Ascomycin

Bezeichnung:Ascomycin

CAS-Nr104987-12-4

Englisch Name:Ascomycin

CBNumberCB2406330

SummenformelC43H69NO12

Molgewicht792.01

MOL-Datei104987-12-4.mol

Ascomycin physikalisch-chemischer Eigenschaften

Schmelzpunkt	153-157°C
Siedepunkt	868℃
Dichte	1.19±0.1 g/cm3(Predicted)
Flammpunkt	>110°(230°F)
storage temp.	Inert atmosphere,Store in freezer, under -20°C
Löslichkeit	≥38.9 mg/mL in DMSO; insoluble in H2O; ≥98.6 mg/mL in EtOH
Aggregatzustand	Powder
pka	9.97±0.70(Predicted)
Wasserlöslichkeit	Soluble in DMSO at 65mg/ml; soluble in ethanol at 50mg/m; with warming. Very poorly soluble in water
InChIKey	ZDQSOHOQTUFQEM-AMASXYNMSA-N

Sicherheit

Kennzeichnung gefährlicher	Xn,F
R-Sätze:	20/21/22-36-11
S-Sätze:	36/37-16
RIDADR	UN 1648 3 / PGII
WGK Germany	3
RTECS-Nr.	KD4185000
F	10
HS Code	29419090

Gefahreninformationscode (GHS)

Ascomycin Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
Chemische Eigenschaften
White Solid
Verwenden
Everolimus is a semi-synthetic macrocyclic lactone prepared from rapamycin by selective alkylation of the 42-hydroxy group with a silyl-protected hydroxyethyl triflate moiety, followed by addition of an ethylhydroxy moiety to provide greater stability and bioavailability. Like all tacrolimus analogues, everolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing it from interacting with target proteins. Everolimus is extensively cited in the literature with over 2,000 citations.
Verwenden
A potent immunosuppressive agent and could be used as a potential therapeutic agent for autoimmune diseases
Verwenden
Ascomycin is a macrocyclic lactone closely related to tacrolimus and rapamycin. Ascomycin is isolated from several species of Streptomyces and was first reported in 1988. Ascomycin exhibits limited, potent antifungal activity but has found considerable utility as an immunosuppressant.
Definition
ChEBI: A macrolide that is produced by the fermentation of Streptomyces hygroscopicus and exhibits strong immunosuppressant properties.
Biologische Aktivität
ascomycin (fk 520, fr900520) is a novel neutral macrolide immunosuppressant, isolated from the cultured broth of streptomyces hygroscopicus subsp. yakushimaensis no. 7238.
in vitro
ascomycin (fk 520, fr900520) suppressed lymphocyte reaction in a dose dependent fashion. ascomycin was non-toxic at concentrations less than 3,200 nm, at which the percent inhibition was 18.9%. ascomycin showed antifungal activity against aspergillus fumigatus ifo 5840. ascomycin had no inhibitory effect on bacteria or yeast at 100 μg/ml [1].
in vivo
ascomycin was dose-dependently effective and clearly prolonged skin allograft survival at 3.2 mg/kg or more, though all skin allografts were rejected within 7 days in rats treated intramuscularly with olive oil. ascomycin, dissolved in olive oil, showed no adverse effect when administered intraperitoneally to ddy mice (male, 8 weeks old) at 100 mg/kg [1].
target
peptidyl-prolyl cis-trans isomerase
Lager
-20°C
Einzelnachweise
[1] hatanaka h, kino t, miyata s, inamura n, kuroda a, goto t, tanaka h, okuhara m. fr-900520 and fr-900523, novel immunosuppressants isolated from a streptomyces. ii. fermentation, isolation and physico-chemical and biological characteristics. j antibiot (tokyo). 1988;41(11):1592-601.

Ascomycin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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