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MedKoo Cat#: 562769 | Name: Saperconazole

Description:

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

Saperconazole is a broad-spectrum antifungal agent. It acts by selective inhibiting the cytochrome P-450-dependent ergosterol synthesis in Candida albicans, Aspergillus fumigatus and Trichophyton mentagrophytes, with in vitro and in vivo activity against F. pedrosoi.

Chemical Structure

Saperconazole
Saperconazole
CAS#110588-57-3

Theoretical Analysis

MedKoo Cat#: 562769

Name: Saperconazole

CAS#: 110588-57-3

Chemical Formula: C35H38F2N8O4

Exact Mass: 672.2984

Molecular Weight: 672.73

Elemental Analysis: C, 62.49; H, 5.69; F, 5.65; N, 16.66; O, 9.51

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.
Bulk Inquiry
Related CAS #
No Data
Synonym
Saperconazole; SPZ; R66905; R-66905; R 66905;
IUPAC/Chemical Name
2-Butan-2-yl-4-[4-[4-[4-[[(2R,4S)-2-(2,4-difluorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one
InChi Key
HUADITLKOCMHSB-ZPGVKDDISA-N
InChi Code
InChI=1S/C35H38F2N8O4/c1-3-25(2)45-34(46)44(24-40-45)29-7-5-27(6-8-29)41-14-16-42(17-15-41)28-9-11-30(12-10-28)47-19-31-20-48-35(49-31,21-43-23-38-22-39-43)32-13-4-26(36)18-33(32)37/h4-13,18,22-25,31H,3,14-17,19-21H2,1-2H3/t25?,31-,35-/m0/s1
SMILES Code
O=C1N(C(CC)C)N=CN1C2=CC=C(N3CCN(C4=CC=C(OC[C@@H]5O[C@@](CN6N=CN=C6)(C7=CC=C(F)C=C7F)OC5)C=C4)CC3)C=C2
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 672.73 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: Meerpoel L, Heeres J, Backx LJ, Van der Veken LJ, Hendrickx R, Corens D, De Groot A, Leurs S, Van der Eycken L, Weerts J, Luyts P, Van Gerven F, Woestenborghs FA, Van Breda A, Oris M, van Dorsselaer P, Willemsens GH, Bellens D, Marichal PJ, Vanden Bossche HF, Odds FC. Synthesis and in vitro and in vivo antifungal activity of the hydroxy metabolites of saperconazole. ChemMedChem. 2010 May 3;5(5):757-69. doi: 10.1002/cmdc.201000040. PubMed PMID: 20379992. 2: Benko I, Hernádi F, Megyeri A, Kiss A, Somogyi G, Tegyey Z, Kraicsovits F, Kovács P. Comparison of the toxicity of fluconazole and other azole antifungal drugs to murine and human granulocyte-macrophage progenitor cells in vitro. J Antimicrob Chemother. 1999 May;43(5):675-81. PubMed PMID: 10382889. 3: Cardona-Castro N, Agudelo-Flórez P, Restrepo-Molina R. Chromoblastomycosis murine model and in vitro test to evaluate the sensitivity of Fonsecaea pedrosoi to ketoconazole, itraconazole and saperconazole. Mem Inst Oswaldo Cruz. 1996 Nov-Dec;91(6):779-84. PubMed PMID: 9283666. 4: Chowdhry L, Khan ZK, Kulshrestha DK. Evaluation of himachalol in murine invasive aspergillosis. Mycoses. 1996 Nov-Dec;39(11-12):449-52. PubMed PMID: 9145002. 5: Hanson LH, Clemons KV, Denning DW, Stevens DA. Efficacy of oral saperconazole in systemic murine aspergillosis. J Med Vet Mycol. 1995 Sep-Oct;33(5):311-7. PubMed PMID: 8544084. 6: Johnson DA, Johns KJ, Robinson RD, Head WS, O'Day DM. The relationship of corneal epithelial defect size to drug penetration. Arch Ophthalmol. 1995 May;113(5):641-4. PubMed PMID: 7748136. 7: Finquelievich J, Costa MR, Iovannitti C, Negroni R. Blood culture as a parameter of treatment effectiveness in experimental histoplasmosis of the hamster. Rev Inst Med Trop Sao Paulo. 1995 Mar-Apr;37(2):99-102. PubMed PMID: 7481478. 8: Khoo SH, Denning DW. Cure of chronic invasive sinus aspergillosis with oral saperconazole. J Med Vet Mycol. 1995 Jan-Feb;33(1):63-6. PubMed PMID: 7650581. 9: Asiri S, Ogbunude PO, Warhurst DC. In vitro assessment of susceptibility of Acanthamoeba polyphaga to drugs using combined methods of dye-binding assay and uptake of radiolabelled adenosine. Int J Parasitol. 1994 Nov;24(7):975-80. PubMed PMID: 7533747. 10: Restrepo A. Treatment of tropical mycoses. J Am Acad Dermatol. 1994 Sep;31(3 Pt 2):S91-102. Review. PubMed PMID: 8077517. 11: Hay RJ. Antifungal drugs on the horizon. J Am Acad Dermatol. 1994 Sep;31(3 Pt 2):S82-6. Review. PubMed PMID: 8077515. 12: Sugar AM, Salibian M, Goldani LZ. Saperconazole therapy of murine disseminated candidiasis: efficacy and interactions with amphotericin B. Antimicrob Agents Chemother. 1994 Feb;38(2):371-3. PubMed PMID: 8192469; PubMed Central PMCID: PMC284460. 13: Lynch ME, Sobel JD. Comparative in vitro activity of antimycotic agents against pathogenic vaginal yeast isolates. J Med Vet Mycol. 1994;32(4):267-74. PubMed PMID: 7983571. 14: Klippenstein K, O'Day DM, Robinson RD, Williams TE, Head WS. The qualitative evaluation of the pharmacokinetics of subconjunctivally injected antifungal agents in rabbits. Cornea. 1993 Nov;12(6):512-6. PubMed PMID: 8261783. 15: Zienicke H, Korting HC. Clinical efficacy and tolerability of saperconazole for tinea of glabrous skin. A report on four cases. Mycoses. 1993 Mar-Apr;36(3-4):131-4. PubMed PMID: 8366876. 16: Degreef H. [New antifungal agents in the treatment of superficial dermatomycoses]. Ann Dermatol Venereol. 1993;120(1):21-31. Review. French. PubMed PMID: 8393313. 17: San-Blas G, Calcagno AM, San-Blas F. A preliminary study of in vitro antibiotic activity of saperconazole and other azoles on Paracoccidioides brasiliensis. J Med Vet Mycol. 1993;31(2):169-74. PubMed PMID: 8389848. 18: Patterson TF, George D, Miniter P, Andriole VT. Saperconazole therapy in a rabbit model of invasive aspergillosis. Antimicrob Agents Chemother. 1992 Dec;36(12):2681-5. PubMed PMID: 1482137; PubMed Central PMCID: PMC245528. 19: Franco L, Gomez I, Restrepo A. Saperconazole in the treatment of systemic and subcutaneous mycoses. Int J Dermatol. 1992 Oct;31(10):725-9. PubMed PMID: 1399205. 20: Otcenásek M. Susceptibility of clinical isolates of fungi to saperconazole. Mycopathologia. 1992 Jun;118(3):179-83. PubMed PMID: 1528231.

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