| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Carebastine targets the histamine H1 receptor, a G protein-coupled receptor that mediates the effects of histamine in allergic responses. As an H1 receptor antagonist, Carebastine blocks the binding of histamine to its receptor, thereby inhibiting the vasodilation, increased vascular permeability, and smooth muscle contraction that characterize allergic reactions. It is formed from ebastine through metabolic conversion.
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| ln Vitro |
In vitro, Carebastine acts as a histamine H1 receptor antagonist with a Ki of 75.86 nM. Its activity is assessed using receptor binding assays to measure its affinity for the H1 receptor. As the active metabolite of ebastine, Carebastine is responsible for the antihistaminic effects observed following ebastine administration.
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| ln Vivo |
In vivo, Carebastine is the active metabolite responsible for the antihistaminic effects of ebastine. It is effective in reducing allergic symptoms such as rhinitis, conjunctivitis, and urticaria. Its favorable pharmacokinetic profile includes once-daily dosing and minimal penetration of the central nervous system, reducing sedative side effects.
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| Enzyme Assay |
In vitro receptor binding assays for Carebastine are performed using membrane preparations expressing histamine H1 receptors. Radioligand binding assays are used to measure the compound's affinity for the H1 receptor. The Ki value (75.86 nM) is determined from competition binding curves. These cell-free assays provide quantitative data on the compound's receptor binding properties.
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| Cell Assay |
In vitro cellular assays for Carebastine are performed using cells expressing histamine H1 receptors. The compound's antagonist activity is assessed by measuring its ability to inhibit histamine-induced cellular responses such as calcium mobilization or cAMP accumulation. These assays provide functional evidence of H1 receptor antagonism.
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| Animal Protocol |
In vivo animal experimental protocols for Carebastine are not extensively documented in the available literature. As the active metabolite of ebastine, its efficacy is typically evaluated in animal models of allergic disease. Ebastine is administered orally, and Carebastine levels and antihistaminic effects are measured.
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| ADME/Pharmacokinetics |
Carebastine is the active metabolite of ebastine with favorable pharmacokinetic properties. It has a molecular weight of 499.64 (or 499.66) and molecular formula C32H37NO4. It is formed from ebastine through metabolic conversion. Its favorable profile includes once-daily dosing and minimal CNS penetration.
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| Toxicity/Toxicokinetics |
Toxicological data for Carebastine are available from studies of ebastine, from which it is derived as the active metabolite. As an antihistamine, its safety profile is well established, with common adverse effects including headache and dry mouth. The compound is intended for research purposes.
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| References | |
| Additional Infomation |
Carebastine is a diarylmethane.
Carebastine is the active metabolite of ebastine with CAS number 90729-42-3, molecular formula C32H37NO4, and molecular weight 499.64. It is a histamine H1 receptor antagonist with a Ki of 75.86 nM. It is used in research on allergic conditions such as rhinitis, conjunctivitis, and urticaria. This product is for research use only. |
| Molecular Formula |
C32H37NO4
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|---|---|
| Molecular Weight |
499.64048
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| Exact Mass |
499.272
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| CAS # |
90729-42-3
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| Related CAS # |
Carebastine-d5;1189661-02-6;Carebastine-d5 Methyl Ester;1190019-51-2
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| PubChem CID |
65820
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
657.9±55.0 °C at 760 mmHg
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| Melting Point |
178-180ºC
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| Flash Point |
351.7±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.609
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| LogP |
6.09
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
37
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| Complexity |
690
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XGHOVGYJHWQGCC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H37NO4/c1-32(2,31(35)36)27-17-15-24(16-18-27)29(34)14-9-21-33-22-19-28(20-23-33)37-30(25-10-5-3-6-11-25)26-12-7-4-8-13-26/h3-8,10-13,15-18,28,30H,9,14,19-23H2,1-2H3,(H,35,36)
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| Chemical Name |
2-[4-[4-(4-benzhydryloxypiperidin-1-yl)butanoyl]phenyl]-2-methylpropanoic acid
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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) |
DMF : 25 mg/mL (~50.04 mM)
DMSO : ~2 mg/mL (~4.00 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.00 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (5.00 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (5.00 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 | 2.0014 mL | 10.0072 mL | 20.0144 mL | |
| 5 mM | 0.4003 mL | 2.0014 mL | 4.0029 mL | |
| 10 mM | 0.2001 mL | 1.0007 mL | 2.0014 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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