Referencia número: HY-18862

PF-03715455

Revisión del cliente

Based on 1 Customer Validation

PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC₅₀ values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC₅₀=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease).

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Pureza: 98.44%
No. CAS: 1056164-52-3
Fòrmula: C₃₅H₃₄ClN₇O₃S₂
Peso molecular:700.27

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-03715455 Chemical Structure

No. CAS: 1056164-52-3

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Amount: USD 0.00

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

p38α

0.88 nM (IC₅₀)

p38β

23 nM (IC₅₀)

Ver todos los productos específicos de isoformas p38 MAPK :

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	0.88 nM Compound: 1ab, PF-03715455	Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha preincubated for 40 mins prior to LPS-challenge by ELISA in the presence of 5 uM ATP Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha preincubated for 40 mins prior to LPS-challenge by ELISA in the presence of 5 uM ATP	[PMID: 21888439]
PBMC	IC₅₀	1.7 nM Compound: 1ab, PF-03715455	Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA	[PMID: 21888439]
PBMC	IC₅₀	8 nM Compound: PF-3715455	Inhibition of LPS-stimulated TNFalpha release in human PBMC cells preincubated for 1 hr followed by LPS stimulation and measured after 18 hrs Inhibition of LPS-stimulated TNFalpha release in human PBMC cells preincubated for 1 hr followed by LPS stimulation and measured after 18 hrs	[PMID: 35546685]

In Vitro

PF-03715455 is a moderate inhibitor of CYP1A2, CYP2C19, and CYP2D6 and a potent inhibitor of CYP’s 2C9 and CYP3A4^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-03715455 treatment shows that the V_ss and T_1/2 are 0.19 L/kg, 1 hour, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male CD Sprague Dawley rats (300-450 g)^[2]
Dosage:

1 mg/kg
Administration:

I.v. (Pharmacokinetic Analysis)
Result:

The V_ss, and T_1/2 were 0.19 L/kg, 1 hour, respectively.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1056164-52-3
Appearance Solid
Peso molecular 700.27
Fòrmula C₃₅H₃₄ClN₇O₃S₂
Color White to off-white
SMILES

CC(C)(C1=NN(C2=CC=C(O)C(Cl)=C2)C(NC(NCC3=CC=CC=C3SC4=CN5C(C6=CC=CC=C6SCCO)=NN=C5C=C4)=O)=C1)C
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (71.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4280 mL

7.1401 mL

14.2802 mL

5 mM

0.2856 mL

1.4280 mL

2.8560 mL

10 mM

0.1428 mL

0.7140 mL

1.4280 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Norman P, et al. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92. [Content Brief]

[2]. Millan DS, et al. Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. J Med Chem. 2011 Nov 24;54(22):7797-814. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4280 mL	7.1401 mL	14.2802 mL	35.7005 mL
	5 mM	0.2856 mL	1.4280 mL	2.8560 mL	7.1401 mL
	10 mM	0.1428 mL	0.7140 mL	1.4280 mL	3.5701 mL
	15 mM	0.0952 mL	0.4760 mL	0.9520 mL	2.3800 mL
	20 mM	0.0714 mL	0.3570 mL	0.7140 mL	1.7850 mL
	25 mM	0.0571 mL	0.2856 mL	0.5712 mL	1.4280 mL
	30 mM	0.0476 mL	0.2380 mL	0.4760 mL	1.1900 mL
	40 mM	0.0357 mL	0.1785 mL	0.3570 mL	0.8925 mL
	50 mM	0.0286 mL	0.1428 mL	0.2856 mL	0.7140 mL
	60 mM	0.0238 mL	0.1190 mL	0.2380 mL	0.5950 mL

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PF-03715455

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Ver todos los productos específicos de isoformas p38 MAPK

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PF-03715455 Related Classifications

HY-18862 Related Classifications