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Rezafungin acetate

Alias: Rezafungin Rezzayo Biafungin SP-3025 CD-101SP 3025 CD101SP3025 CD 101.
Cat No.:V13715 Purity: ≥98%
Rezafunginacetate (Biafungin;CD101 acetate; SP-3025 acetate; Rezzayo) is a novel, broad-spectrum, and long-lasting echinocandin with antifungal activity against Candida spp.
Rezafungin acetate
Rezafungin acetate Chemical Structure CAS No.: 1631754-41-0
Product category: New12
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
Other Sizes

Other Forms of Rezafungin acetate:

  • Rezafungin
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Rezafungin acetate (Biafungin; CD101 acetate; SP-3025 acetate; Rezzayo) is a novel, broad-spectrum, and long-lasting echinocandin with antifungal activity against Candida spp., Aspergillus spp., and Pneumocystis spp and subsets of echinocandin-resistant Candida auris and azole-resistant Aspergillus isolates. It is chemically related with anidulafungin, and acts as a 1,3-β-D-glucan synthase inhibitor. In Mar 2023, it has been approved by FDA for the treatment of Candidiasis.

Biological Activity I Assay Protocols (From Reference)
ln Vivo
In a mouse infection model, rezafunginacetate (Biafunginacetate) (1 mg/kg; i.p. once daily for 6 days) has demonstrated efficient in vivo prophylaxis against Pneumocystis jiroveci [1].
Animal Protocol
Animal/Disease Models: C3H/HeN mice [1]
Doses: 1 mg/kg
Route of Administration: intraperitoneal (ip) injection; one time/day for 6 days
Experimental Results: The burden of cell nuclei and ascus was Dramatically diminished.
Toxicity/Toxicokinetics
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the use of rezafungin during breastfeeding. Because rezafungin is about 90% bound to plasma proteins and has poor oral bioavailability, it is unlikely to reach the milk and be absorbed by the infant. If rezafungin is required by the mother, it is not a reason to discontinue breastfeeding.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
References

[1]. Rezafungin Prophylactic Efficacy in a Mouse Model of Pneumocystis Pneumonia. VOLUME 25, ISSUE 3, SUPPLEMENT, S366, MARCH 01, 2019.

[2]. Rezafungin (CD101), a next-generation echinocandin: A systematic literature review and assessment of possible place in therapy. J Glob Antimicrob Resist. 2018 Sep;14:58-64.

Additional Infomation
Rezafungin is a member of the family of echinocandins that inhibits 1,3-beta-D-glucan synthase. It is developed by Cidara Therapeutics and approved for the treatment of candidaemia and invasive candidiasis in patients aged >= 18 years who have limited or no alternative treatment options. It is an echinocandin, a quaternary ammonium ion, an antibiotic antifungal drug, an azamacrocycle, a homodetic cyclic peptide and an aromatic ether.
Rezafungin is an Echinocandin Antifungal.
Rezafungin is a next-generation, semi-synthetic, cyclic lipopeptide and echinocandin derivative, with potential antifungal activity. Upon administration, rezafungin inhibits the fungal specific enzyme 1,3-beta-D-glucan synthase, which is essential for fungal cell wall synthesis, and results in decreased synthesis of beta(1,3)-D-glucan. This weakens the fungal cell wall thereby causing osmotic lysis, fungal cell wall rupture and fungal cell death.
See also: Rezafungin (annotation moved to).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C65H88N8O19
Molecular Weight
1285.43643856049
Exact Mass
1225.602
Elemental Analysis
C, 60.73; H, 6.90; N, 8.72; O, 23.65
CAS #
1631754-41-0
Related CAS #
Rezafungin;1396640-59-7
PubChem CID
78318119
Appearance
White to off-white solid powder
LogP
2.9
Hydrogen Bond Donor Count
13
Hydrogen Bond Acceptor Count
17
Rotatable Bond Count
18
Heavy Atom Count
88
Complexity
2300
Defined Atom Stereocenter Count
15
SMILES
CCCCCOC1=CC=C(C=C1)C2=CC=C(C=C2)C3=CC=C(C=C3)C(=O)N[C@H]4C[C@H]([C@H](NC(=O)[C@@H]5[C@H]([C@H](CN5C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]6C[C@H](CN6C(=O)[C@@H](NC4=O)[C@@H](C)O)O)[C@@H]([C@H](C7=CC=C(C=C7)O)O)O)[C@@H](C)O)C)O)OCC[N+](C)(C)C)O
InChi Key
MXMWJAPNUIKPGF-DPHATNFGSA-N
InChi Code
InChI=1S/C63H84N8O17.C2H4O2/c1-8-9-10-28-87-45-25-21-40(22-26-45)38-13-11-37(12-14-38)39-15-17-42(18-16-39)56(80)64-46-31-48(76)61(88-29-27-71(5,6)7)68-60(84)52-53(77)34(2)32-70(52)63(86)50(36(4)73)66-59(83)51(55(79)54(78)41-19-23-43(74)24-20-41)67-58(82)47-30-44(75)33-69(47)62(85)49(35(3)72)65-57(46)811-2(3)4/h11-26,34-36,44,46-55,61,72-73,75-79H,8-10,27-33H2,1-7H3,(H5-,64,65,66,67,68,74,80,81,82,83,84)1H3,(H,3,4)/t34-,35+,36+,44+,46-,47-,48+,49?,50-,51?,52-,53-,54-,55-,61+/m0./s1
Chemical Name
2-(((2R,9S,11R,12R,14aS,15S,16S,20S,25aS)-23-((1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl)-2,11,15-trihydroxy-6,20-bis((R)-1-hydroxyethyl)-16-methyl-5,8,14,19,22,25-hexaoxo-9-(4''-(pentyloxy)-[1,1'
Synonyms
Rezafungin Rezzayo Biafungin SP-3025 CD-101SP 3025 CD101SP3025 CD 101.
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~230 mg/mL (~178.93 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 5.75 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 5.75 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 5.75 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.7779 mL 3.8897 mL 7.7794 mL
5 mM 0.1556 mL 0.7779 mL 1.5559 mL
10 mM 0.0778 mL 0.3890 mL 0.7779 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • Enter 10 in the Concentration box and choose the correct unit (mM)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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