Dilmapimod
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MedKoo CAT#: 205999

CAS#: 444606-18-2 (free base)

Description: Dilmapimod, also known as SB-681323 and GW-681323 , is p38 MAPK inhibitor. SB-681323 inhibited the p38 MAPK pathway to a greater degree than prednisolone did. SB-681323 inhibited TNF-alpha production. SB-681323 is a potent p38 MAPK inhibitor that potentially suppresses inflammation in COPD. The treatment with SB-681832 is a safe and effective means of reducing hsCRP in patients undergoing elective PCI.

Chemical Structure

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Dilmapimod
CAS# 444606-18-2 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 205999
Name: Dilmapimod
CAS#: 444606-18-2 (free base)
Chemical Formula: C23H19F3N4O3
Exact Mass: 456.14
Molecular Weight: 456.420
Elemental Analysis: C, 60.52; H, 4.20; F, 12.49; N, 12.28; O, 10.52

Price and Availability

Size Price Availability Quantity
5mg USD 90 Ready to ship
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1350 Ready to ship
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Related CAS #: 937169-00-1 (tosylate)   444606-18-2 (free base)  

Synonym: SB681323; SB 681323; SB-681323; GW 681323; GW-681323; GW681323; Dilmapimod;

IUPAC/Chemical Name: 8-(2,6-difluorophenyl)-2-((1,3-dihydroxypropan-2-yl)amino)-4-(4-fluoro-2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one

InChi Key: ORVNHOYNEHYKJG-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H19F3N4O3/c1-12-9-13(24)5-6-15(12)20-16-7-8-19(33)30(21-17(25)3-2-4-18(21)26)22(16)29-23(28-20)27-14(10-31)11-32/h2-9,14,31-32H,10-11H2,1H3,(H,27,28,29)

SMILES Code: O=C1C=CC2=C(C3=CC=C(F)C=C3C)N=C(NC(CO)CO)N=C2N1C4=C(F)C=CC=C4F

Appearance: 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:         

Biological target: Dilmapimod, also known as SB-681323 and GW-681323 , is p38 MAPK inhibitor.
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 125.0 273.87

Preparing Stock Solutions

The following data is based on the product molecular weight 456.42 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.

Recalculate based on batch purity %
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:
In vitro protocol:
In vivo protocol:

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1: Yang S, Dumitrescu TP. Population Pharmacokinetics and Pharmacodynamics Modelling of Dilmapimod in Severe Trauma Subjects at Risk for Acute Respiratory Distress Syndrome. Drugs R D. 2017 Mar;17(1):145-158. doi: 10.1007/s40268-016-0161-9. PMID: 28004376; PMCID: PMC5318329.


2: Anand P, Shenoy R, Palmer JE, Baines AJ, Lai RY, Robertson J, Bird N, Ostenfeld T, Chizh BA. Clinical trial of the p38 MAP kinase inhibitor dilmapimod in neuropathic pain following nerve injury. Eur J Pain. 2011 Nov;15(10):1040-8. doi: 10.1016/j.ejpain.2011.04.005. Epub 2011 May 14. PMID: 21576029.


3: Betts JC, Mayer RJ, Tal-Singer R, Warnock L, Clayton C, Bates S, Hoffman BE, Larminie C, Singh D. Gene expression changes caused by the p38 MAPK inhibitor dilmapimod in COPD patients: analysis of blood and sputum samples from a randomized, placebo-controlled clinical trial. Pharmacol Res Perspect. 2015 Feb;3(1):e00094. doi: 10.1002/prp2.94. Epub 2014 Dec 9. PMID: 25692013; PMCID: PMC4317226.


4: Christie JD, Vaslef S, Chang PK, May AK, Gunn SR, Yang S, Hardes K, Kahl L, Powley WM, Lipson DA, Bayliffe AI, Lazaar AL. A Randomized Dose-Escalation Study of the Safety and Anti-Inflammatory Activity of the p38 Mitogen-Activated Protein Kinase Inhibitor Dilmapimod in Severe Trauma Subjects at Risk for Acute Respiratory Distress Syndrome. Crit Care Med. 2015 Sep;43(9):1859-69. doi: 10.1097/CCM.0000000000001132. PMID: 26102252.


5: Suter MR. Microglial role in the development of chronic pain. Curr Opin Anaesthesiol. 2016 Oct;29(5):584-9. doi: 10.1097/ACO.0000000000000373. PMID: 27496572.


6: Horie S, McNicholas B, Rezoagli E, Pham T, Curley G, McAuley D, O'Kane C, Nichol A, Dos Santos C, Rocco PRM, Bellani G, Laffey JG. Emerging pharmacological therapies for ARDS: COVID-19 and beyond. Intensive Care Med. 2020 Dec;46(12):2265-2283. doi: 10.1007/s00134-020-06141-z. Epub 2020 Jul 11. PMID: 32654006; PMCID: PMC7352097.


7: Singh D, Smyth L, Borrill Z, Sweeney L, Tal-Singer R. A randomized, placebo- controlled study of the effects of the p38 MAPK inhibitor SB-681323 on blood biomarkers of inflammation in COPD patients. J Clin Pharmacol. 2010 Jan;50(1):94-100. doi: 10.1177/0091270009347873. Epub 2009 Oct 30. PMID: 19880675.