Ascomycin (FK520)

Catalog No.S7411

Ascomycin (FK520), an FK-506 analog, is a neutral macrolide immunosuppressant, which prevents rejection after an organ transplant. Phase 3.

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Ascomycin (FK520) Chemical Structure

Ascomycin (FK520) Chemical Structure
Molecular Weight: 792.01

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Ascomycin (FK520) is available in the following compound libraries:

Product Information

Product Description

Biological Activity

Description Ascomycin (FK520), an FK-506 analog, is a neutral macrolide immunosuppressant, which prevents rejection after an organ transplant. Phase 3.
Targets calcineurin phosphatase [2]
IC50 49 nM
In vitro Ascomycin, isolated from Streptomyces, suppresses immune response in vitro with IC50 of 0.55 nM for mouse mixed lymphocyte. [1] Ascomycin inhibits calcineurin phosphatase with IC50 of 49 nM through formation of an FKBP12-FK520-calcineurin ternary complex. FK520 also accelerate the rate of nerve regeneration, and promotes neurite outgrowth. [2] Ascomycin shows antimalarial effects via inhibition of the chaperone activity of this bifunctional protein. [3]
In vivo Ascomycin (3.2 mg/kg, i.m.) clearly prolongs skin allograft survival in rats. [1] Ascomycin, at 50 or 100 μM, produces anticonvulsant effect against picrotoxin-induced seizures when infused into the rat hippocampus. [4]
Features

Protocol(Only for Reference)

Animal Study: [1]

Animal Models Recipient WKA rats transplanted with F344 skin allografts.
Formulation Olive oil
Dosages ~32 mg/kg 5 days a week.
Administration i.m.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Hatanaka H, et al. J Antibiot (Tokyo). 1988, 41(11), 1592-1601.

[2] Revill WP, et al. J Pharmacol Exp Ther. 2002, 302(3), 1278-1285.

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Chemical Information

Download Ascomycin (FK520) SDF
Molecular Weight (MW) 792.01
Formula

C43H69NO12

CAS No. 104987-12-4
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms FR 900520, Immunomycin
Solubility (25°C) * In vitro DMSO 100 mg/mL (126.26 mM)
Ethanol 100 mg/mL (126.26 mM)
Water <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-8-Ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)tetrone

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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