PF-03715455

Name: PF-03715455
Brand: MedChemExpress
SKU: HY-18862
Rating: 4.5 (1 reviews)

Cat. No.: HY-18862 Purity: 98.44%: Data Sheet
COA

SDS
Handling Instructions
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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).

For research use only. We do not sell to patients.

PF-03715455 Chemical Structure

CAS No. : 1056164-52-3

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

p38 MAPK p38α p38β MAPK13 p38δ p38γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

p38α

0.88 nM (IC₅₀)

p38β

23 nM (IC₅₀)

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.

Clinical Trial

Molecular Weight

700.27

Formula

C₃₅H₃₄ClN₇O₃S₂

CAS No.

1056164-52-3

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.44%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (251 KB) HNMR (303 KB) LCMS (109 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

PF-03715455 Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-037154551056164-52-3PF03715455PF 03715455p38 MAPKselectivityCOPDLPSTNFαproductioninhaledairwayinflammationInhibitorinhibitorinhibit

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PF-03715455

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PF-03715455 Related Antibodies

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Biological Activity

Purity & Documentation

References

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PF-03715455 Related Antibodies

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Complete Stock Solution Preparation Table

PF-03715455 Related Classifications

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