BAFILOMYCIN A1

Bezeichnung:BAFILOMYCIN A1

CAS-Nr88899-55-2

Englisch Name:BAFILOMYCIN A1

CBNumberCB3743951

SummenformelC35H58O9

Molgewicht622.83

MOL-Datei88899-55-2.mol

BAFILOMYCIN A1 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>106°C (dec.)
Siedepunkt	582.86°C (rough estimate)
Dichte	1.0594 (rough estimate)
Brechungsindex	1.5000 (estimate)
RTECS-Nr.	RN9781000
Flammpunkt	87℃
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (up to 5 mg/ml, with warming).
pka	12.66±0.70(Predicted)
Aggregatzustand	Powder or Solid
Farbe	White to off-white
Wasserlöslichkeit	Soluble in methanol, ethanol, acetone and chloroform. Insoluble in water.
BRN	4730700
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-36
RIDADR	3172
WGK Germany	3
F	10
HazardClass	6.1(b)
PackingGroup	III
HS Code	29419090

Gefahreninformationscode (GHS)

BAFILOMYCIN A1 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Bafilomycin A₁ is a fungal metabolite that has been found in Streptomyces and has diverse biological activities. It is an inhibitor of vacuolar H⁺-ATPases (V-ATPases; K_i = 0.5 nM in N. crassa vacuolar membranes) and is greater than 1,000-fold selective for V-ATPases over Na⁺/K⁺-, Ca²⁺-, and H⁺-ATPases. Bafilomycin A₁ (100 nM) inhibits autophagosome maturation and protein degradation in H-4-II-E cells. It inhibits chloroquine-induced apoptosis in primary cerebellar granule neurons (CGNs) but not chloroquine-induced inhibition of macroautophagy. Bafilomycin A₁ (100 nM) reduces viral yield in the culture supernatant of Vero E6 and Huh7 cells, as well as HEK293T cells expressing human angiotensin-converting enzyme 2 (ACE2), infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). It also reduces lung RNA copy numbers and viral pneumonia in ACE2 transgenic mice infected with SARS-CoV-2 when administered at a dose of 0.1 mg/kg.
Chemische Eigenschaften
white to off-white powder
Verwenden
Bafilomycin A1 is a member of a potent family of macrocyclic lactones with broad spectrum biological activity, including activity against bacteria, yeast, fungi, nematodes, insects and tumour cell lines. Bafilomycin A1 is an inhibitor of vacuolar-type ATPase.
Verwenden
A macrolide antibiotic and potent and selective inhibitor of vacuolar-type (v-type) H+ ATPase
Verwenden
Bafilomycin A1 is a specific potent inhibitor of vacuolar ATPases.It is used as an antibacterial, antifungal, antineoplastic and an immunosuppressive. It prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes and is a macrolide antibiotic and potent and selective inhibitor of vacuolar-type H+ ATPase (V-ATPase).
Definition
ChEBI: The most used of the bafilomycins, a family of toxic macrolide antibiotics derived from Streptomyces griseus.
Allgemeine Beschreibung
A macrolide antibiotic that acts as a specific inhibitor of vacuolar-type H⁺-ATPase (V-type; K_i = 500 pM). A valuable tool for distinguishing among different types of ATPases. Blocks lysosomal cholesterol trafficking in macrophages and is known to interfere with pH regulation in brain cells. Exhibits cytotoxic effects on a number of cell lines in a cell viability assay. Reported to selectively inhibit β-secretase, an enzyme involved in the processing of amyloid precursor protein (APP). The InSolution format with a purity of ≥97% by HPLC in 90% DMSO is also available (Cat. No. 508409).
Biologische Aktivität
Highly potent, selective inhibitor of vacuolar H + -ATPases (IC 50 = 500 pM as measured in chromaffin granule membranes). Selective over other ATP hydrolyzing enzymes such as F-ATPases, Ca 2+ -ATPases, Na + /K + -ATPases and plasma membrane H + -ATPases.
Biochem/physiol Actions
Bafilomycin A1 is a macrolide antibiotic. Bafilomycin A1 acts as a potent and selective inhibitor of vacuolar-type H+-ATPase.
Lager
-20°C
Einzelnachweise
1) Werner?et al.? (1984) Metabolic products of microorganisms. Bafilomycins, a new group of macrolide antibiotics. Production, isolation, chemical structure and biological activity; J. Antibiot.,?37?110 2) Drose and Altendorf? (1997)?Bafilomycins and concanamycins as inhibitors of V-ATPase and P-ATPase;?J. Exp. Biol.,?200?1 3) Yamamoto?et al. (1998)?Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells;?Cell Struct. Func.,?23?33

BAFILOMYCIN A1 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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