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JNJ-42041935

Cat. No. M8963
JNJ-42041935 Structure
Size Price Availability Quantity
5mg USD 135 In stock
10mg USD 210 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

JNJ-42041935 was the most potent inhibitor of PHD2181–417 with a pIC50 value of 7.0 ± 0.03. JNJ-42041935 caused a concentration-dependent elevation of cellular HIF-1α and erythropoietin release in Hep3B cells. JNJ-42041935 (100 μmol/kg, once a day for 14 days) was effective in reversing inflammation-induced anemia.

Protocol
Cell Experiment
Cell lines Hep3B cells
Preparation method The potency of compounds for stabilization of intracellular HIF-1α and release of erythropoietin into the media was assessed in the human hepatoma cell line Hep3B. Cells were cultured in Dulbecco's modified Eagle's medium/high glucose (Invitrogen) supplemented with 10% fetal calf serum and 2 mM l-glutamine, 1% nonessential amino acids, 1 mM sodium pyruvate, 50 IU/ml penicillin, and 50 μg/ml streptomycin. A range of concentrations was incubated in 96-well plates with 30,000 cells/well for 24 h. Incubation media were collected, and cells were subsequently lysed for assessment of cellular HIF-1α content and erythropoietin concentration.
Concentrations 1 to 10 μM
Incubation time 24 h
Animal Experiment
Animal models Balb/C mice
Formulation
Dosages 30, 100, and 300 μmol/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 346.65
Formula C12H6ClF3N4O3
CAS Number 1193383-09-3
Purity >98%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

A role for prolyl hydroxylase domain proteins in hippocampal synaptic plasticity.
Corcoran A, et al. Hippocampus. 2013 Oct;23(10):861-72. PMID: 23674383.

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.
Barrett TD, et al. Mol Pharmacol. 2011 Jun;79(6):910-20. PMID: 21372172.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: JNJ-42041935 supplier, HIF, inhibitors

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