Art. -Nr.: HY-16715

Copy Link Print Information

Acumapimod

(Synonyms: BCT197)

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC₅₀ of less than 1 μM for p38α.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.68%
CAS. Nr.: 836683-15-9
Formel: C₂₂H₁₉N₅O₂
Molecular Weight:385.42

Speicherung:

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

Acumapimod Chemical Structure

CAS. Nr.: 836683-15-9

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC₅₀ of less than 1 μM for p38α.

IC₅₀ & Target

IC50: less than 1 μM (p38α)^[1]

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

In Vitro

Acumapimod is an inhibitor of p38α with an IC₅₀ value of less than 1 μM.

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

In Vivo

Acumapimod is an oral low-molecular-weight p38 inhibitor currently in development for the treatment of several inflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-term dosing of Acumapimod (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients^[2].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 836683-15-9
Appearance Solid
Molecular Weight 385.42
Formel C₂₂H₁₉N₅O₂
Color White to off-white
SMILES

O=C(NC1CC1)C2=CC=C(C)C(N3N=CC(C(C4=CC=CC(C#N)=C4)=O)=C3N)=C2
Synonyms

BCT197
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (1)

All

Sort by:

Journal Impact Factor

J Pharmacol Exp Ther

Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. [Abstract]

2019 Aug;370(2):219-230. PMID: 31189728

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (129.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.5946 mL

12.9729 mL

25.9457 mL

5 mM

0.5189 mL

2.5946 mL

5.1891 mL

10 mM

0.2595 mL

1.2973 mL

2.5946 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (781 KB)
- English - EN (781 KB)
- Français - FR (781 KB)
- Deutsch - DE (781 KB)
- Norwegian - NO (781 KB)
- Español - ES (781 KB)
- Swedish - SV (781 KB)
- Italian - IT (781 KB)
- Korean - KR (781 KB)
- Portuguese - PT (781 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)
Handling Instructions (2659 KB)

Verweise

[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]. De Buck S, et al. Population PK-PD Model for Tolerance Evaluation to the p38 MAP Kinase Inhibitor BCT197. CPT Pharmacometrics Syst Pharmacol. 2015 Dec;4(12):691-700. [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, 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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5946 mL	12.9729 mL	25.9457 mL	64.8643 mL
	5 mM	0.5189 mL	2.5946 mL	5.1891 mL	12.9729 mL
	10 mM	0.2595 mL	1.2973 mL	2.5946 mL	6.4864 mL
	15 mM	0.1730 mL	0.8649 mL	1.7297 mL	4.3243 mL
	20 mM	0.1297 mL	0.6486 mL	1.2973 mL	3.2432 mL
	25 mM	0.1038 mL	0.5189 mL	1.0378 mL	2.5946 mL
	30 mM	0.0865 mL	0.4324 mL	0.8649 mL	2.1621 mL
	40 mM	0.0649 mL	0.3243 mL	0.6486 mL	1.6216 mL
	50 mM	0.0519 mL	0.2595 mL	0.5189 mL	1.2973 mL
	60 mM	0.0432 mL	0.2162 mL	0.4324 mL	1.0811 mL
	80 mM	0.0324 mL	0.1622 mL	0.3243 mL	0.8108 mL
	100 mM	0.0259 mL	0.1297 mL	0.2595 mL	0.6486 mL

Keywords

Acumapimod

1 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Acumapimod

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Clinical Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Acumapimod

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Acumapimod Related Classifications

HY-16715 Related Classifications