JNJ-42041935 - 99%, high purity , CAS No.1193383-09-3

  • ≥99%
Item Number
J646612
Grouped product items
SKUSizeAvailabilityPrice Qty
J646612-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$100.90
J646612-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$150.90
J646612-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$450.90
J646612-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$720.90

Basic Description

SynonymsAZACITIDINE (USP-RS) | 1-[6-chloro-5-(trifluoromethoxy)-1H-1,3-benzodiazol-2-yl]-1H-pyrazole-4-carboxylic acid | 1H-Pyrazole-4-carboxylic acid, 1-(6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl)- | CS-4216 | Q27289665 | BDBM50446900 | BS-14602 | JNJ42
Specifications & Purity≥99%
Biochemical and Physiological MechanismsJNJ-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.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

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.

In Vitro

JNJ-42041935 is the most potent inhibitor of PHD2 181–417 with a pIC 50 value of 7.0±0.03. JNJ-42041935 also inhibits full-length PHD1, PHD2, and\nPHD3 enzymes (pK i values 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively). 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:pK i : 7.91±0.04 (PHD1), 7.29 ±0.05 (PHD2), 7.65±0.09(PHD3)

Associated Targets(Human)

EGLN1 Tclin Egl nine homolog 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EGLN1 Tclin Egl nine homolog 1 (1702 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]pyrazole-4-carboxylic acid
INCHI InChI=1S/C12H6ClF3N4O3/c13-6-1-7-8(2-9(6)23-12(14,15)16)19-11(18-7)20-4-5(3-17-20)10(21)22/h1-4H,(H,18,19)(H,21,22)
InChi Key FXHHASJVTYRJHH-UHFFFAOYSA-N
Canonical SMILES C1=C2C(=CC(=C1Cl)OC(F)(F)F)N=C(N2)N3C=C(C=N3)C(=O)O
Isomeric SMILES C1=C2C(=CC(=C1Cl)OC(F)(F)F)N=C(N2)N3C=C(C=N3)C(=O)O
PubChem CID 45102710
Molecular Weight 346.65

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : ≥ 36 mg/mL (103.85 mM)

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