Saperconazole

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

MedKoo CAT#: 562769

CAS#: 110588-57-3

Description: 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

img
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 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.

Request quote for custom synthesis

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

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.