Art. -Nr.: HY-13557

Ascomycin

(Synonyms: Immunomycin; FR-900520; FK520)

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research.

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Reinheit: 99.96%
CAS. Nr.: 104987-12-4
Formel: C₄₃H₆₉NO₁₂
Molecular Weight:792.01

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ascomycin Chemical Structure

CAS. Nr.: 104987-12-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Plasmodium

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Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC₅₀	0.205 nM Compound: 2, FK520	Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay	10.1039/C2MD20266B
Murine T-cell line	IC₅₀	0.69 nM Compound: 2	Inhibition of proliferation of PMA and Ionomycin stimulated murine T cells Inhibition of proliferation of PMA and Ionomycin stimulated murine T cells	10.1016/0960-894X(95)00161-L
T-cell	IC₅₀	0.69 nM Compound: 3 (Ascomycin)	Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control	10.1016/S0960-894X(01)81248-8
T-cell	IC₅₀	0.69 nM Compound: 1	In vitro immunosuppressive activity in murine splenic T cells In vitro immunosuppressive activity in murine splenic T cells	[PMID: 10450986]
T-cell	IC₅₀	0.69 nM Compound: 1	Immunosuppressive activity was determined as the ability to inhibit T cell proliferation. Immunosuppressive activity was determined as the ability to inhibit T cell proliferation.	[PMID: 9873523]
T-cell	IC₅₀	0.69 nM Compound: 2 ; 2A, (L-683590)	In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells	10.1016/S0960-894X(01)80265-1
T-cell	IC₅₀	0.69 nM Compound: 2, (L-683590)	In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells	10.1016/S0960-894X(01)80264-X
T-cell	IC₅₀	0.69 nM Compound: Ascomycin	In vitro suppression of T-cell proliferation. In vitro suppression of T-cell proliferation.	10.1016/S0960-894X(97)00409-5

In Vitro

Ascomycin (FR-900520) suppresses immune response in vitro with an IC₅₀ value of 0.55 nM for mouse mixed lymphocyte reaction^[1].
Ascomycin is a powerful calcium-dependent serine/threonine protein phosphatase (calcineurin [CaN], protein phosphatase 2B) inhibitors. Its mechanism of action involves the formation of a molecular complex with the intracellular FK506-binding protein-12 (FKBP12), thereby acquiring the ability to interact with CaN and to interfere with the dephosphorylation of various substrates^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ascomycin (FR-900520; i.m.; 0.32-32 mg/kg; 5 days a week; for 2 weeks) clearly prolongs skin allograft survival in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

WKA rats (8-10 weeks old) transplanted with F344 skin allografts^[1]
Dosage:

0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg, 32 mg/kg
Administration:

i.m.; 5 days a week; for 2 weeks
Result:

Clearly prolonged skin allograft survival in rats

Chemical Information

CAS. Nr. 104987-12-4
Appearance Solid
Molecular Weight 792.01
Formel C₄₃H₆₉NO₁₂
Color White to off-white
SMILES

O=C([C@@](CCCC1)([H])N1C(C([C@@]2(O)[C@H](C)C[C@H](OC)[C@@](O2)([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H]3CC)=O)=O)O[C@H](/C(C)=C/[C@H]4C[C@@H](OC)[C@H](O)CC4)[C@H](C)[C@@H](O)CC3=O
Synonyms

Immunomycin; FR-900520; FK520
Structure Classification
- Antibiotics
- Macrolide Antibiotics
Initial Source
- Microorganisms
Streptomyces tubercidicus
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

All Cell Proliferation/Viability Assay

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Journal Impact Factor

Proc Natl Acad Sci U S A

Calcineurin controls proximodistal blastema polarity in zebrafish fin regeneration. [Abstract]

2021 Jan 12;118(2):e2009539118. PMID: 33376206
Pharmaceutics

Synergistic Combination of Irinotecan and Rapamycin Orally Delivered by Nanoemulsion for Enhancing Therapeutic Efficacy of Pancreatic Cancer. [Abstract]

2023 Jan 31;15(2):473. PMID: 36839795
MBio

FKBP12-Dependent Inhibition of Calcineurin Mediates Immunosuppressive Antifungal Drug Action in Malassezia. [Abstract]

2017 Oct 24;8(5). pii: e01752-17. PMID: 29066552

Ascomycin purchased from MedChemExpress. Usage Cited in: MBio. 2017 Oct 24;8(5). pii: e01752-17. [Abstract]

Deletion of the FKB1 gene of M. furfur confers resistance to FK506. Sensitivity of the M. furfur strain CBS 14141 to the calcineurin inhibitors FK506, Ascomycin, and Pimecrolimus.
Neurochem Res

Systemic Rapamycin Attenuates Morphine-Induced Analgesic Tolerance and Hyperalgesia in Mice. [Abstract]

2019 Feb;44(2):465-471. PMID: 30547365
Biopharm Drug Dispos

Metabolic interaction between biflavonoids in Ginkgo biloba leaves and tacrolimus. [Abstract]

2023 Apr;44(2):157-164. PMID: 36840704
Hong Kong Polytechnic University

2023 Apr.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 39 mg/mL (49.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2626 mL

6.3131 mL

12.6261 mL

5 mM

0.2525 mL

1.2626 mL

2.5252 mL

10 mM

0.1263 mL

0.6313 mL

1.2626 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (3.16 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (2.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (2.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (607 KB)
- English - EN (607 KB)
- Français - FR (607 KB)
- Deutsch - DE (607 KB)
- Norwegian - NO (607 KB)
- Español - ES (607 KB)
- Swedish - SV (607 KB)
- Italian - IT (607 KB)
- Korean - KR (607 KB)
- Portuguese - PT (607 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hatanaka H, et al. FR-900520 and FR-900523, novel immunosuppressants isolated from a Streptomyces. II. Fermentation, isolation and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1988 Nov;41(11):1592-601. [Content Brief]

[2]. Krishika Sambyal, et al. Bioprocess and genetic engineering aspects of ascomycin production: a review. J Genet Eng Biotechnol. 2020 Nov 19;18(1):73. [Content Brief]

[3]. Germán Sierra-Paredes, et al. Ascomycin and FK506: pharmacology and therapeutic potential as anticonvulsants and neuroprotectants. CNS Neurosci Ther. Spring 2008;14(1):36-46. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2626 mL	6.3131 mL	12.6261 mL	31.5653 mL
	5 mM	0.2525 mL	1.2626 mL	2.5252 mL	6.3131 mL
	10 mM	0.1263 mL	0.6313 mL	1.2626 mL	3.1565 mL
	15 mM	0.0842 mL	0.4209 mL	0.8417 mL	2.1044 mL
	20 mM	0.0631 mL	0.3157 mL	0.6313 mL	1.5783 mL
	25 mM	0.0505 mL	0.2525 mL	0.5050 mL	1.2626 mL
	30 mM	0.0421 mL	0.2104 mL	0.4209 mL	1.0522 mL
	40 mM	0.0316 mL	0.1578 mL	0.3157 mL	0.7891 mL

Ascomycin

6 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Ascomycin

Alle Parasite Isoform-spezifische Produkte anzeigen

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ascomycin Related Classifications

HY-13557 Related Classifications