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JNJ-42041935

Name: JNJ-42041935
Brand: TargetMol
SKU: T3180
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3180Cas No. 1193383-09-3

Alias HIF-PHD Inhibitor II

JNJ-42041935 (HIF-PHD Inhibitor II) is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.

JNJ-42041935

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Purity: 99.95%

Catalog No. T3180Alias HIF-PHD Inhibitor IICas No. 1193383-09-3

JNJ-42041935 (HIF-PHD Inhibitor II) is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
2 mg	$48	In Stock	In Stock
5 mg	$80	In Stock	In Stock
10 mg	$122	In Stock	In Stock
25 mg	$222	In Stock	In Stock
50 mg	$372	In Stock	In Stock
100 mg	$597	In Stock	In Stock
500 mg	$1,260	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$89	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.95%

Color:White

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Product Introduction

Bioactivity

Description	JNJ-42041935 (HIF-PHD Inhibitor II) is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
In vitro	JNJ-42041935 is the most potent inhibitor of PHD2181–417 with a pIC50 value of 7.0±0.03. JNJ-42041935 also inhibits full-length PHD1, PHD2, and PHD3 enzymes (pKi values 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively) [1].
In vivo	JNJ-42041935 has been evaluated for its capability to selectively inhibit prolyl hydroxylase domain (PHD) enzymes compared to the effect of intermittent, high doses (50 μg/kg i.p.) of an erythropoietin receptor agonist in a rat model of inflammation-induced anemia. The study demonstrates that JNJ-42041935, administered at a dose of 100 µmol/kg orally once daily for 14 days, successfully ameliorates inflammation-induced anemia, whereas erythropoietin shows no efficacy. Further, a 5-day consecutive oral administration of JNJ-42041935 at 100 µmol/kg led to a doubling in reticulocyte count, a 2.3 g/dl increase in hemoglobin levels, and a 9% rise in hematocrit values. Additionally, a single oral dose of 300 µmol/kg of JNJ-42041935 resulted in a 2.2 ± 0.3-fold increase in peritoneal bioluminescence, relative to luciferase-treated vehicle controls in mice, indicating enhanced activity two hours post-administration [1].
Kinase Assay	The potency of JNJ-42041935 for inhibition of the structurally related enzyme FIH is assessed by methods similar to those described for PHD2. In brief, activity of FIH is determined using purified glutathione transferase-tagged full-length FIH amino acids 1 to 350 and a synthetic HIF-1α peptide corresponding to residues Asp788 to Leu822. Compounds are preincubated with 17.1 nM FIH for 30 min, followed by a 10-min incubation with 1 μM [2-14C]2-oxoglutarate, in the presence of 10 μM FeNH4SO4 in reaction buffer. The selectivity of JNJ-42041935 for inhibition of a range of other targets available for testing in commercial assays is also assessed at concentrations of 1 and 10 μM[1].
Synonyms	HIF-PHD Inhibitor II

Chemical Properties

Molecular Weight	346.65
Formula	C₁₂H₆ClF₃N₄O₃
Cas No.	1193383-09-3
Smiles	OC(=O)c1cnn(c1)-c1nc2cc(Cl)c(OC(F)(F)F)cc2[nH]1
Relative Density.	1.82 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (144.24 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.77 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8848 mL	14.4238 mL	28.8475 mL	144.2377 mL
5 mM	0.5770 mL	2.8848 mL	5.7695 mL	28.8475 mL
10 mM	0.2885 mL	1.4424 mL	2.8848 mL	14.4238 mL
20 mM	0.1442 mL	0.7212 mL	1.4424 mL	7.2119 mL
50 mM	0.0577 mL	0.2885 mL	0.5770 mL	2.8848 mL
100 mM	0.0288 mL	0.1442 mL	0.2885 mL	1.4424 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc