product name
佛司可林，毛喉鞘蕊花,
检测方案
≥99% (HPLC)
质量水平
形式
crystalline solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
white to off-white
溶解性
DMSO: 5 mg/mL
运输
ambient
储存温度
10-30°C
InChI
1S/C22H34O7/c1-8-19(5)11-14(25)22(27)20(6)13(24)9-10-18(3,4)16(20)15(26)17(28-12(2)23)21(22,7)29-19/h8,13,15-17,24,26-27H,1,9-11H2,2-7H3/t13-,15-,16-,17-,19-,20-,21+,22-/m0/s1
InChI key
OHCQJHSOBUTRHG-KGGHGJDLSA-N
一般描述
从印度植物毛喉鞘蕊花中分离出的主要细胞渗透性二萜。在低剂量时，它用作正性肌力药。在较高剂量下，由于其作为平滑肌肉松弛药的作用，因此可作为低血压和血管舒张剂。在有效剂量下未观察到主要副作用。毛喉素的药理活性是由于其激活腺苷酸环化酶（EC50 = 4 µM），导致cAMP水平升高。毛喉素正性肌力效应的确切机制尚不清楚，但可能与cAMP依赖性Na+通透性增加有关，导致Ca2+释放间接增加。抑制大鼠肾系膜细胞中的MAP激酶（IC50 = 25 µM）。还充当Hh途径拮抗剂。显示抑制小脑颗粒细胞中的凋亡，并诱导静息人B淋巴细胞中的凋亡。
从印度植物毛喉鞘蕊花中分离出的具有心脏活性的二萜。在低剂量时，在狗、猫、自发性高血压和正常大鼠以及离体豚鼠心脏中用作正性肌力药。在较高剂量下，由于其作为平滑肌肉松弛药的作用，因此可作为低血压和血管舒张剂。在有效剂量下未观察到主要副作用。膜和完整细胞中腺苷酸环化酶（EC50 = 4 µM）的快速可逆激活剂。不影响鸟苷酸环化酶或环核苷酸磷酸二酯酶的活性。毛喉素′正性肌力效应的确切机制尚不清楚，但可能与cAMP依赖性Na+通透性增加有关，导致Ca2+释放间接增加。抑制大鼠肾系膜细胞中的MAP激酶（IC50 = 25 µM）。还充当Hh途径拮抗剂。显示抑制小脑颗粒细胞中的凋亡，并诱导静息人B淋巴细胞中的凋亡。
生化/生理作用
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：25 µM，抑制大鼠肾系膜细胞中的MAP激酶；腺苷酸环化酶激活的EC50 = 4 µM。
注意
据报道，乙醇抑制毛喉素介导的腺苷酸环化酶的活化。DMSO为推荐溶剂；在DMSO终浓度为≤5%时，几乎不会抑制腺苷酸环化酶的活化。
警告
毒性：有害（C）
重悬
在复溶后存放于冰箱（4°C）。DMSO储备液可在4°C下稳定保存4个月。
其他说明
D′Orazio, J.A., et al. 2006.Nature443, 340.
Noveen, A., et al. 1996.Biochem.Biophys.Res. Commun.219, 180.
Galli, C., et al. 1995.J. Neurosci.15, 1172.
Li, X., et al. 1995.Am. J. Physiol.269, C986.
Lomo, J., et al. 1995.J. Immunol.154, 1634.
Uneyama, H., et al. 1993.J. Biol. Chem.268, 168.
Laurenza, A., et al. 1989.Trends Pharmacol.Sci.10, 442.
Adashi, E.Y., and Resnick, C.E.1986.J. Cell.Biochem.31, 217.
Seamon, K.B., and Daly, J.W.1986.Adv.Cyclic Nucleotide Protein Phosphorylation Res.20, 1.
Huang, R., et al. 1982.Cyclic Nucleotide Res.8, 385.
Metzger, H., and Lindner, E. 1981.IRCS Med. Sci. Biochem.Cardiovasc.System Pharmacol.9, 99.
Noveen, A., et al. 1996.Biochem.Biophys.Res. Commun.219, 180.
Galli, C., et al. 1995.J. Neurosci.15, 1172.
Li, X., et al. 1995.Am. J. Physiol.269, C986.
Lomo, J., et al. 1995.J. Immunol.154, 1634.
Uneyama, H., et al. 1993.J. Biol. Chem.268, 168.
Laurenza, A., et al. 1989.Trends Pharmacol.Sci.10, 442.
Adashi, E.Y., and Resnick, C.E.1986.J. Cell.Biochem.31, 217.
Seamon, K.B., and Daly, J.W.1986.Adv.Cyclic Nucleotide Protein Phosphorylation Res.20, 1.
Huang, R., et al. 1982.Cyclic Nucleotide Res.8, 385.
Metzger, H., and Lindner, E. 1981.IRCS Med. Sci. Biochem.Cardiovasc.System Pharmacol.9, 99.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Dermal
WGK
WGK 3
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