JNJ-42041935

Cat. No.: HY-12832 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

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JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pK_i values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.

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

JNJ-42041935 Chemical Structure

CAS No. : 1193383-09-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
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HIF-1α HIF

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

pK_i: 7.91±0.04 (PHD1), 7.29 ±0.05 (PHD2), 7.65±0.09(PHD3)^[1]

In Vitro

JNJ-42041935 is the most potent inhibitor of PHD2_181–417with a pIC₅₀ value of 7.0±0.03. JNJ-42041935 also inhibits full-length PHD1, PHD2, and PHD3 enzymes (pK_i values 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively) ^[1].

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

In Vivo

JNJ-42041935 is used to compare the effect of selective inhibition of PHD to intermittent, high doses (50 μg/kg i.p.) of an exogenous erythropoietin receptor agonist in an inflammation induced anemia model in rats. JNJ-42041935 (100 μmol/kg, once a day for 14 days) is effective in reversing inflammation induced anemia, whereas erythropoietin has no effect. Administration of JNJ-42041935 (100 μmol/kg p.o.) for 5 consecutive days resulted in a 2-fold increase in reticulocytes, an increase in hemoglobin by 2.3 g/dl, and an increase in the hematocrit of 9%. Two hours after oral administration of 300 μmol/kg JNJ-42041935, the bioluminescence over the peritoneal area is increased by 2.2 ± 0.3-fold relative to luciferase-treated vehicle controls in the mouse ^[1].

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

Molecular Weight

346.65

Formula

C₁₂H₆ClF₃N₄O₃

CAS No.

1193383-09-3

Appearance

Solid

Color

White to off-white

SMILES

OC(C(C=N1)=CN1C2=NC3=CC(Cl)=C(OC(F)(F)F)C=C3N2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 36 mg/mL (103.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8848 mL	14.4238 mL	28.8475 mL
5 mM	0.5770 mL	2.8848 mL	5.7695 mL
10 mM	0.2885 mL	1.4424 mL	2.8848 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (248 KB) HNMR (129 KB) LCMS (482 KB)

Handling Instructions (2659 KB)

References

[1]. Barrett TD, et al. Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor. Mol Pharmacol. 2011 [Content Brief]

Kinase Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: JNJ-42041935 is administered at doses of 30, 100, and 300 μmol/kg to Balb/C mice . Plasma is collected 6 h after the dose. Plasma erythropoietin concentration is measured. The hematological effects of JNJ-42041935 are assessed by administering the 100 μmol/kg dose on 5 consecutive days and collecting blood anticoagulated with EDTA on day 8 (3 days after the last dose)^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Barrett TD, et al. Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor. Mol Pharmacol. 2011 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8848 mL	14.4238 mL	28.8475 mL	72.1189 mL
	5 mM	0.5770 mL	2.8848 mL	5.7695 mL	14.4238 mL
	10 mM	0.2885 mL	1.4424 mL	2.8848 mL	7.2119 mL
	15 mM	0.1923 mL	0.9616 mL	1.9232 mL	4.8079 mL
	20 mM	0.1442 mL	0.7212 mL	1.4424 mL	3.6059 mL
	25 mM	0.1154 mL	0.5770 mL	1.1539 mL	2.8848 mL
	30 mM	0.0962 mL	0.4808 mL	0.9616 mL	2.4040 mL
	40 mM	0.0721 mL	0.3606 mL	0.7212 mL	1.8030 mL
	50 mM	0.0577 mL	0.2885 mL	0.5770 mL	1.4424 mL
	60 mM	0.0481 mL	0.2404 mL	0.4808 mL	1.2020 mL
	80 mM	0.0361 mL	0.1803 mL	0.3606 mL	0.9015 mL
	100 mM	0.0288 mL	0.1442 mL	0.2885 mL	0.7212 mL

JNJ-42041935 Related Classifications

Inflammation/Immunology

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:

JNJ-420419351193383-09-3JNJ42041935JNJ 42041935HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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