| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
β2AR
β2-adrenergic receptor (β2AR). Todralazine hydrochloride is a β2AR blocker. |
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| ln Vitro |
In vitro, Todralazine hydrochloride acts as a β2AR antagonist with peripheral vasodilator activity. It possesses antioxidant and free radical scavenging activities. The compound is used in anti-hypertensive research.
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| ln Vivo |
In vivo, Todralazine hydrochloride is an antihypertensive agent that lowers blood pressure. Administration of todralazine (5 µM) to pre-larval zebrafish led to hematopoietic cell expansion and protection from ionizing radiation. The compound has some central nervous system depressant effects.
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| Enzyme Assay |
Non-cell receptor binding assays for Todralazine hydrochloride are performed using membrane preparations from cells expressing β2-adrenergic receptors. Radioligand binding studies are conducted using [³H]dihydroalprenolol ([³H]DHA) or [¹²⁵I]iodocyanopindolol as tracers. Membranes are incubated with the radioligand and varying concentrations of Todralazine (0.001-100 μM). Nonspecific binding is determined with excess propranolol. After incubation at 25°C for 60 minutes, bound and free ligand are separated by filtration, and radioactivity is counted. Ki values are calculated from competition curves.
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| Cell Assay |
Cellular assays for Todralazine hydrochloride are performed using cells expressing β2-AR (e.g., HEK-293 or CHO cells). Cells are treated with Todralazine at concentrations ranging from 0.01-100 μM. Inhibition of isoproterenol-induced cAMP accumulation is measured using HTRF or ELISA assays. IC₅₀ values for receptor blockade are calculated from dose-response curves. Antioxidant activity is assessed by DPPH or ABTS radical scavenging assays.
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| Animal Protocol |
In vivo animal studies are conducted in rodent models of hypertension. Todralazine hydrochloride is administered orally or intraperitoneally at doses determined from pharmacokinetic studies. Blood pressure is measured by tail-cuff or telemetry. In zebrafish studies, todralazine (5 µM) is administered to pre-larval zebrafish to assess hematopoietic cell expansion and protection from ionizing radiation.
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| ADME/Pharmacokinetics |
Todralazine hydrochloride has a molecular weight of 268.7 and a molecular formula of C11H13ClN4O2. It is also known as Ecarazine hydrochloride. The compound is a β2AR blocker with antioxidant activity.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Todralazine hydrochloride are limited. As a β2AR blocker, potential adverse effects may include those associated with beta-blockade. No significant organ-specific toxicity has been reported at effective doses. Standard safety pharmacology studies would be required for therapeutic development.
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| References | |
| Additional Infomation |
An antihypertensive drug with both central and peripheral effects; it also has some central nervous system depressant effects. See also: Todralazine (note moved to).
Todralazine hydrochloride (Ecarazine hydrochloride) is an antihypertensive agent and a β2-adrenergic receptor blocker. It has peripheral vasodilator activity and antioxidant properties. Todralazine hydrochloride is used in anti-hypertensive research. |
| Molecular Formula |
C11H13CLN4O2
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|---|---|
| Molecular Weight |
268.69952
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| Exact Mass |
268.073
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| Elemental Analysis |
C, 49.17; H, 4.88; Cl, 13.19; N, 20.85; O, 11.91
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| CAS # |
3778-76-5
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| Related CAS # |
Todralazine; 14679-73-3
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| PubChem CID |
19604
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| Appearance |
White to off-white solid powder
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| Density |
1.328g/cm3
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| LogP |
2.968
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
262
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.CCOC(NNC1=NN=CC2=CC=CC=C12)=O
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| InChi Key |
OMCOKCNIYWULQH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12N4O2.ClH/c1-2-17-11(16)15-14-10-9-6-4-3-5-8(9)7-12-13-10;/h3-7H,2H2,1H3,(H,13,14)(H,15,16);1H
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| Chemical Name |
ethyl N-(phthalazin-1-ylamino)carbamate;hydrochloride
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| Synonyms |
Todralazine hydrochloride; Todralazine HCl
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| HS Tariff Code |
2934.99.03.00
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ~125 mg/mL (~465.2 mM)
H2O: ~14.29 mg/mL (~53.2 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.74 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 (7.74 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 20.8 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: ≥ 2.08 mg/mL (7.74 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 | 3.7216 mL | 18.6081 mL | 37.2162 mL | |
| 5 mM | 0.7443 mL | 3.7216 mL | 7.4432 mL | |
| 10 mM | 0.3722 mL | 1.8608 mL | 3.7216 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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