JNJ-42041935

SKU: orb1304454

Description

JNJ-42041935

Research Area

Epigenetics & Chromatin, Metabolism Research

Key Properties

• CAS Number: 1193383-09-3
• MW: 346.65
• Purity: >99.99% (May vary between batches)
• Formula: C₁₂H₆ClF₃N₄O₃
• SMILES: OC(=O)c1cnn(c1)-c1nc2cc(Cl)c(OC(F)(F)F)cc2[nH]1
• Target: HIF/HIF Prolyl-Hydroxylase
• Solubility: DMSO:50 mg/mL (144.24 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.77 mM)

Bioactivity

• 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 .
• 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) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Hypoxia-inducible factors, HIF-PH, HIF/HIFProlylHydroxylase, HIF/HIF ProlylHydroxylase, HIF/HIF Prolyl-Hydroxylase, HIF Prolyl-Hydroxylase, HIF ProlylHydroxylase, HIF-PHD Inhibitor II, HIFProlylHydroxylase, HIFs, HIF, JNJ-42041935, JNJ42041935, JNJ 42041935, inhibit, Inhibitor, PHD1, PHD2, PHD3

Compound Identifiers

PubChem CID

45102710