Org 48762-0

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Cat.No. 6014 - Org 48762-0 | C24H16F2N4 | CAS No. 755753-89-0
Description: Selective p38α/β inhibitor; orally bioavailable
Chemical Name: 4,6-Bis(4-fluorophenyl)-2-methyl-5-(4-pyridinyl)-2H-pyrazolo[3,4-b]pyridine
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

Selective p38α and β kinase inhibitor (EC50 = 0.1 μM for p38α). Selective for p38α/β over a panel of 48 other human kinases. Inhibits LPS-induced TNFα release from PBMCs. Also inhibits cytokine release in an LPS-induced endotoxemia model in mice. Orally bioavailable.

Technical Data

M. Wt 398.41
Formula C24H16F2N4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 755753-89-0
PubChem ID 24822135
InChI Key VMAKTIDYMSNPOV-UHFFFAOYSA-N
Smiles CN1C=C2C(N=C(C(C3=CC=NC=C3)=C2C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 19.92 50
DMSO 39.84 100
ethanol 39.84 100

Preparing Stock Solutions

The following data is based on the product molecular weight 398.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.51 mL 12.55 mL 25.1 mL
5 mM 0.5 mL 2.51 mL 5.02 mL
10 mM 0.25 mL 1.25 mL 2.51 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Mihara et al (2008) A potent and selective p38 inhibitor protects against bone damage in murine collagen-induced arthritis: a comparison with neutralization of mouse TNFalpha. Br.J.Pharmacol. 154 153 PMID: 8297096


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Keywords: Org 48762-0, supplier, Org48762-0, MAPK, mitogen-activated, protein, kinases, inhibitors, inhibits, p38, α, β, alpha, beta, selective, orally, bioavailable, p38, p38, Tocris Bioscience

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Pathways for Org 48762-0

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.