p38 MAPK-IN-1

Name: p38 MAPK-IN-1
Brand: MedChemExpress
SKU: HY-12839
Rating: 5.0 (11 reviews)

Cat. No.: HY-12839 Purity: 99.58%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC₅₀ of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.

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

p38 MAPK-IN-1 Chemical Structure

CAS No. : 1006378-90-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 462	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 462	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2520	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

11 Publications Citing Use of MCE p38 MAPK-IN-1

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC₅₀ of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.

IC₅₀ & Target^[1]

p38 MAPK

68 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	IC₅₀	187 nM Compound: 4	Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production after 5 hrs by ELISA method Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production after 5 hrs by ELISA method	[PMID: 21999461]

In Vivo

p38 MAPK-IN-1 (Compound 4; 1 mg/kg for iv and 10 mg/kg for po) has a t_1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a C_max of 5.3 μM for po in male wistar rats^[1].
p38 MAPK-IN-1 dose-dependently inhibits TNFα production with an ED₅₀ of 0.5 mg/kg^[1].

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

Animal Model:	Male wistar rats^[1]
Dosage:	10 mg/kg for po and 1 mg/kg for iv (Pharmacokinetic Analysis)
Administration:	Po and iv
Result:	Had a t_1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a C_max of 5.3 μM for po.

Molecular Weight

349.35

Formula

C₂₁H₁₅F₂N₂O

CAS No.

1006378-90-0

Appearance

Solid

Color

Off-white to yellow

SMILES

FC1=CC(F)=C(C2=CC=NC(C2=CC=[NH+]3[O-])=C3C4=C(C)C=CC=C4)C=C1

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 : 33.33 mg/mL (95.41 mM; ultrasonic and warming and heat to 60°C; 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	2.8625 mL	14.3123 mL	28.6246 mL
5 mM	0.5725 mL	2.8625 mL	5.7249 mL
10 mM	0.2862 mL	1.4312 mL	2.8625 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.

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (2.38 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (2.38 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.83 mg/mL (2.38 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.58%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (250 KB) LCMS (104 KB)

Handling Instructions (2659 KB)

References

[1]. Lumeras W, et al. 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. J Med Chem. 2011 Nov 24;54(22):7899-910. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8625 mL	14.3123 mL	28.6246 mL	71.5615 mL
	5 mM	0.5725 mL	2.8625 mL	5.7249 mL	14.3123 mL
	10 mM	0.2862 mL	1.4312 mL	2.8625 mL	7.1561 mL
	15 mM	0.1908 mL	0.9542 mL	1.9083 mL	4.7708 mL
	20 mM	0.1431 mL	0.7156 mL	1.4312 mL	3.5781 mL
	25 mM	0.1145 mL	0.5725 mL	1.1450 mL	2.8625 mL
	30 mM	0.0954 mL	0.4771 mL	0.9542 mL	2.3854 mL
	40 mM	0.0716 mL	0.3578 mL	0.7156 mL	1.7890 mL
	50 mM	0.0572 mL	0.2862 mL	0.5725 mL	1.4312 mL
	60 mM	0.0477 mL	0.2385 mL	0.4771 mL	1.1927 mL
	80 mM	0.0358 mL	0.1789 mL	0.3578 mL	0.8945 mL

p38 MAPK-IN-1 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:

p38 MAPK-IN-11006378-90-0p38 MAPKAutophagysustainedlevelslowclearancebioavailabilityInhibitorinhibitorinhibit

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p38 MAPK-IN-1

Customer Review

p38 MAPK-IN-1 Related Antibodies

11 Publications Citing Use of MCE p38 MAPK-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All p38 MAPK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

p38 MAPK-IN-1 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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