Concanamycin A (Folimycin; Antibiotic X 4357B) 是一种大环内酯类抗生素，是空泡状 H+-ATP 酶 (V-ATPase) 抑制剂。Concanamycin A 是一种溶酶体酸化抑制剂，可用于 T 细胞介导的炎症研究。
| 生物活性 | Concanamycin A (Folimycin;AntibioticX 4357B) is amacrolideantibiotic, avacuolar 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]. |
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体外研究
(In Vitro) | Concanamycin A can come fromS. diastatochromogenes545, 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 (IC50=0.061 nM), and inhibits oleate incorporation into cholesteryl ester (IC50=14 nM)[4].
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. |
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体内研究
(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].
| 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. |
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| 来源 | Streptomyces diastatochromogenes S-45 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: Methanol : 10 mg/mL(11.55 mM;Need ultrasonic and warming) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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