| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Lacidipine (GX-1048, GR-43659X, SN-305; GX1048, GR43659X, SN305; Caldine, Lacimen, Lacipil, Midotens, Motens) is a potent and 3rd-generation L-type CCB (calcium channel blocker) that has been approved in 1990s for treating high blood pressure.
| ln Vitro |
HKC proliferation is inhibited in vitro by lacidipine (0.01-100 μM; 24 h) in a concentration-dependent manner[1]. By controlling the caspase-3 pathway, lacidipine (0.01-100 μM; 24 h) shields HKCs from apoptosis brought on by ATP depletion and recovery[1].
|
|---|---|
| ln Vivo |
In the apoE-deficient animal, lacedipine (0.3, 1.0, 3.0 mg/kg; po; once daily for 10 weeks) decreases plasma endothelin concentrations and exhibits anti-atherogenic properties[2].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HKC cells Tested Concentrations: 0.01-100 μM Incubation Duration: 24 h Experimental Results: demonstrated anti-proliferative activity in a concentration-dependent manner. Apoptosis Analysis[1] Cell Types: HKC cells (renal ischemia reperfusion (I/R) model) Tested Concentrations: 1, 10 μM Incubation Duration: 24 h Experimental Results: AA-induced HKC cells apoptosis, with proportion of early apoptotic cells of 1.47% and 0.30% for 1 and 10 μM dosage, respectively. Western Blot Analysis[1] Cell Types: HKC cells (renal ischemia reperfusion (I/R) model) Tested Concentrations: 1, 10 μM Incubation Duration: 24 h (pretreat) Experimental Results: diminished the expression of cyt c of injured cells following ATP depletion and recovery. Dramatically increased the expression of the Bcl-2 protein, but diminished the Bax protein. |
| Animal Protocol |
Animal/Disease Models: Female C57BL/6 mice (Homozygous ; apoE-deficient; atherosclerosis model)[2].
Doses: 0.3, 1.0, 3.0 mg/kg Route of Administration: po (oral gavage); single daily for 10 weeks. Experimental Results: Induced a significant dose-dependent decrease in plasma endothelin levels. Dramatically decreased the mean lesion area in a dose-related manner by 10, 17 and 53% for 0.3, 1.0, 3.0 mg/kg, respectively. |
| References |
[1]. Zhang A, et al. Lacidipine attenuates apoptosis via a caspase-3 dependent pathway in human kidney cells. Cell Physiol Biochem. 2013;32(4):1040-9.
[2]. Cristofori P, et al. The calcium-channel blocker lacidipine reduces the development of atherosclerotic lesions in the apoE-deficient mouse. J Hypertens. 2000 Oct;18(10):1429-36. |
| Molecular Formula |
C26H33NO6
|
|
|---|---|---|
| Molecular Weight |
455.54
|
|
| CAS # |
103890-78-4
|
|
| Related CAS # |
Lacidipine-13C8;1261432-01-2
|
|
| SMILES |
O(C([H])([H])C([H])([H])[H])C(C1=C(C([H])([H])[H])N([H])C(C([H])([H])[H])=C(C(=O)OC([H])([H])C([H])([H])[H])C1([H])C1=C([H])C([H])=C([H])C([H])=C1/C(/[H])=C(\[H])/C(=O)OC(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.49 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 (5.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1952 mL | 10.9760 mL | 21.9520 mL | |
| 5 mM | 0.4390 mL | 2.1952 mL | 4.3904 mL | |
| 10 mM | 0.2195 mL | 1.0976 mL | 2.1952 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
COA