TP0463518

TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively.

TP0463518 Chemical Structure

TP0463518 Chemical Structure

CAS No. 1558021-37-6

Purity & Quality Control

Batch: S072901 DMSO]40 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 98.66%
98.66

TP0463518 Related Products

Signaling Pathway

Biological Activity

Description TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively.
Targets
hPHD2 [1]
(Cell-free assay)
hPHD1 [1]
(Cell-free assay)
monkey PHD2 [1]
(Cell-free assay)
hPHD3 [1]
(Cell-free assay)
5.3 nM(Ki) 18 nM 22 nM 63 nM

Chemical Information & Solubility

Molecular Weight 431.83 Formula

C20H18ClN3O6

CAS No. 1558021-37-6 SDF --
Smiles C1CN(C(=O)C(=C1O)C(=O)NCC(=O)O)CC2=CN=C(C=C2)OC3=CC=C(C=C3)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 40 mg/mL ( (92.62 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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