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400093 HIF-PHD Inhibitor II, JNJ-42041935 - CAS 1193383-09-3 - Calbiochem

The HIF-PHD Inhibitor II, JNJ-42041935 controls the biological activity of HIF-PHD. This small molecule/inhibitor is primarily used for Cell Structure applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, HIF Prolyl Hydroxylase Inhibitor II

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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1193383-09-3C₁₂H₆ClF₃N₄O₃

Products

Catalog NumberPackaging Qty/Pack
400093-10MG Glass bottle 10 mg
Description
OverviewA cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg). Shown to inhibit malate dehydrogenase 2 (MDH2) activity and suppress mitochondrial respiration.
Catalogue Number400093
Brand Family Calbiochem®
Synonyms1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, HIF Prolyl Hydroxylase Inhibitor II
References
ReferencesLee, K., et al., 2013. Angew. Chem. Int. Ed. 52, In press.
Barrett, T.D., et al. 2011. Mol. Pharmacol. 79, 910.
Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.
Product Information
CAS number1193383-09-3
FormWhite solid
Hill FormulaC₁₂H₆ClF₃N₄O₃
Chemical formulaC₁₂H₆ClF₃N₄O₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥99% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
400093-10MG 04055977212402

Documentation

HIF-PHD Inhibitor II, JNJ-42041935 - CAS 1193383-09-3 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

HIF-PHD Inhibitor II, JNJ-42041935 - CAS 1193383-09-3 - Calbiochem Certificates of Analysis

TitleLot Number
400093

References

Reference overview
Lee, K., et al., 2013. Angew. Chem. Int. Ed. 52, In press.
Barrett, T.D., et al. 2011. Mol. Pharmacol. 79, 910.
Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision31-August-2012 JSW
Synonyms1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, HIF Prolyl Hydroxylase Inhibitor II
DescriptionA cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg).
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1193383-09-3
Chemical formulaC₁₂H₆ClF₃N₄O₃
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesLee, K., et al., 2013. Angew. Chem. Int. Ed. 52, In press.
Barrett, T.D., et al. 2011. Mol. Pharmacol. 79, 910.
Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.