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Merck
CN

5.08409

巴弗洛霉素A1

≥90% (HPLC), liquid,V-ATPase inhibitor

别名:

InSolution 巴弗洛霉素 A1, InSolution 巴弗洛霉素 A1，≥97% HPLC测定

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关于此项目

经验公式（希尔记法）:
C35H58O9
化学文摘社编号:
88899-55-2
分子量:
622.83
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD06795130

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产品名称

巴弗洛霉素A1, InSolution, ≥90%, A macrolide antibiotic that acts as a specific inhibitor of vacuolar-type H+-ATPase

SMILES string

O1[C@@H]([C@H]([C@@H](C[C@]1(O)[C@H]([C@H](O)[C@@H]([C@H]2OC(=O)\C(=C\C(=C\[C@H]([C@H]([C@H](C\C(=C\C=C\[C@@H]2OC)\C)C)O)C)\C)\OC)C)C)O)C)C(C)C

InChI

1S/C35H58O9/c1-19(2)32-24(7)27(36)18-35(40,44-32)26(9)31(38)25(8)33-28(41-10)14-12-13-20(3)15-22(5)30(37)23(6)16-21(4)17-29(42-11)34(39)43-33/h12-14,16-17,19,22-28,30-33,36-38,40H,15,18H2,1-11H3/b14-12+,20-13+,21-16+,29-17-/t22-,23+,24-,25-,26-,27+,28-,30-,31+,32+,33+,35+/m0/s1

InChI key

XDHNQDDQEHDUTM-JQWOJBOSSA-N

assay

≥90% (HPLC)

form

liquid

shelf life

2 yr

Quality Level

100

storage condition

OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light

storage temp.

−20°C

相关类别

Packaging

用惰性气体包装

Biochem/physiol Actions

主要靶标
液泡型H+-ATP酶
细胞可渗透性：具有

Disclaimer

毒性：标准处理（A）

General description

一种大环内酯类抗生素，可作为液泡型H+-ATP酶（V型；Ki=0.5 nM）的特异性抑制剂，是区分不同类型ATP酶的有价值的工具。据报告，可选择性地抑制β-分泌酶，这是一种参与淀粉样蛋白前体蛋白（APP）加工的酶。阻断巨噬细胞中的溶酶体胆固醇运输。已知会干扰脑细胞中的pH值调节。抑制体内和体外的骨吸收。在细胞活率测定中，已对多种细胞系具有细胞毒性作用。

Other Notes

Sinha, S., and Lieberburg, I. 1999.Proc.Natl.Acad.Sci. USA96, 11049.
Calvert, C.M., and Sanders, D. 1995.J. Biol. Chem.270, 7272.
Nishihara, T., et al. 1995.Biochem.Biophys.Res. Commun.269, 255.
Crider, B.P., et al. 1994.J. Biol. Chem.269, 17379.
Palokangas, H., et al. 1994.J. Biol. Chem.269, 17577.
Sundquist, K.T., and Marks, S.C., Jr. 1994.J. Bone Miner.Res.9, 1575.
Drose, S., et al. 1993.Biochemistry32, 3902.
Furuchi, T., et al. 1993.J. Biol. Chem.268, 27345.
Bowman, E.J., et al. 1988.Proc.Natl.Acad.Sci. USA85, 7972.

Preparation Note

初次融化后，等分并冷冻（-20°C）。等分试样在-20°C下可稳定保存1年。仅使用新鲜的DMSO进行进一步稀释。

存储类别

10 - Combustible liquids

wgk

WGK 1

flash_point_f

188.6 °F - (refers to pure substance)

flash_point_c

87 °C - (refers to pure substance)

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S Sinha et al.
Proceedings of the National Academy of Sciences of the United States of America, 96(20), 11049-11053 (1999-09-29)
The major constituent of senile plaques in Alzheimer's disease is a 42-aa peptide, referred to as beta-amyloid (Abeta). Abeta is generated from a family of differentially spliced, type-1 transmembrane domain (TM)-containing proteins, called APP, by endoproteolytic processing. The major, relatively
K T Sundquist et al.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research, 9(10), 1575-1582 (1994-10-01)
It has been shown that a specific inhibitor of vacuolar H(+)-ATPases, bafilomycin A1, inhibits bone resorption by isolated chicken osteoclasts by blocking the proton pump in the ruffled border membrane. We report here the effects of bafilomycin A1 on bone
T Furuchi et al.
The Journal of biological chemistry, 268(36), 27345-27348 (1993-12-25)
Certain steroids having an oxo group at the C-17 or C-20 position such as pregnenolone and dehydroisoandrosterone inhibit the cholesterol transport from lysosomes to other cellular sites. Taking advantage of the fact that the inhibition is reversed upon removal of
B P Crider et al.
The Journal of biological chemistry, 269(26), 17379-17381 (1994-07-01)
Vacuolar-type proton-translocating ATPases are complex heterooligomers that are characterized by a specific inhibition by bafilomycin A1. These enzymes have a peripheral ATP hydrolytic domain as well as a transmembranous sector. The transmembranous sector has been isolated by glycerol gradient centrifugation
H Palokangas et al.
The Journal of biological chemistry, 269(26), 17577-17585 (1994-07-01)
Bafilomycin A1 (Baf), a specific inhibitor of the vacuolar-type proton pump, inhibited the entry of Semliki Forest virus and vesicular stomatitis virus into BHK-21 cells. The inhibition occurred at concentrations that dissipated intracellular acidic compartments. Viral infection was totally inhibited
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