Dimethyl lithospermate B
(Synonyms: 丹酚酸B二甲酯,dmLSB) 目录号 : GC38484Dimethyl lithospermate B (dmLSB) 是一种选择性的 Na+ 通道激动剂。Dimethyl lithospermate B 减缓钠电流 (INa) 失活,导致动作电位 (AP) 早期内向电流增加。
Cas No.:875313-64-7
Sample solution is provided at 25 µL, 10mM.
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Dimethyl lithospermate B (dmLSB) is a selective Na+ channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP)[1][2].
[1]. Fish JM, et al. Dimethyl lithospermate B, an extract of Danshen, suppresses arrhythmogenesis associated with the Brugada syndrome. Circulation. 2006 Mar 21;113(11):1393-400. [2]. Yoon JY, et al. A novel Na+ channel agonist, dimethyl lithospermate B, slows Na+ current inactivation and increases action potential duration in isolated rat ventricular myocytes. Br J Pharmacol. 2004 Nov;143(6):765-73.
Cas No. | 875313-64-7 | SDF | |
别名 | 丹酚酸B二甲酯,dmLSB | ||
Canonical SMILES | OC1=C(O)C=CC(C[C@H](C(OC)=O)OC([C@H]2C3=C(/C=C/C(O[C@@H](C(OC)=O)CC4=CC(O)=C(O)C=C4)=O)C=CC(O)=C3O[C@@H]2C5=CC(O)=C(O)C=C5)=O)=C1 | ||
分子式 | C38H34O16 | 分子量 | 746.67 |
溶解度 | Soluble in DMSO | 储存条件 | -20°C, protect from light |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.3393 mL | 6.6964 mL | 13.3928 mL |
5 mM | 0.2679 mL | 1.3393 mL | 2.6786 mL |
10 mM | 0.1339 mL | 0.6696 mL | 1.3393 mL |
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Dimethyl lithospermate B, an extract of Danshen, suppresses arrhythmogenesis associated with the Brugada syndrome
Circulation 2006 Mar 21;113(11):1393-400.PMID:16534004DOI:10.1161/CIRCULATIONAHA.105.601690.
Background: Dimethyl lithospermate B (dmLSB) is an extract of Danshen, a traditional Chinese herbal remedy, which slows inactivation of INa, leading to increased inward current during the early phases of the action potential (AP). We hypothesized that this action would be antiarrhythmic in the setting of Brugada syndrome. Methods and results: The Brugada syndrome phenotype was created in canine arterially perfused right ventricular wedge preparations with the use of either terfenadine or verapamil to inhibit INa and ICa or pinacidil to activate IK-ATP. AP recordings were simultaneously recorded from epicardial and endocardial sites together with an ECG. Terfenadine, verapamil, and pinacidil each induced all-or-none repolarization at some epicardial sites but not others, leading to ST-segment elevation as well as an increase in both epicardial and transmural dispersions of repolarization (EDR and TDR, respectively) from 12.9+/-9.6 to 107.0+/-54.8 ms and from 22.4+/-8.1 to 82.2+/-37.4 ms, respectively (P<0.05; n=9). Under these conditions, phase 2 reentry developed as the epicardial AP dome propagated from sites where it was maintained to sites at which it was lost, generating closely coupled extrasystoles and ventricular tachycardia and fibrillation. Addition of dmLSB (10 micromol/L) to the coronary perfusate restored the epicardial AP dome, reduced EDR and TDR to 12.4+/-18.1 and 24.4+/-26.7 ms, respectively (P<0.05; n=9), and abolished phase 2 reentry-induced extrasystoles and ventricular tachycardia and fibrillation in 9 of 9 preparations. Conclusions: Our data suggest that dmLSB is effective in eliminating the arrhythmogenic substrate responsible for the Brugada syndrome and that it deserves further study as a pharmacological adjunct to implanted cardioverter/defibrillator usage.
Synthesis of a dual-labeled probe of Dimethyl lithospermate B with photochemical and fluorescent properties
Molecules 2011 Nov 28;16(12):9886-99.PMID:22124203DOI:10.3390/molecules16129886.
Dimethyl lithosermate B (DLB) is a highly potent natural antioxidant and antidiabetic polyphenol with unknown mode of action. To determine its cellular targets, a photochemical and fluorescent dimethyl lithopermate B probe was designed and efficiently synthesized. The dual-labeled chemical probe for biological application was evaluated by UV and fluorescence to determine its electrochemical absorption and emission properties. This probe could be valuable for investigating ligand-protein interactions and subcellular localization.
