Art. -Nr.: HY-147017

GSK2556286

(Synonyms: GSK286)

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GSK2556286 (GSK286) is an orally active and cholesterol-dependent Mycobacterium tuberculosis inhibitor. GSK2556286 inhibits Mycobacterium tuberculosis inside infected macrophages (IC₅₀ = 0.07 μM in THP-1 cells), in the presence of cholesterol. GSK2556286 acts via Rv1625c, a membrane-bound adenylyl cyclase in Mycobacterium tuberculosis. GSK2556286 is an Rv1625 agonist leading to increased cAMP and reduced cholesterol metabolism. GSK2556286 can be studied in research for antitubercular purposes.

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Reinheit: 99.70%
CAS. Nr.: 1210456-20-4
Formel: C₁₈H₂₃N₃O₃
Molecular Weight:329.39

Speicherung:

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

GSK2556286 Chemical Structure

CAS. Nr.: 1210456-20-4

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 0.07 μM (human macrophage)^[1]

In Vitro

GSK2556286 requires the presence of cholesterol to demonstrate activity in axenic culture with IC₅₀ of 2.12 and 0.71 μM in H37Rv and Erdman respectively, whilst the IC₅₀ with glucose medium is >125 and >50 μM in H37Rv and Erdman respectively^[2].
GSK2556286 (5 μM, 24 h) increases the intracellular cAMP levels around 50-fold higher in M. tuberculosis lysates than untreated cells only when Rv1625c is expressed^[1].
GSK2556286 (10 μM) reduces the amount of ¹⁴CO₂ released from ¹⁴C-cholesterol by 90% and the propionyl-CoA levels in M. tuberculosis when bacteria cultured in cholesterol media supplemented with acetate^[1].
GSK2556286 (1 nM-10 μM) exhibits decreased MIC in cholesterol media around 10-fold and decreased concertration required to inhibit GFP signal in wild-type M. tuberculosis overexpressing rv1625c^[1].

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

Parmacokinetics

Species	Dose	Route	V_d	T_1/2	Bioavailability	Clearance (CL)
Dog	3 mg/kg	p.o.	2.50 L/kg	1.92 h	51.3 %	23.7 mL/min/kg
Dog	5 mg/kg	i.v.	2.50 L/kg	1.92 h	51.3 %	23.7 mL/min/kg
Mice	1 mg/kg	i.v.	1.76 L/kg	2.47 h	99.0 %	9.02 mL/min/kg
Mice	10 mg/kg	p.o.	1.76 L/kg	2.47 h	99.0 %	9.02 mL/min/kg
Rat	5 mg/kg	i.v.	2.1 L/kg	2.31 h	49.8 %	34.7 mL/min/kg
Rat	5 mg/kg	p.o.	2.1 L/kg	2.31 h	49.8 %	34.7 mL/min/kg

In Vivo

GSK2556286 (0.3-500 mg/kg, p.o, 8 consecutive days) shows greatest effect in acute TB infection mice model receiving 200 mg/kg dosage^[2].
GSK2556286 (10-200 mg/kg, p.o., 5 days per week for 4 weeks) shows a significant bactericidal effect in chronic TB infection BALB/c and C3HeB/FeJ mice model, and the maximal effect is achieved with around 10 mg/kg^[2].
GSK2556286 (50 mg/kg, p.o., one single dose) has increased efficacy when coadministered with Bedaquiline (B) (HY-14881) (25 mg/kg) and Pretomanid (Pa) (HY-10844) (100 mg/kg) in subacute infection model in BALB/c mice^[2].

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

Animal Model:

Subacute infection model in BALB/c mice^[2]
Dosage:

50 mg/kg
Administration:

Oral gavage (p.o.)
Result:

Resulted in significantly lower lung CFU counts when combined with BPa, BL or BPaL.
Was less active when combined with BL or PaL than BPaL.
Resulted in lower proportions of mice relapsing when combined with BPa or BPaL in comparison with RHZ for 4 months.
Associated with significantly more relapses when combined with PaL, and more relapses after 2 months of treatment when combined with BL.

Clinical Trial

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

Chemical Information

CAS. Nr. 1210456-20-4
Appearance Solid
Molecular Weight 329.39
Formel C₁₈H₂₃N₃O₃
Color White to off-white
SMILES

O=C1C=C(CN2CCC(CC2)OC3=CC=CC(C)=C3C)NC(N1)=O
Synonyms

GSK286
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 3.33 mg/mL (10.11 mM; ultrasonic and warming and heat to 60°C; 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

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0359 mL

15.1796 mL

30.3591 mL

5 mM

0.6072 mL

3.0359 mL

6.0718 mL

10 mM

0.3036 mL

1.5180 mL

3.0359 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.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Brown KL, et al., 2023. Cyclic AMP-Mediated Inhibition of Cholesterol Catabolism in Mycobacterium tuberculosis by the Novel Drug Candidate GSK2556286. Antimicrob Agents Chemother 67:e01294-22.

[2]. Nuermberger EL, et al. GSK2556286 Is a Novel Antitubercular Drug Candidate Effective In Vivo with the Potential To Shorten Tuberculosis Treatment. Antimicrob Agents Chemother. 2022 May 24:e0013222. [Content Brief]

[3]. Vladimir Finger, et al., Pyrimidine derivatives with antitubercular activity, European Journal of Medicinal Chemistry, Volume 246, 2023, 114946, ISSN 0223-5234.

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	3.0359 mL	15.1796 mL	30.3591 mL	75.8979 mL
	5 mM	0.6072 mL	3.0359 mL	6.0718 mL	15.1796 mL
	10 mM	0.3036 mL	1.5180 mL	3.0359 mL	7.5898 mL

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GSK2556286

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Antibacterial Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Anti-tuberculosis Compound Library

Macrophage Related Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK2556286

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Antibacterial Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Anti-tuberculosis Compound Library

Macrophage Related Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK2556286 Related Classifications

HY-147017 Related Classifications