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| 25mg |
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| Targets |
L‑type calcium channels in ventricular myocytes of guinea pig [1].
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| ln Vitro |
Heteroclitin D at 1 μmol/L decreased the L‑type calcium current from (770±155) pA to (482±104) pA (n=6 cells from 3 guinea pigs, P<0.05) [1].
Heteroclitin D at 10 μmol/L decreased the L‑type calcium current from (770±155) pA to (384±85) pA (n=6 cells from 3 guinea pigs, P<0.01) [1]. The maximal inhibitory rates of Heteroclitin D on L‑type calcium current were 37.45% at 1 μmol/L and 50.05% at 10 μmol/L, as determined from current‑voltage relationship experiments (holding potential −40 mV, depolarizing steps from −40 to +60 mV in 10 mV increments, step pulse 500 ms) [1]. Heteroclitin D (10 μmol/L) did not affect the steady‑state activation curve of L‑type calcium channels, but it significantly altered the steady‑state inactivation curve: the half inactivation voltage (V₀.₅) changed from −22.7 mV to −40.9 mV, and the slope factor (κ) changed from 10.2 to 20.6 (n=4 cells from 3 guinea pigs, P<0.05) [1]. |
| Cell Assay |
Single ventricular myocytes were isolated from adult guinea pigs by enzymatic disaggregation. Only rod‑shaped cells with clear striations were used. Whole‑cell patch‑clamp recording was performed with microelectrodes (resistance 3–4 MΩ when filled with intracellular solution). After gigaseal formation and membrane rupture, the test solution was switched to a Na⁺‑free solution (Na⁺ substituted by TEA‑Cl). Calcium current was recorded using an amplifier and software. Capacitive transients and series resistance were compensated, and linear leakage currents were subtracted using the p/4 protocol. The holding potential was −40 mV, and a step pulse to 0 mV at 1 Hz was applied to evoke inward calcium current. For current‑voltage relationship, membrane potential was depolarized from −40 to +60 mV in 10 mV increments, with step pulse duration of 500 ms. For inactivation curves, the holding potential was −80 mV, conditioning potentials from −80 to +20 mV in 10 mV steps were applied, followed by a test potential at 0 mV. Heteroclitin D at 1 and 10 μmol/L was added to the perfusate, and the effects on calcium current were measured within 10 min (low concentration) and 20 min (high concentration) to distinguish drug effects from the “run‑down” phenomenon [1].
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| References | |
| Additional Infomation |
Heteroclitin D is a tannin. It has been reported that Heteroclitin D exists in Schisandra chinensis (Kadsura interior), Schisandra heteroclita, and Schisandra rubriflora, and relevant data are available.
Heteroclitin D is one of two lignans (the other is gomisin J) from Kadsura medicinal plants with higher biological activities. The compound blocks L‑type calcium channels by accelerating channel inactivation, suggesting high affinity to the inactivated state. Unlike existing calcium channel blockers, Heteroclitin D also possesses anti‑lipid peroxidative activity, which may be potentially useful for treating ischemic heart disease and atherosclerosis [1]. |
| Molecular Formula |
C27H30O8
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|---|---|
| Molecular Weight |
482.5223
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| Exact Mass |
482.194
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| CAS # |
140369-76-2
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| PubChem CID |
10367978
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| Appearance |
Off-white to light yellow solid
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
640.3±55.0 °C at 760 mmHg
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| Flash Point |
273.3±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.598
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| LogP |
5.66
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
995
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O1C2C3=C(C([H])=C4[C@@]([H])([C@]([H])(C([H])([H])[H])[C@]([H])(C([H])([H])[H])C([H])([H])C5=C([H])C(=C(C([C@]5(C1([H])[H])C4=2)=O)OC([H])([H])[H])OC([H])([H])[H])OC(C(=C([H])C([H])([H])[H])C([H])([H])[H])=O)OC([H])([H])O3
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| InChi Key |
CGWKMZYZZCWGCK-YSKMNHBWSA-N
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| InChi Code |
InChI=1S/C27H30O8/c1-7-13(2)26(29)35-21-15(4)14(3)8-16-9-18(30-5)23(31-6)25(28)27(16)11-32-24-20(27)17(21)10-19-22(24)34-12-33-19/h7,9-10,14-15,21H,8,11-12H2,1-6H3/b13-7-/t14-,15-,21-,27+/m1/s1
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| Chemical Name |
[(1S,12R,13R,14R)-18,19-dimethoxy-13,14-dimethyl-20-oxo-3,6,8-trioxapentacyclo[9.9.1.01,16.04,21.05,9]henicosa-4(21),5(9),10,16,18-pentaen-12-yl] (Z)-2-methylbut-2-enoate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~103.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.18 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0725 mL | 10.3623 mL | 20.7245 mL | |
| 5 mM | 0.4145 mL | 2.0725 mL | 4.1449 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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