[CAS NO. 80890-47-7] Concanamycin A
PRODUCTS SPECIFICATIONS [80890-47-7]
DESCRIPTION [80890-47-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 866.09 |
| Molecular Formula | C46H75NO14 |
| SMILES | C[C@H]([C@@](C[C@H]1O[C@@](O[C@H](C)[C@H]2OC(N)=O)([H])C[C@H]2O)(O[C@H](/C=C/C)[C@H]1C)O)[C@H](O)[C@@H]([C@](OC(/C(OC)=C/C(C)=C/[C@H]([C@@H](O)[C@H]3CC)C)=O)([H])[C@H](/C=C/C=C(C[C@H]([C@@H]3O)C)/C)OC)C |
3 Publications Citing Use of MCE
Summary
Concanamycin A (Folimycin; Antibiotic X 4357B) is a macrolide antibiotic , a vacuolar type H + -ATPase (V-ATPase) inhibitor. Concanamycin A is also an inhibitor of lysosomal acidification, can be used to T cell-mediated inflammation research [1] - [5] .
IC50 & Target
|
Macrolide |
In Vitro
Concanamycin A can come from
S. diastatochromogenes
545, as a microbial metabolite with immunomodulatory activity
[1]
.
Concanamycin A (100 nM; 0-20 h) results DNA fragmentation in CD4
+
and selectively induces CD8
+
T cells rapid cell death between normal and the immunized mice source, while CD8
+
population in mice immunized is more sensitive
[2]
.
Concanamycin A (3-50 nM; 16 h) inhibits LPS-induced NO production in elicited peritoneal macrophages, but (25 nM; 7 h) doesn’t inhibit LPS-induced TNF-α production
[3]
.
Concanamycin A (0.01 nM-1 nM) inhibits the acidification of rat liver lysosomes (IC
50
=0.061 nM), and inhibits oleate incorporation into cholesteryl ester (IC
50
=14 nM)
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [2]
| Cell Line: | CD8 + cytotoxic T lymphocytes (CTLs) |
| Concentration: | 100 nM |
| Incubation Time: | 0, 4, 8, 12, 16, 20 hours |
| Result: | Induced rapid cell death instead of apoptosis at 20 h, without observed condensed nuclei. |
In Vivo
Concanamycin A (15 mg/kg; i.v.; 0, 10 or 24 h prior to sacrifice) induced T cell-mediated hepatitis in mice
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Wild type mice [5] |
| Dosage: | 15 mg/kg |
| Administration: | Intravenous injection 0, 10 or 24 h prior to sacrifice |
| Result: | Resulted significant liver injury as demonstrated by serum transaminase levels, inflammatory cell infiltrate, hepatocyte apoptosis, and expression of several cytokines including interleukin 4 (IL4) and interferon gamma (IFNγ) at 10 h and 24 h following administration. |
Appearance
Solid
Source
Streptomyces diastatochromogenes S-45
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
Methanol : 10 mg/mL ( 11.55 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.1546 mL | 5.7731 mL | 11.5461 mL |
| 5 mM | 0.2309 mL | 1.1546 mL | 2.3092 mL |
| 10 mM | 0.1155 mL | 0.5773 mL | 1.1546 mL |
References
- [1] Vaněk, Z., et al. Immunomodulators isolated from microorganisms. Folia Microbiol. 1991. 36:99–111.
- [2] Togashi K, et al. Concanamycin A, a vacuolar type H(+)-ATPase inhibitor, induces cell death in activated CD8(+) CTL. Cytotechnology. 1997 Nov;25(1-3):127-35.
- [3] Eswarappa SM, et al. Folimycin (concanamycin A) inhibits LPS-induced nitric oxide production and reduces surface localization of TLR4 in murine macrophages. Innate Immun. 2008 Feb;14(1):13-24.
- [4] Hines IN, et al. Impaired T cell-mediated hepatitis in peroxisome proliferator activated receptor alpha (PPARα)-deficient mice. Biol Res. 2018 Feb 15;51(1):5.
- [5] Woo JT, et al. Isolation, characterization and biological activities of concanamycins as inhibitors of lysosomal acidification. J Antibiot (Tokyo). 1992 Jul;45(7):1108-16.
Synonyms