PH-797804
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $850 | Check With Us |
| 1g | $1350 | Check With Us |
| 5g | $3415 | Check With Us |
: Cat #: V0481 CAS #: 586379-66-0 Purity ≥ 98%
Description: PH-797804 (PH797804), a diarylpyridinone analog, is a novel, potent, selective and ATP-competitive inhibitor of p38 mitogen-activated protein (p38α) with potential anti-inflammatory and anticancer activity.
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- Related Biological Data
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| Molecular Weight (MW) | 477.3 |
|---|---|
| Molecular Formula | C22H19BrF2N2O3 |
| CAS No. | 586379-66-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 96 mg/mL (201.1 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 7 mg/mL (14.7mM) | |
| Solubility In Vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL |
| SMILES Code | O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1 |
| Synonyms | Synonym: PH 797804; PH797804; PH-797804. |
| Protocol | In Vitro | PH-797804 blocks LPS-induced TNF-α production and p38 kinase activity in the human monocytic U937 cell line, with comparable IC50 of 5.9 nM and 1.1 nM. PH-797804 has no inhibitory effect on either the JNK pathway (c-Jun phosphorylation) or ERK pathway (ERK phosphorylation) in U937 cells at concentrations up to 1 μM. PH-797804 inhibits RANKL- and M-CSF-induced osteoclast formation in a concentration-dependent manner, with IC50 of 3 nM in primary rat bone marrow cells. |
|---|---|---|
| In Vivo | Orally dosing of PH-797804 effectively inhibits acute inflammatory responses induced by systemically administered endotoxin in both rat and cynomolgus monkeys. PH-797804 treatment for 10 days demonstrates robust anti-inflammatory activity in chronic disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and mouse collagen-induced arthritis. Dose-response analysis resulted in ED50 values of 0.07 mg/kg and 0.095 mg/kg in rat and cynomolgus monkeys, respectively. PH-797804 inhibits LPS-induced TNF-α, IL-6, and MK-2 activity in a dose- and concentration-dependent manner in a human endotoxin challenge model. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0951 mL | 10.4756 mL | 20.9512 mL | 41.9024 mL |
| 5mM | 0.4190 mL | 2.0951 mL | 4.1902 mL | 8.3805 mL |
| 10mM | 0.2095 mL | 1.0476 mL | 2.0951 mL | 4.1902 mL |
| 20mM | 0.1048 mL | 0.5238 mL | 1.0476 mL | 2.0951 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.