| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
| 50mg | |||
| 100mg | |||
| 250mg |
Purity: ≥98%
Rezafungin (Biafungin; Rezzayo) is a novel, broad-spectrum, and long-lasting echinocandin with antifungal activity against Candida spp., Aspergillus spp., and Pneumocystis spp. It acts as a 1,3-β-D-glucan synthase inhibitor. In Mar 2023, it has been approved by FDA for the treatment of Candidiasis.
| Targets |
1,3-β-D-glucan synthase enzyme complex
|
|---|---|
| ln Vitro |
Rezafungin is an echinocandin antifungal drug. It inhibits the 1,3-β-D-glucan synthase enzyme complex present in the cell walls of fungi, responsible for the formation of 1,3-β-D-glucan. Since 1,3-β-D-glucan is an essential component of fungal cell walls, rezafungin disrupts the cell wall of fungal species, including _Candida_ spp., and acts as a concentration-dependent _in vitro_ fungicidal. Mammalian cells do not express β-1-3-glucan synthase; therefore, the action of rezafungin is specific to fungi. Rezafungin is a member of the family of echinocandins that inhibits 1,3-beta-D-glucan synthase.
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| ln Vivo |
In a mouse infection model, rezafungin (Biafungin) has demonstrated strong in vivo prophylaxis against Pneumocystis jiroveci [1].
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| 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. |
| ADME/Pharmacokinetics |
Absorption
Rezafungin dosage ranges from 50 mg (equivalent to 0.125 times the maximum recommended loading dose) to 400 mg, with both Cmax and AUC increasing proportionally with the dose, regardless of whether it is a single or multiple dose. In patients with candidemia and invasive candidiasis, an initial loading dose of 400 mg rezafungin, followed by weekly 200 mg doses, resulted in Cmax of 19.2 mcg/mL, AUC0-168 (AUC0-168) of 0-168 hours post-dose, and Cmin of 2.4 mcg/mL on day 1. In the same cohort, Cmax, AUC0-168, and Cmin of day 15 were 11.8 mcg/mL, 667 mcg/mL, and 2.2 mcg/mL, respectively. Compared with healthy subjects, patients with candidemia had reduced AUC0-168 and Cmax by 30% and 19%, respectively. Age, sex, race, weight, and hepatic impairment had no clinically significant effect on the pharmacokinetics of rezafenib. Elimination Route Rizafenib is primarily excreted in feces. In healthy subjects, 74.3% of the drug was primarily excreted in feces as rezafenib, while 25.7% was primarily excreted in urine as inactive metabolites of rezafenib. Volume of Distribution The volume of distribution of rezafenib is 67 L. Clearance The clearance of rezafenib is 0.35 L/hr. Protein Binding Rizafenib has a high protein binding rate. Protein binding in patients increased from 87.5% to 93.6%, and in healthy adults from 95.6% to >98.6%. Metabolism/Metabolites Rizafenone is metabolized via hydroxylation of the terphenylpentyl ether side chain, producing three hydroxylated metabolite isomers: 2'-, 3'-, or 4'-hydroxypentylrezafenone. Rizafenone can also lose the pentyl group via O-dealkylation to produce depentylrezafenone. Subsequent binding (sulfation) reactions of the hydroxyl metabolites are minimal. Rizafenone is not metabolized in the liver and is not expected to become a clinically relevant substrate for CYP450 enzymes. Biological Half-Life The terminal half-life of rizafenone is 152 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information regarding the use of rezafenamic acid during lactation. Because rezafenamic acid binds to plasma proteins at a rate of approximately 90% and has low oral bioavailability, it is unlikely to enter breast milk and be absorbed by the infant. If the mother needs to use rezafenamic acid, breastfeeding should not be discontinued. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. |
| References |
[1]. Melanie Cushion, et al. Rezafungin Prophylactic Efficacy in a Mouse Model of Pneumocystis Pneumonia. VOLUME 25, ISSUE 3, SUPPLEMENT, S366, MARCH 01, 2019.
[2]. Sofjan AK, et al. 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 an echinocandin antibiotic that inhibits 1,3-β-D-glucan synthase. Developed by Cidara Therapeutics, it is approved for the treatment of candidemia and invasive candidiasis in patients aged 18 years and older with limited alternative treatment options. Rezafungin is an echinocandin antifungal drug, belonging to the quaternary ammonium ion class of antibiotics, and is also a nitrogen-containing macrocyclic compound, homocyclic peptide, and aromatic ether compound. Rezafungin is a new generation of semi-synthetic cyclic lipopeptide and echinocandin derivative with potential antifungal activity. After administration, rezafungin inhibits the fungal-specific enzyme 1,3-β-D-glucan synthase (which is crucial for fungal cell wall synthesis), resulting in reduced β(1,3)-D-glucan synthesis. This weakens the fungal cell wall, leading to osmotic lysis, fungal cell wall rupture, and fungal cell death. See also: Rizafenib (note moved to).
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| Molecular Formula |
C63H85N8O17
|
|---|---|
| Molecular Weight |
1226.3924176693
|
| Exact Mass |
1225.603
|
| CAS # |
1396640-59-7
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| Related CAS # |
Rezafungin acetate;1631754-41-0; 1396640-59-7 (cation) ; 1396640-60-0 (TFA)
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| PubChem CID |
78318119
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
2.9
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| 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 |
LNFCWEXGZIEGJW-TXSVMFMRSA-O
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| InChi Code |
InChI=1S/C63H84N8O17/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)81/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)/p+1/t34-,35+,36+,44+,46-,47-,48+,49-,50-,51-,52-,53-,54-,55-,61+/m0/s1
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| Chemical Name |
2-[[(3S,6S,9S,11R,15S,18S,20R,21R,24S,25S,26S)-6-[(1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]-11,20,25-trihydroxy-3,15-bis[(1R)-1-hydroxyethyl]-26-methyl-2,5,8,14,17,23-hexaoxo-18-[[4-[4-(4-pentoxyphenyl)phenyl]benzoyl]amino]-1,4,7,13,16,22-hexazatricyclo[22.3.0.09,13]heptacosan-21-yl]oxy]ethyl-trimethylazanium
|
| Synonyms |
Rezafungin; rezafungin acetate; 1631754-41-0; Rezafungin (acetate); acetate de rezafungine; acetato de rezafungina; Biafungin; Rezzayo
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8154 mL | 4.0770 mL | 8.1540 mL | |
| 5 mM | 0.1631 mL | 0.8154 mL | 1.6308 mL | |
| 10 mM | 0.0815 mL | 0.4077 mL | 0.8154 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.
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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