| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Beta-adrenergic receptors (β1, β2, and β3 adrenoceptors). Carazolol is a beta1/beta2 adrenoceptor antagonist of high potency. It has highest affinity for β2- and lowest for β3-adrenoceptors. Carazolol also acts as a synthetic β3AR agonist. 3H-Carazolol binds saturably to cortical β-receptors with a KD of 0.15 nM, approximately four times lower than that for 3H-DHA.
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| ln Vitro |
Carazolol is a beta-adrenoceptor antagonist/inverse agonist with highest affinity for β2- and lowest for β3-adrenoceptors. As a beta1/beta2 adrenoceptor antagonist, it blocks the effects of catecholamines (epinephrine and norepinephrine) at beta-adrenergic receptors, reducing heart rate, cardiac output, and blood pressure. Carazolol also acts as a synthetic β3AR agonist, demonstrating its complex pharmacology at different beta-adrenoceptor subtypes. 3H-Carazolol binds to β-receptors with a KD of 0.15 nM.
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| ln Vivo |
There have been no notable negative effects reported with calalol (0.01 mg/kg; IM; once) [2].
In vivo, carazolol is used as an antihypertensive agent in humans and as a stress-reducing agent in veterinary medicine. In veterinary medicine, carazolol is used to reduce stress in animals during transportation. Its activity and safety have been evaluated in clinical trials in healthy subjects and in patients suffering from either chronic bronchitis or asthma. The drug's beta-blocking activity reduces heart rate and myocardial oxygen demand. |
| Enzyme Assay |
In vitro receptor binding assays for carazolol involve measuring the compound's affinity for beta-adrenergic receptors using radioligand binding techniques. 3H-Carazolol binds saturably to cortical β-receptors with a KD of 0.15 nM. Membranes from tissues expressing beta-adrenergic receptors are incubated with 3H-carazolol and increasing concentrations of unlabeled carazolol. Bound and free ligand are separated by filtration, and radioactivity is measured. These assays confirm the high affinity of carazolol for beta-adrenergic receptors.
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| Cell Assay |
Cellular assays for carazolol involve measuring the compound's effects on beta-adrenergic receptor signaling in cells expressing β1, β2, or β3 adrenoceptors. Cells are treated with carazolol, and downstream signaling events such as cAMP accumulation, PKA activation, or changes in gene expression are measured. These assays demonstrate the antagonist activity of carazolol at β1 and β2 receptors and its agonist activity at β3 receptors.
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| Animal Protocol |
Animal/Disease Models: Kivircik sheep, 25-45 kg, non-pregnant [2]
Doses: 0.01 mg/kg Route of Administration: intramuscularinjection, one time Experimental Results: Urea, creatinine, ALT, ALP, GGT, LDH, Ca, P, T.Protein, Mg, copper levels in serum parameters were found to be at normal levels, but serum iron and zinc levels were diminished. In vivo animal studies for carazolol typically involve administration to normotensive or hypertensive animal models to assess its antihypertensive and beta-blocking effects. In veterinary medicine, the drug is used to reduce stress in animals during transportation. Activity and safety of the drug were evaluated in clinical trials in healthy subjects and in patients with chronic bronchitis or asthma. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies of carazolol show that the compound is absorbed following oral administration. The drug distributes widely in the body and crosses the blood-brain barrier, as demonstrated by 3H-carazolol binding to cortical β-receptors. Carazolol is metabolized in the liver and eliminated primarily by renal excretion. The compound's pharmacokinetic profile supports its use as an antihypertensive agent with once-daily or twice-daily dosing.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of carazolol have established its safety profile as a beta-blocker. The drug's adverse effects are primarily related to its beta-blocking activity and include bradycardia, hypotension, bronchospasm (particularly in patients with asthma), and fatigue. In patients with chronic bronchitis or asthma, carazolol should be used with caution due to its β2-blocking activity.
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| References | |
| Additional Infomation |
Carbazool is a type of carbazole compound.
Carazolol is a beta-adrenoceptor antagonist with high potency, used in the treatment of hypertension. It has highest affinity for β2- and lowest for β3-adrenoceptors. In veterinary medicine, carazolol is used to reduce stress in animals during transportation. The compound also acts as a synthetic β3AR agonist, demonstrating complex pharmacology at different beta-adrenoceptor subtypes. 3H-Carazolol is widely used as a radioligand for studying beta-adrenergic receptors due to its high affinity (KD = 0.15 nM). |
| Molecular Formula |
C18H22N2O2
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|---|---|
| Molecular Weight |
298.3795
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| Exact Mass |
298.168
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| CAS # |
57775-29-8
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| Related CAS # |
Carazolol-d7;1173021-02-7;Carazolol-d7 hydrochloride;1276197-44-4
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| PubChem CID |
71739
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
531.2±40.0 °C at 760 mmHg
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| Melting Point |
133-137 °C
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| Flash Point |
275.1±27.3 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.652
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| LogP |
3.59
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
350
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BQXQGZPYHWWCEB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22N2O2/c1-12(2)19-10-13(21)11-22-17-9-5-8-16-18(17)14-6-3-4-7-15(14)20-16/h3-9,12-13,19-21H,10-11H2,1-2H3
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| Chemical Name |
1-(Carbazol-4-yloxy)-3-(isopropylamino)-2-propanol
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| Synonyms |
BM-51052 CCRIS-1047BM 51052 CCRIS 1047BM51052 CCRIS1047
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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 : ~100 mg/mL (~335.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.38 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 (8.38 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 (8.38 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 | 3.3514 mL | 16.7572 mL | 33.5143 mL | |
| 5 mM | 0.6703 mL | 3.3514 mL | 6.7029 mL | |
| 10 mM | 0.3351 mL | 1.6757 mL | 3.3514 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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