10 mM	0.1932 mL	0.9660 mL	1.9319 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner
Verdünnungsrechner

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Reinheit & Dokumentation

Purity: 98.79%

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Data Sheet (273 KB) SDS (251 KB)

COA (249 KB) HNMR (264 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Qiu Q, et al. Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. J Med Chem. 2017 Apr 27;60(8):3289-3302. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9319 mL	9.6596 mL	19.3192 mL	48.2980 mL
	5 mM	0.3864 mL	1.9319 mL	3.8638 mL	9.6596 mL
	10 mM	0.1932 mL	0.9660 mL	1.9319 mL	4.8298 mL
	15 mM	0.1288 mL	0.6440 mL	1.2879 mL	3.2199 mL
	20 mM	0.0966 mL	0.4830 mL	0.9660 mL	2.4149 mL
	25 mM	0.0773 mL	0.3864 mL	0.7728 mL	1.9319 mL
	30 mM	0.0644 mL	0.3220 mL	0.6440 mL	1.6099 mL

P-gp inhibitor 1 Related Classifications

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:

P-gp inhibitor 12050747-49-2P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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P-gp inhibitor 1

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Other Forms of P-gp inhibitor 1:

P-gp inhibitor 1 Related Antibodies

Spezialitätsempfehlungen

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•Related Small Molecules:

•Related Proteins:

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P-gp inhibitor 1 Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

P-gp inhibitor 1 Related Classifications

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