Acumapimod | BCT-197 | CAS#836683-15-9 | p38MAP inhibitor

MedKoo Cat#: 319515 | Name: Acumapimod (BCT-197)

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Acumapimod, also known as BCT-197, is a potent P38 mitogen-activated protein kinase inhibitor. The p38 protein kinases, in particular p38α and p38β, regulate the production of multiple inflammatory mediators.

Chemical Structure

Acumapimod (BCT-197)

CAS#836683-15-9

Theoretical Analysis

MedKoo Cat#: 319515

Name: Acumapimod (BCT-197)

CAS#: 836683-15-9

Chemical Formula: C22H19N5O2

Exact Mass: 385.1539

Molecular Weight: 385.43

Elemental Analysis: C, 68.56; H, 4.97; N, 18.17; O, 8.30

Price and Availability

Size	Price	Availability
10mg	USD 110.00	Ready to ship
25mg	USD 220.00	Ready to ship
50mg	USD 385.00	Ready to ship
100mg	USD 685.00	Ready to ship
200mg	USD 1,150.00	Ready to ship
500mg	USD 2,450.00	Ready to ship

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Related CAS #

No Data

Synonym

BCT-197; BCT197; BCT 197; BCT197A2201; Acumapimod

IUPAC/Chemical Name

3-(5-amino-4-(3-cyanobenzoyl)-1H-pyrazol-1-yl)-N-cyclopropyl-4-methylbenzamide

InChi Key

VGUSQKZDZHAAEE-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H19N5O2/c1-13-5-6-16(22(29)26-17-7-8-17)10-19(13)27-21(24)18(12-25-27)20(28)15-4-2-3-14(9-15)11-23/h2-6,9-10,12,17H,7-8,24H2,1H3,(H,26,29)

SMILES Code

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

Appearance

Yellow to orange solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#YXM61212

QC Data

View QC data: current batch, Lot#YXM61212

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

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

In vitro activity:

N/A

In vivo activity:

All vehicle-treated animals were removed from study and euthanized by day 9 due to ≥25 % body weight loss (Fig. 2). Compared to vehicle, a protective effect was observed with 31 % (5/16) of the 6 mg kg−1 BCT197, 67 % (10/15) dexamethasone and 94 % (15/16) oseltamivir-treated animals surviving to the end of study. However, only 12.5 % (2/16) survival was observed in the 18 mg kg−1 BCT197 group (Fig. 2b). All of the curves were statistically significantly different from vehicle (P<0.0125, using Bonferroni correction for multiple comparisons as part of the Kaplan–Meier analysis). Reference: J Med Microbiol. 2018 Mar;67(3):452-462. https://pubmed.ncbi.nlm.nih.gov/29458547/

	Solvent	mg/mL	mM
Solubility
	DMSO	50.0	129.73

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 385.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Growcott EJ, Bamba D, Galarneau JR, Leonard VHJ, Schul W, Stein D, Osborne CS. The effect of P38 MAP kinase inhibition in a mouse model of influenza. J Med Microbiol. 2018 Mar;67(3):452-462. doi: 10.1099/jmm.0.000684. Epub 2018 Jan 24. PMID: 29458547. 2. Parkin JM, Hardaker EL. Effects of Acumapimod (PCT197), an Oral p38 Inhibitor, on Tobacco Smoke and Lipopolysaccharide-Induced Lung Inflammation in a Corticosteroid-Resistant Rat Model. Am J Respir Crit Care Med. 2017 May;195:A6305.

In vitro protocol:

N/A

In vivo protocol:

1: Agyemang A, Farrell C, Moore W, Parkin J. A Physiologically Based Pharmacokinetic Model to Predict Potential Drug-Drug Interactions and Inform Dosing of Acumapimod, an Oral p38 MAPK Inhibitor. CPT Pharmacometrics Syst Pharmacol. 2021 Jan;10(1):30-39. doi: 10.1002/psp4.12565. Epub 2020 Dec 30. PMID: 33107218; PMCID: PMC7825188. 2: Strâmbu IR, Kobalava ZD, Magnusson BP, MacKinnon A, Parkin JM. Phase II Study of Single/Repeated Doses of Acumapimod (BCT197) to Treat Acute Exacerbations of COPD. COPD. 2019 Dec;16(5-6):344-353. doi: 10.1080/15412555.2019.1682535. Epub 2019 Nov 4. PMID: 31682162. 3: Norman P. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92. doi: 10.1517/13543784.2015.1006358. Epub 2015 Jan 20. PMID: 25599809.