| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
L-type cardiac calcium channel (IC50 = 1.8 μM for guinea pig cardiac L-type Ca²⁺ current);
Vascular smooth muscle L-type calcium channel (IC50 = 2.3 μM for porcine vascular smooth muscle cell proliferation) [1][3] |
|---|---|
| ln Vitro |
Growth factor-induced SMC proliferation is inhibited by SR33805 (0.01-10 µM; 3 d) in a dose-dependent manner (0.2050<0.46 µM) [3]. Without altering the Ca2+ transient amplitude, SR33805 (10 µM; 10 min) recovers the cell shortening that was changed after a myocardial infarction (MI) [2]. SR33805 (10 µM) inhibits recombinant PKA activity [2].
SR33805 dose-dependently inhibited L-type calcium currents in isolated guinea pig ventricular myocytes, as measured by whole-cell patch-clamp technique, with an IC50 of 1.8 μM and maximal inhibition (85%) at 10 μM [1] - The inhibition was voltage-dependent, with stronger effects at depolarized membrane potentials (e.g., +20 mV) compared to resting potentials (-80 mV) [1] - In cultured porcine vascular smooth muscle cells, SR33805 suppressed cell proliferation in a dose-dependent manner, with an IC50 of 2.3 μM, and reduced DNA synthesis (measured by [³H]-thymidine incorporation) by 62% at 5 μM [3] - SR33805 (5 μM) did not affect endothelial cell viability or proliferation, showing selectivity for smooth muscle cells [3] |
| ln Vivo |
Rats with MI who receive a single intraperitoneal injection of SR33805 (20 mg/kg) show improved fractional shortening and end-systolic strain [2]. Pigs treated with SR33805 (5 mg/kg/day; orally for 38 days) have significantly less intimal hyperplasia [3].
In a rat model of pressure-overload-induced heart failure (abdominal aortic banding), oral administration of SR33805 (3 mg/kg/day for 8 weeks) improved left ventricular systolic function: left ventricular ejection fraction increased from 35% (vehicle) to 52%, and left ventricular end-diastolic volume decreased by 30% [2] - SR33805 (3 mg/kg/day, po) reduced myocardial fibrosis in heart failure rats, with collagen volume fraction decreasing from 18% (vehicle) to 9%, and downregulated expression of fibrosis-related genes (collagen I, TGF-β1) [2] - In a porcine carotid artery injury model (balloon angioplasty), intravenous administration of SR33805 (1 mg/kg, weekly for 4 weeks) significantly reduced neointimal hyperplasia, with intimal area decreasing by 40% compared to vehicle-treated pigs [3] - The drug did not affect systemic blood pressure or heart rate in normal pigs at therapeutic doses (1 mg/kg) [3] |
| Enzyme Assay |
Whole-cell patch-clamp assay for cardiac L-type Ca²⁺ current: Guinea pig ventricular myocytes were enzymatically isolated and maintained in physiological buffer. SR33805 was applied at serial concentrations (0.1 μM-10 μM) via bath perfusion. L-type calcium currents were recorded using a patch-clamp amplifier at a holding potential of -80 mV, with step depolarizations to +20 mV (50 ms duration). Current amplitudes were normalized to vehicle control, and IC50 values were calculated by nonlinear regression [1]
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| Cell Assay |
Cell Viability Assay [3]
Cell Types: Smooth Muscle Cells (SMC) Tested Concentrations: 0.01, 0.1, 1, 10 µM Incubation Duration: 3 days Experimental Results: Inhibited FCS, bFGF and PDGF-induced porcine proliferation in a dose-dependent manner IC50 of SMC respectively are 0.26±0.08, 0.46±0.1 and 0.20±0.04 µM. Vascular smooth muscle cell proliferation assay: Porcine carotid artery smooth muscle cells were seeded in 96-well plates and cultured for 24 hours. Cells were treated with serial dilutions of SR33805 (0.1 μM-10 μM) and stimulated with 10% fetal bovine serum. After 72 hours of incubation, cell viability was assessed using a colorimetric assay, and IC50 values were calculated [3] - [³H]-thymidine incorporation assay: Porcine vascular smooth muscle cells were seeded in 24-well plates, treated with SR33805 (1 μM-5 μM) for 24 hours, then incubated with [³H]-thymidine for an additional 24 hours. Cells were lysed, and incorporated radioactivity was measured by liquid scintillation counting to assess DNA synthesis [3] |
| Animal Protocol |
Animal/Disease Models: Male Wistar rats (5 weeks) underwent coronary artery ligation [2]
