344270
Forskolin
from Coleus forskohlii, ≥99% (HPLC), crystalline solid, positive inotropic agent, Calbiochem
别名:
佛司可林，毛喉鞘蕊花, 7β-乙酰氧基-8，13-环氧-1α，6β，9-α三羟基-LABD-14-en-11-酮，Colforsin
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关于此项目
经验公式（希尔记法）:
C22H34O7
化学文摘社编号:
分子量:
410.50
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
佛司可林，毛喉鞘蕊花,
description
Merck USA index - 14, 2476
Quality Level
assay
≥99% (HPLC)
form
crystalline solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white to off-white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
10-30°C
SMILES string
O1[C@]2([C@@]([C@@]3([C@@H]([C@@H]([C@@H]2OC(=O)C)O)C(CC[C@@H]3O)(C)C)C)(C(=O)C[C@]1(C)C=C)O)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
General description
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。
Biochem/physiol Actions
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。
Preparation Note
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。
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
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。
毒性：有害（C）
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signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Dermal
存储类别
11 - Combustible Solids
Alex D White et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(13), 7455-7460 (2020-03-19)
cAMP production upon activation of Gs by G protein-coupled receptors has classically been considered to be plasma membrane-delimited, but a shift in this paradigm has occurred in recent years with the identification of several receptors that continue to signal from
Ieva Sutkeviciute et al.
Nature chemical biology, 18(3), 272-280 (2021-12-25)
Class B G protein-coupled receptors (GPCRs) are notoriously difficult to target by small molecules because their large orthosteric peptide-binding pocket embedded deep within the transmembrane domain limits the identification and development of nonpeptide small molecule ligands. Using the parathyroid hormone
Ravneet Jaura et al.
Nature communications, 13(1), 2733-2733 (2022-05-19)
Mammalian genomes comprise largely intergenic noncoding DNA with numerous cis-regulatory elements. Whether and how the size of intergenic DNA affects gene expression in a tissue-specific manner remain unknown. Here we show that genes with extended intergenic regions are preferentially expressed
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 344270-10MG | 07790788049294 |
| 344270-25MG | 04055977215359 |
| 344270-50MG | 04055977215366 |