Cat. No.: HY-19888

GSK-1482160

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Based on 1 Customer Validation

GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC₅₀s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).

For research use only. We do not sell to patients.

Purity: 98.67%
CAS No.: 1001389-72-5
Formula: C₁₄H₁₄ClF₃N₂O₂
Molecular Weight:334.72

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GSK-1482160 Chemical Structure

CAS No.: 1001389-72-5

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

P2X7 Receptor

All P2X Receptor Isoforms :

All Interleukin Related Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	119.3 nM Compound: 1b; GSK1482160	Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome	[PMID: 31525963]
HEK293	IC₅₀	332.4 nM Compound: 1b; GSK1482160	Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method	[PMID: 31525963]
HEK293	IC₅₀	8.9 nM Compound: GSK1482160	Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay	[PMID: 31005444]

In Vitro

GSK-1482160 (Compound 31) has extremely low clearance rates in both rat and human liver microsomes, and shows no significant inhibition on the major CYP450 subtypes (1A2, 2C9, 2C19, 2D6, 3A4)^[2].

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

Parmacokinetics

Species	Dose	Route	CL	T_1/2	V_ss	T_max	C_max	AUC	F
Rat^[2]	1 mg/kg	i.v.	9 mL/min/kg	1.5 h	1.1 L/kg	/	/	/	/
Rat^[2]	3 mg/kg	p.o.	/	/	/	1.0 h	2.45 μM	13.7 mL/min/kg	65 %

In Vivo

GSK-1482160 (Compound 31) (5-50 mg/kg, p.o., twice daily for 5 days) effectively alleviates rats chronic inflammatory pain^[2].
GSK-1482160 (20 mg/kg, p.o., twice daily for 8 days) significantly reverses mechanical allodynia 1 h post dose on day 1 and this effect was maintained for the duration of the dosing period in the rat chronic constriction injury (CCI) model^[2].

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

Animal Model:

Chronic knee joint inflammatory pain induced by complete Freund's adjuvant (CFA) established in rats^[2]
Dosage:

5, 20 and 50 mg/kg
Administration:

Oral administration (p.o.), twice daily for 5 days
Result:

Exhibited the analgesic effect comparable to that of the Celecoxib (HY-14398) at a dose of 50 mg/kg.

Animal Model:

Neurogenic pain induced by sciatic nerve ligation in rats^[2]
Dosage:

20 mg/kg
Administration:

Oral administration (p.o.), twice daily for 8 days
Result:

Effectively alleviated neuropathic pain, and its effect was comparable to that of Gabapentin (HY-A0057).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1001389-72-5
Appearance Solid
Molecular Weight 334.72
Formula C₁₄H₁₄ClF₃N₂O₂
Color White to off-white
SMILES

O=C([C@H](CC1)N(C)C1=O)NCC2=CC=CC(C(F)(F)F)=C2Cl
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (298.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9876 mL

14.9379 mL

29.8757 mL

5 mM

0.5975 mL

2.9876 mL

5.9751 mL

10 mM

0.2988 mL

1.4938 mL

2.9876 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

References

[1]. Ali Z, et al. Pharmacokinetic and pharmacodynamic profiling of a P2X7 receptor allosteric modulator GSK1482160 in healthy human subjects. Br J Clin Pharmacol. 2013;75(1):197-207. doi:10.1111/j.1365-2125.2012.04320.x

[2]. Abdi MH, et al. Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5080-4. [Content Brief]

[3]. Liu X, et al. Unlocking the therapeutic potential of P2X7 receptor: a comprehensive review of its role in neurodegenerative disorders. Front Pharmacol. 2024 Jul 30;15:1450704. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9876 mL	14.9379 mL	29.8757 mL	74.6893 mL
	5 mM	0.5975 mL	2.9876 mL	5.9751 mL	14.9379 mL
	10 mM	0.2988 mL	1.4938 mL	2.9876 mL	7.4689 mL
	15 mM	0.1992 mL	0.9959 mL	1.9917 mL	4.9793 mL
	20 mM	0.1494 mL	0.7469 mL	1.4938 mL	3.7345 mL
	25 mM	0.1195 mL	0.5975 mL	1.1950 mL	2.9876 mL
	30 mM	0.0996 mL	0.4979 mL	0.9959 mL	2.4896 mL
	40 mM	0.0747 mL	0.3734 mL	0.7469 mL	1.8672 mL
	50 mM	0.0598 mL	0.2988 mL	0.5975 mL	1.4938 mL
	60 mM	0.0498 mL	0.2490 mL	0.4979 mL	1.2448 mL
	80 mM	0.0373 mL	0.1867 mL	0.3734 mL	0.9336 mL
	100 mM	0.0299 mL	0.1494 mL	0.2988 mL	0.7469 mL

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GSK-1482160

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Differentiation Inducing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Ion Channel Compound Library

Allosteric Modulators (AMs) Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

All P2X Receptor Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK-1482160

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Differentiation Inducing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Ion Channel Compound Library

Allosteric Modulators (AMs) Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

All P2X Receptor Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK-1482160 Related Classifications

HY-19888 Related Classifications