| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Allocryptopine is an alkaloid extracted from Corydalis decumbens. In this study, it modulates cardiac ion channels, specifically reducing th
|
|---|---|
| ln Vitro |
Inhibition of Delayed Afterdepolarizations and Triggered Activities: In isolated mouse ventricular myocytes treated with isoproterenol (ISO, 30 nM) to induce arrhythmogenic activity, treatment with 10 μM Allocryptopine significantly reduces the incidence of delayed afterdepolarizations and triggered activities. Under 5.0 Hz pacing, DAD incidence drops from 20% (ISO-only) to 9% (ISO + ALL), and TA incidence drops from 12% (ISO-only) to 4% (ISO + ALL) [1].
Frequency-Dependent Effect: The suppressive effect of Allocryptopine on DADs and TAs is rate-dependent, with stronger inhibitory effects observed at higher stimulation frequencies (e.g., 4.0 and 5.0 Hz) [1]. Reduction of Transient Inward Current: Allocryptopine (10 μM) significantly reduces the ISO-induced increase in transient inward current density. The peak Iti density is reduced from -2.38 ± 0.08 pA/pF in ISO-treated myocytes to -1.21 ± 0.14 pA/pF in myocytes co-treated with ISO and ALL (p < 0.05). This effect is most prominent at a test potential of -60 mV [1]. Reduction of L-type Calcium Current: Allocryptopine (10 μM) significantly reduces the ISO-induced increase in ICa,L density. At a test potential of 0 mV, ICa,L density is -15.5 ± 0.3 pA/pF in ISO-treated myocytes and is reduced to -10.3 ± 0.4 pA/pF in myocytes co-treated with ISO and ALL (p < 0.01). The inhibition is concentration-dependent with an IC50 of 16.08 ± 1.23 μM and a Hill coefficient of 0.84 [1]. Modulation of ICa,L Gating Kinetics: Allocryptopine reverses the ISO-induced changes in ICa,L gating. It shifts the steady-state activation curve to a more positive potential and the steady-state inactivation curve to a more negative potential, effectively counteracting the effects of ISO. It also prolongs the time constant of recovery from inactivation, slowing the channel's recovery. The recovery time constant is 312 ± 16 ms in ISO-treated cells and increases to 545 ± 22 ms in cells co-treated with ISO and ALL (p < 0.01) [1]. |
| Cell Assay |
Isolation of Mouse Ventricular Myocytes: Ventricular myocytes were isolated from mice using an established enzymatic digestion protocol. Cells were plated on laminin-coated dishes. Only quiescent, Ca2+-tolerant, and rod-shaped cells were used for experiments [1].
Patch-Clamp Recordings: Transmembrane action potentials and currents were recorded using the whole-cell patch-clamp technique with a MultiClamp 700B amplifier. Data were sampled at 10 kHz and filtered at 5 kHz. Patch pipettes had resistances of 2-5.5 MΩ. Series resistance was compensated by >80% [1]. Action Potential and DAD/TA Recording: Action potentials were induced by 30 trains of suprathreshold current pulses (1.5 nA, 3 ms) at frequencies of 1.0, 2.0, 3.0, 4.0, and 5.0 Hz under current clamp. DADs were defined as a depolarization >5 mV for >10 ms during diastole. TAs were defined as spontaneous action potentials arising from DADs [1]. Transient Inward Current Recording: To record Iti, 20 conditioning pulses (from -80 mV to +50 mV, 150 ms each) were applied, followed by 2s test pulses from -100 mV to +30 mV in 10 mV increments. Iti amplitude was measured as the difference between the peak and the base of the transient current [1]. L-type Calcium Current Recording: To isolate ICa,L, Na+ current was inhibited with 0.05 mM TTX and K+ current with 5.0 mM CsCl in the extracellular solution. ICa,L was elicited by 200 ms depolarizing pulses from a holding potential of -40 mV to test potentials ranging from -40 mV to +60 mV in 10 mV steps. Current-voltage relationships, steady-state activation/inactivation curves, and recovery from inactivation were analyzed [1]. |
| References |
|
| Additional Infomation |
Isocryptine is a dibenzo[a]azine heterocyclic alkaloid, belonging to the organic heterotetracyclic compounds, tertiary amine compounds, cyclic ketones, cyclic acetals, and aromatic ethers. It has been reported to exist in Corydalis solida, Corydalis ternata, and other organisms with relevant data. See also: Root (part) of Sanguinaria canadensis.
Allocryptopine is an alkaloid derived from Corydalis decumbens (Thunb.) Pers. Papaveraceae. It is a derivative of tetrahydropalmatine. Previous studies have indicated that it has antiarrhythmic effects in various animal models, which were thought to be due to its ability to prolong the action potential duration. This study reveals a more specific mechanism: it suppresses triggered arrhythmias by reducing ISO-induced DADs and TAs. This effect is achieved through the inhibition of ICa,L and the subsequent reduction of Iti, as well as potentially through a direct blocking effect on Iti itself. By modulating these ion currents, Allocryptopine shows potential as an agent for treating triggered arrhythmias, particularly those associated with conditions of calcium overload such as heart failure [1]. |
| Molecular Formula |
C21H23NO5
|
|---|---|
| Molecular Weight |
369.4110
|
| Exact Mass |
369.157
|
| Elemental Analysis |
C, 68.28; H, 6.28; N, 3.79; O, 21.65
|
| CAS # |
485-91-6
|
| PubChem CID |
98570
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
552.7±50.0 °C at 760 mmHg
|
| Flash Point |
288.1±30.1 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.574
|
| LogP |
3.64
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
27
|
| Complexity |
529
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C([H])([H])OC2=C1C([H])=C1C(=C2[H])C(C([H])([H])C2C([H])=C([H])C(=C(C=2C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])OC([H])([H])[H])OC([H])([H])[H])=O
|
| InChi Key |
HYBRYAPKQCZIAE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H23NO5/c1-22-7-6-14-9-19-20(27-12-26-19)10-15(14)17(23)8-13-4-5-18(24-2)21(25-3)16(13)11-22/h4-5,9-10H,6-8,11-12H2,1-3H3
|
| Chemical Name |
7,8-dimethoxy-11-methyl-17,19-dioxa-11-azatetracyclo[12.7.0.04,9.016,20]henicosa-1(21),4(9),5,7,14,16(20)-hexaen-2-one
|
| Synonyms |
Allocryptopine
|
| HS Tariff Code |
2934.99.03.00
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~135.35 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (6.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7070 mL | 13.5351 mL | 27.0702 mL | |
| 5 mM | 0.5414 mL | 2.7070 mL | 5.4140 mL | |
| 10 mM | 0.2707 mL | 1.3535 mL | 2.7070 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