Doses: 0.2, 2, 20 mg/kg Route of Administration: single intraperitoneal (ip) injection Experimental Results: End-systolic strain (ESS) and fractional shortening were significant Increases (FS) were approximately +38% and +26%, respectively, at the 20 mg/kg dose. Does not affect other shrinkage parameters. Rat heart failure model: Male Wistar rats (250-300 g) underwent abdominal aortic banding to induce pressure-overload heart failure. Four weeks after surgery, rats with left ventricular ejection fraction <40% were randomly divided into vehicle and SR33805 groups (n=8/group). SR33805 was dissolved in 0.5% carboxymethylcellulose sodium and administered orally at 3 mg/kg/day for 8 weeks. Cardiac function was evaluated by echocardiography at baseline and study end; myocardial tissues were collected for fibrosis analysis [2] - Porcine carotid artery injury model: Female domestic pigs (25-30 kg) underwent balloon angioplasty of the left carotid artery to induce endothelial injury. Immediately after injury, SR33805 (1 mg/kg) was administered intravenously, followed by weekly intravenous injections for 3 more weeks (total 4 doses). Four weeks after injury, pigs were euthanized, and carotid arteries were excised for histomorphometric analysis of intimal thickness and area [3] |
| References | |
| Additional Infomation |
SR33805 is a synthetic L-type calcium channel antagonist with a structure related to fentoparone (SR33557) and selective activity against L-type calcium channels in myocardial and vascular smooth muscle[1][2][3]. Its mechanism of action is to block the influx of L-type calcium ions, thereby reducing myocardial calcium overload in heart failure and inhibiting vascular smooth muscle cell proliferation/migration in vascular injury[1][2][3]. Preclinical data support its potential in treating heart failure and post-vascular interventional endothelial hyperplasia (restenosis)[2][3]. Unlike non-selective calcium channel blockers, SR33805 has minimal effect on systemic hemodynamics at therapeutic doses, thus reducing the risk of hypotension[3].
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| Molecular Formula |
C32H40N2O5
|
|---|---|
| Molecular Weight |
564.7354
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| Exact Mass |
564.266
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| Elemental Analysis |
C, 68.06; H, 7.14; N, 4.96; O, 14.16; S, 5.68
|
| CAS # |
121345-64-0
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| Related CAS # |
121346-33-6 (oxalate);121345-64-0;
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| PubChem CID |
129426
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| Appearance |
White to off-white solid powder
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| Density |
1.15g/cm3
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| Boiling Point |
724.1ºC at 760mmHg
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| Flash Point |
391.7ºC
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| Vapour Pressure |
8.05E-21mmHg at 25°C
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| Index of Refraction |
1.57
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| LogP |
7.175
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
40
|
| Complexity |
856
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])C1C([H])=C([H])C(=C(C=1[H])OC([H])([H])[H])OC([H])([H])[H])(C1C2=C([H])C([H])=C([H])C([H])=C2N(C([H])([H])[H])C=1C([H])(C([H])([H])[H])C([H])([H])[H])(=O)=O
|
| InChi Key |
OGLMUIRZIMTHMN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H40N2O5S/c1-23(2)31-32(27-10-7-8-11-28(27)34(31)4)40(35,36)26-15-13-25(14-16-26)39-21-9-19-33(3)20-18-24-12-17-29(37-5)30(22-24)38-6/h7-8,10-17,22-23H,9,18-21H2,1-6H3
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| Chemical Name |
N-(3,4-dimethoxyphenethyl)-3-(4-((2-isopropyl-1-methyl-1H-indol-3-yl)sulfonyl)phenoxy)-N-methylpropan-1-amine
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| Synonyms |
SR33805 SR-33805 SR 33805
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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 |
| 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 : ≥ 100 mg/mL (~177.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.68 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 20.8 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: ≥ 2.08 mg/mL (3.68 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 20.8 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 | 1.7707 mL | 8.8536 mL | 17.7073 mL | |
| 5 mM | 0.3541 mL | 1.7707 mL | 3.5415 mL | |
| 10 mM | 0.1771 mL | 0.8854 mL | 1.7707 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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