2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. GSK360A

GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .

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

GSK360A Chemical Structure

GSK360A Chemical Structure

CAS No. : 931399-19-8

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Based on 1 publication(s) in Google Scholar

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Description

GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) [1].

In Vivo

GSK360A (30 mg/kg i.g.) improves long-term ventricular function, remodeling, and vascularity in a model of established ventricular dysfunction[1].

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

Animal Model: male Lewis rats with ventricular dysfunction model[1]
Dosage: 30 mg/kg
Administration: oral gavage
Result: Increased circulating levels of erythropoietin and hemoglobin and hemoxygenase-1 expression in the heart and skeletal muscle of male rats.
Molecular Weight

348.33

Formula

C17H17FN2O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CNC(C1=C(C2=C(C=CC(F)=C2)N(C1=O)CCC3CC3)O)=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (5.74 mM; Need ultrasonic and warming; 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 2.8708 mL 14.3542 mL 28.7084 mL
5 mM 0.5742 mL 2.8708 mL 5.7417 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.90%

COA (249 KB)

Handling Instructions (2659 KB)
References

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 (sealed storage, away from moisture). 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 2.8708 mL 14.3542 mL 28.7084 mL 71.7710 mL
5 mM 0.5742 mL 2.8708 mL 5.7417 mL 14.3542 mL
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GSK360A 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:

GSK360A931399-19-8HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHHIF-1 alphafailing heartmyocardial infarctionInhibitorinhibitorinhibit

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