Iclaprim mesylate

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MedKoo CAT#: 573247

CAS#: 474793-41-4

Description: Iclaprim mesylate is an antibiotic drug candidate that is active against Gram positive organisms such as methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Staphylococcus aureus (VRSA), and strains of Streptococcus pneumoniae resistant to several common antibiotics. It is also active against some Gram-negative bacteria.

Chemical Structure

Iclaprim mesylate
CAS# 474793-41-4

Theoretical Analysis

MedKoo Cat#: 573247
Name: Iclaprim mesylate
CAS#: 474793-41-4
Chemical Formula: C20H26N4O6S
Exact Mass: 450.1573
Molecular Weight: 450.51
Elemental Analysis: C, 53.32; H, 5.82; N, 12.44; O, 21.31; S, 7.12

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: AR-100.001, Iclaprim mesylate

IUPAC/Chemical Name: 2,4-Pyrimidinediamine, 5-((2-cyclopropyl-7,8-dimethoxy-2H-1-benzopyran-5-yl)methyl)-, monomethanesulfonate


InChi Code: 1S/C19H22N4O3.CH4O3S/c1-24-15-8-11(7-12-9-22-19(21)23-18(12)20)13-5-6-14(10-3-4-10)26-16(13)17(15)25-2;1-5(2,3)4/h5-6,8-10,14H,3-4,7H2,1-2H3,(H4,20,21,22,23);1H3,(H,2,3,4)

SMILES Code: NC1=NC=C(CC2=C3C=CC(C4CC4)OC3=C(OC)C(OC)=C2)C(N)=N1.CS(=O)(O)=O

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

Shelf Life: >3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 450.51 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

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1: Noviello S, Huang DB, Corey GR. Iclaprim: a differentiated option for the treatment of skin and skin structure infections. Expert Rev Anti Infect Ther. 2018 Nov;16(11):793-803. doi: 10.1080/14787210.2018.1536545. Epub 2018 Oct 23. PubMed PMID: 30317894.

2: Patel N, Huang D, Lodise T. Potential for Cost Saving with Iclaprim Owing to Avoidance of Vancomycin-Associated Acute Kidney Injury in Hospitalized Patients with Acute Bacterial Skin and Skin Structure Infections. Clin Drug Investig. 2018 Oct;38(10):935-943. doi: 10.1007/s40261-018-0686-5. PubMed PMID: 30105549.

3: Aliouat EM, Dei-Cas E, Gantois N, Pottier M, Pinçon C, Hawser S, Lier A, Huang DB. In vitro and in vivo activity of iclaprim, a diaminopyrimidine compound and potential therapeutic alternative against Pneumocystis pneumonia. Eur J Clin Microbiol Infect Dis. 2018 Mar;37(3):409-415. doi: 10.1007/s10096-018-3184-z. Epub 2018 Jan 12. PubMed PMID: 29330709.

4: Huang DB, Morrissey I, Murphy T, Hawser S, Wilcox MH. Efficacy evaluation of iclaprim in a neutropenic rat lung infection model with methicillin-resistant Staphylococcus aureus entrapped in alginate microspheres. Eur J Clin Microbiol Infect Dis. 2018 Apr;37(4):673-678. doi: 10.1007/s10096-017-3159-5. Epub 2017 Dec 8. PubMed PMID: 29222698.

5: Lodise TP, Bosso J, Kelly C, Williams PJ, Lane JR, Huang DB. Pharmacokinetic and Pharmacodynamic Analyses To Determine the Optimal Fixed Dosing Regimen of Iclaprim for Treatment of Patients with Serious Infections Caused by Gram-Positive Pathogens. Antimicrob Agents Chemother. 2018 Jan 25;62(2). pii: e01184-17. doi: 10.1128/AAC.01184-17. Print 2018 Feb. PubMed PMID: 29133566; PubMed Central PMCID: PMC5786772.

6: Huang DB, Duncan LR, Flamm RK, Dryden M, Corey GR, Wilcox MH, Torres A, File TM Jr. The effect of pulmonary surfactant on the in vitro activity of Iclaprim against common respiratory bacterial pathogens. Diagn Microbiol Infect Dis. 2018 Jan;90(1):64-66. doi: 10.1016/j.diagmicrobio.2017.09.011. Epub 2017 Sep 20. PubMed PMID: 29103875.

7: Huang DB, File TM Jr, Torres A, Shorr AF, Wilcox MH, Hadvary P, Dryden M, Corey GR. A Phase II Randomized, Double-blind, Multicenter Study to Evaluate Efficacy and Safety of Intravenous Iclaprim Versus Vancomycin for the Treatment of Nosocomial Pneumonia Suspected or Confirmed to be Due to Gram-positive Pathogens. Clin Ther. 2017 Aug;39(8):1706-1718. doi: 10.1016/j.clinthera.2017.07.007. Epub 2017 Jul 27. PubMed PMID: 28756068.