Pamapimod (Synonyms: Ro4402257; R1503)

Name: Pamapimod
Brand: MedChemExpress
SKU: HY-10405
Rating: 4.5 (1 reviews)

Cat. No.: HY-10405 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

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Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC₅₀s of 14 nM and 480 nM and K_is of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.

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

Pamapimod Chemical Structure

CAS No. : 449811-01-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 165	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 165	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 768	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Pamapimod:

Pamapimod-d₄ Get quote

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View All p38 MAPK Isoform Specific Products:

View All Isoforms

p38 MAPK p38α p38β MAPK13 p38δ p38γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

p38α

14 nM (IC₅₀)

p38α

1.3 nM (Ki)

p38β

480 (IC₅₀)

p38β

120 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 30 μM Compound: 5	Cytotoxicity against HEK293 after 24 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against HEK293 after 24 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 26704265]
THP-1	IC₅₀	0.025 μM Compound: 2b, Pamapimod	Inhibition of LPS-induced TNFalpha production in human THP1 cells after 2 hrs by ELISA Inhibition of LPS-induced TNFalpha production in human THP1 cells after 2 hrs by ELISA	[PMID: 21375264]
THP-1	IC₅₀	25 nM Compound: 1	Inhibition of LPS-induced TNFalpha production in human THP1 cells by ELISA Inhibition of LPS-induced TNFalpha production in human THP1 cells by ELISA	[PMID: 19950901]

In Vitro

Pamapimod binds to JNK kinases with K_i values of 190 nM, 16 nM and 19 nM for Jnk1, Jnk2 and Jnk3, respectively^[1].
After lipopolysaccharide (LPS) stimulation of the human myelomonocytic cell line (THP-1), secretion of TNF-α is inhibited by Pamapimod, with an EC₅₀ of 25 nM. Pamapimod suppresses TNF-α and IL-1β production in whole blood, with EC₅₀ values of 0.40 and 0.10 μM, respectively^[1].

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

In Vivo

Pamapimod (0-150 mg/kg; oral gavage; once daily; DBA/1J female mice) treatment reduces inflammation and bone loss in murine collagen-induced arthritis^[1].

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

Animal Model:	DBA/1J female mice (8-10 weeks of age) induced murine collagen^[1]
Dosage:	0 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 90 mg/kg, 150 mg/kg
Administration:	Oral gavage; once daily
Result:	Reduced inflammation and bone loss.

Molecular Weight

406.38

Formula

C₁₉H₂₀F₂N₄O₄

CAS No.

449811-01-2

Appearance

Solid

Color

White to off-white

SMILES

O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 34 mg/mL (83.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4608 mL	12.3038 mL	24.6075 mL
5 mM	0.4922 mL	2.4608 mL	4.9215 mL
10 mM	0.2461 mL	1.2304 mL	2.4608 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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)

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (247 KB) LCMS (123 KB)

Handling Instructions (2659 KB)

References

[1]. Hill, R. J. et al. Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity. The Journal of pharmacology and experimental therapeutics 327, 610-619, doi:10.1124/jpet.108.139006 (2008). [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4608 mL	12.3038 mL	24.6075 mL	61.5188 mL
	5 mM	0.4922 mL	2.4608 mL	4.9215 mL	12.3038 mL
	10 mM	0.2461 mL	1.2304 mL	2.4608 mL	6.1519 mL
	15 mM	0.1641 mL	0.8203 mL	1.6405 mL	4.1013 mL
	20 mM	0.1230 mL	0.6152 mL	1.2304 mL	3.0759 mL
	25 mM	0.0984 mL	0.4922 mL	0.9843 mL	2.4608 mL
	30 mM	0.0820 mL	0.4101 mL	0.8203 mL	2.0506 mL
	40 mM	0.0615 mL	0.3076 mL	0.6152 mL	1.5380 mL
	50 mM	0.0492 mL	0.2461 mL	0.4922 mL	1.2304 mL
	60 mM	0.0410 mL	0.2051 mL	0.4101 mL	1.0253 mL
	80 mM	0.0308 mL	0.1538 mL	0.3076 mL	0.7690 mL

Pamapimod 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.

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Pamapimod (Synonyms: Ro4402257; R1503)

Customer Review

Other Forms of Pamapimod:

Pamapimod Related Antibodies

Featured Recommendations

•Related Screening Libraries:

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•Related Proteins:

View All p38 MAPK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Pamapimod Related Antibodies

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Complete Stock Solution Preparation Table

Pamapimod Related Classifications

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