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400093

HIF-PHD Inhibitor II, JNJ-42041935

Name: HIF-PHD Inhibitor II, JNJ-42041935
Brand: MM

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.

別名:

HIF-PHD Inhibitor II, JNJ-42041935, 1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, HIF Prolyl Hydroxylase Inhibitor II

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この商品について

実験式（ヒル表記法）:

C₁₂H₆ClF₃N₄O₃

CAS番号:

1193383-09-3

分子量:

346.65

UNSPSC Code:

12352200

NACRES:

NA.28

MDL number:

MFCD28900740

Assay:

≥99% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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特性

Quality Segment

100

assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

ClC1=CC2=C(NC(N3C=C(C=N3)C(O)=O)=N2)C=C1OC(F)(F)F

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

詳細

General description

A 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 (pK_i = 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.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c