A novel Na+ channel agonist, Dimethyl lithospermate B, slows Na+ current inactivation and increases action potential duration in isolated rat ventricular myocytes
Br J Pharmacol 2004 Nov;143(6):765-73.PMID:15504759DOI:10.1038/sj.bjp.0705969.
Voltage-gated Na(+) channel blockers have been widely used as local anaesthetics and antiarrhythmic agents. It has recently been proposed that Na(+) channel agonists can be used as inotropic agents. Here, we report the identification of a natural substance that acts as a Na(+) channel agonist. Using the patch-clamp technique in isolated rat ventricular myocytes, we investigated the electrophysiological effects of the substances isolated from the root extract of Salvia miltiorrhiza, which is known as 'Danshen' in Asian traditional medicine. By the intensive activity-guided fractionation, we identified Dimethyl lithospermate B (dmLSB) as the most active component, while LSB, which is the major component of the extract, showed negligible electrophysiological effect. Action potential duration (APD(90)) was increased by 20 microM dmLSB from 58.8 +/- 12.1 to 202.3 +/- 9.5 ms. In spite of the prolonged APD, no early after-depolarization (EAD) was observed. dmLSB had no noticeable effect on K(+) or Ca(2+) currents, but selectively affected Na(+) currents (I(Na)). dmLSB slowed the inactivation kinetics of I(Na) by increasing the proportion of slowly inactivating component without inducing any persistent I(Na). The relative amplitude of slow component compared to the peak fast I(Na) was increased dose dependently by dmLSB (EC(50) = 20 microM). Voltage dependence of inactivation was not affected by dmLSB, while voltage dependence of activation shifted by 5 mV to the depolarised direction. Since the APD prolongation by dmLSB did not provoke EAD, which is thought as a possible mechanism for the proarrhythmia seen in other Na(+) channel agonists, dmLSB might be an excellent candidate for a Na(+) channel agonist.
Anti-inflammatory activity of caffeic acid derivatives isolated from the roots of Salvia miltiorrhiza Bunge
Arch Pharm Res 2018 Jan;41(1):64-70.PMID:29124660DOI:10.1007/s12272-017-0983-1.
Ten caffeic acid derivatives (1-10) were isolated from the roots of Salvia miltiorrhiza by using various chromatographic methods and their chemical structures were spectroscopically elucidated. The absolute configurations of chiral centers were determined by comparison with reported coupling constants, optical rotation values, and CD techniques. Anti-inflammatory activities were evaluated using nitric oxide (NO), inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2 inhibition assays, and by determining the expression of heme oxygenase (HO)-1. Two new caffeic acid derivatives, 8-epiblechnic acid 9-methyl ester (4) and 8-epiblechnic acid 9'-methyl ester (5), and eight known derivatives, caffeic acid methyl ester (1), shimobashiric acid B (2), rosmarinic acid methyl ester (3), salvianolic acid C (6), methyl salvianolate C (7), lithospermic acid monomethyl ester (8), lithospermic acid dimethyl ester (9), and Dimethyl lithospermate B (10), were isolated from the ethyl acetate fraction of S. miltiorrhiza. All caffeic acid derivatives were evaluated for their inhibitory effect on NO production. Compounds 2 and 3 inhibited NO production with IC50 values of 1.4 and 0.6 μM, respectively. These compounds also strongly inhibited the production of iNOS and COX-2. In addition, compound 3 induced the expression HO-1 in a concentration-dependent manner at 0.1, 0.3, and 1.0 μM.
[Chemical constituents of Salvia chinensis]
Zhongguo Zhong Yao Za Zhi 2013 May;38(10):1556-9.PMID:23947137doi
Chemical constituents were investigated on the ethyl acetate extract of Salvia chinensis. Compounds were separated and purified by various chromatograhic techniques including silica gel, Sephadex LH-20 and reversed-phase HPLC. Their structures were identified by spectroscopic data analysis. Eleven compounds were isolated and purified and their structures were identified as oresbiusin A(1), ethyl dihydrocaffeate (2), ethyl rosmarinate (3), rosmarinic acid (4), methyl rosmarinate (5), bis (2-ethylhexyl) phthalate (6), salvianol acid C (7), methyl salvianol acid C (8), methyl salvianolate A (9), Dimethyl lithospermate B (10), and salvianolic acid A(11). Except for rosmarinic acid, the remaining compounds were isolated from S. chinensis for the first time.