MedKoo Cat#: 525847 | Name: PD 140248

Description:

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

PD 140248 is a novel broad-spectrum 7-pyrrolidinyl fluoronaphthyridines with a cyclopropyl or a difluorophenyl substitution at the 1 positions, respectively. It has been demonstrated to have excellent in vitro activity against gram-positive organisms. This compound was evaluated for its in vivo potencies against acute systemic infections in mice and in a mouse pneumococcal pneumonia model. Most remarkable was its comparative median protective value against methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Streptococcus pyogenes. PD 140248 has excellent therapeutic potential against clinically important gram-positive pathogens when the drugs are administered both orally and parenterally.

Chemical Structure

PD 140248
PD 140248
CAS#147208-55-7

Theoretical Analysis

MedKoo Cat#: 525847

Name: PD 140248

CAS#: 147208-55-7

Chemical Formula: C21H19F3N4O3

Exact Mass: 432.1409

Molecular Weight: 432.40

Elemental Analysis: C, 58.33; H, 4.43; F, 13.18; N, 12.96; O, 11.10

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
PD-140248; PD140248; PD 140248
IUPAC/Chemical Name
7-(3-(1-aminoethyl)pyrrolidin-1-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
InChi Key
VMHBXZLMBJVYFA-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H19F3N4O3/c1-10(25)11-4-5-27(8-11)20-16(24)7-13-18(29)14(21(30)31)9-28(19(13)26-20)17-3-2-12(22)6-15(17)23/h2-3,6-7,9-11H,4-5,8,25H2,1H3,(H,30,31)
SMILES Code
O=C(C1=CN(C2=CC=C(F)C=C2F)C3=C(C=C(F)C(N4CC(C(N)C)CC4)=N3)C1=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
>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

Preparing Stock Solutions

The following data is based on the product molecular weight 432.40 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
1: Shapiro MA, Dever JA, Joannides ET, Sesnie JC, Vanderroest SR. In vivo therapeutic efficacies of PD 138312 and PD 140248, two novel fluoronaphthyridines with outstanding gram-positive potency. Antimicrob Agents Chemother. 1995 Oct;39(10):2183-6. PubMed PMID: 8619563; PubMed Central PMCID: PMC162910. 2: Steiert M, Schmitz FJ. PD-140248 (Parke-Davis & Co). IDrugs. 2000 Feb;3(2):223-7. PubMed PMID: 16107942. 3: Pankuch GA, Jacobs MR, Appelbaum PC. Susceptibilities of 123 Xanthomonas maltophilia strains to clinafloxacin, PD 131628, PD 138312, PD 140248, ciprofloxacin, and ofloxacin. Antimicrob Agents Chemother. 1994 Feb;38(2):369-70. PubMed PMID: 8192468; PubMed Central PMCID: PMC284459. 4: Huband MD, Cohen MA, Meservey MA, Roland GE, Yoder SL, Dazer ME, Domagala JM. In vitro antibacterial activities of PD 138312 and PD 140248, new fluoronaphthyridines with outstanding gram-positive potency. Antimicrob Agents Chemother. 1993 Dec;37(12):2563-70. PubMed PMID: 8109918; PubMed Central PMCID: PMC192739. 5: Domagala JM, Hagen SE, Joannides T, Kiely JS, Laborde E, Schroeder MC, Sesnie JA, Shapiro MA, Suto MJ, Vanderroest S. Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy. J Med Chem. 1993 Apr 2;36(7):871-82. PubMed PMID: 8385225. 6: García-Rodríguez JA, García Sánchez JE, Trujillano I, García Sánchez E, García García MI, Fresnadillo MJ. Susceptibilities of Brucella melitensis isolates to clinafloxacin and four other new fluoroquinolones. Antimicrob Agents Chemother. 1995 May;39(5):1194-5. PubMed PMID: 7625815; PubMed Central PMCID: PMC162710.