| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Histamine H1 receptor and neurotensin receptor subtype 2 (NTR2). Levocabastine is a potent and selective H1 receptor antagonist and a selective NTR2 antagonist with a Ki of 17 nM.
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| ln Vitro |
Levocabastine hydrochloride (0-1000 μM; HEK-293 cells) suppresses, in a concentration-dependent manner, the binding of 125I-FN to the α4β1 integrin linked with SPA beads (IC50 = 406.2 μm [3]. In vitro, α4β1 integrin/VCAM-1-mediated cell adhesion is inhibited by levocabastine hydrochloride (0-1000 μM; 30 min; Jurkat cells and EoL-1 cells). Levocabastine inhibits the α4β1 integrin-dependent adhesion of Jurkat cells to VCAM-1, exhibiting an IC50 of 395.6 μM, and an IC50 of 403.6 μM for EoL-1 cells. Furthermore, it has been observed that Levocabastine can prevent human eosinophils from adhering to wells coated with VCAM-1 (IC50=443.7 μM) 3.
In vitro, Levocabastine acts as a potent and selective histamine H1-receptor antagonist. It is also a selective, high-affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mouse NTR2. The compound's potent and selective H1 receptor antagonist activity has been clinically applied as a topical treatment. |
| ln Vivo |
In guinea pigs infected with the parainfluenza-3 (PI-3) virus, levocarbastine hydrochloride (R 50547; 0.25 mg/kg; intraperitoneal injection; twice daily for five days) suppresses the hyperresponsiveness of the airways caused by the virus [ 1]. Male C57BL/6J mice were injected intraperitoneally once with 0.05 mg/kg levocarbastine hydrochloride to prevent the anti-stress impact of β-LT on behavior [2]. In ovalbumin-sensitized guinea pigs, levocarbastine hydrochloride (500 µg/eye; eye drops; once) can cause allergic conjunctivitis (AC) and a considerable elevation of conjunctival VLA-4. [3].
In vivo, Levocabastine hydrochloride produces a noteworthy protection from allergic conjunctivitis and prevents the conjunctival elevation of VLA-4 as well as conjunctival eosinophil infiltration. It reduces itching, rhinorrhea, and symptoms of allergic rhinitis or conjunctivitis when applied locally to the eye. Levocabastine is a long-acting antihistamine. |
| Enzyme Assay |
Non-cell receptor binding assays for Levocabastine are performed using membrane preparations from cells expressing histamine H1 receptors or neurotensin receptor subtype 2 (NTR2). Radioligand binding studies are conducted using [³H]mepyramine for H1 or [³H]neurotensin for NTR2 as tracers. Membranes are incubated with the radioligand and varying concentrations of Levocabastine (0.001-100 μM). Nonspecific binding is determined with excess unlabeled mepyramine or neurotensin. 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 Levocabastine are performed using cells expressing histamine H1 receptors. Cells are treated with Levocabastine at concentrations ranging from 0.001-100 μM. Inhibition of histamine-induced calcium mobilization is measured using fluorescent calcium indicators (e.g., Fluo-4). IC₅₀ values for H1 receptor antagonism are calculated from dose-response curves. Alternatively, inhibition of histamine-induced cAMP accumulation is measured.
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| Animal Protocol |
Animal/Disease Models: Parainfluenza-3 (PI-3) virus guinea pig [1]
Doses: 0.25 mg/kg Route of Administration: intraperitoneal (ip) injection; twice (two times) daily for five days Experimental Results: Inhibition of bronchoalveolar cell influx and increased albumin content . Animal/Disease Models: Male C57BL/6J mice (8-9 weeks old) [2] Doses: 0.05 mg/kg; 30 mg/kg (β-LT) Route of Administration: intraperitoneal (ip) injection; primary Experimental Results:blocking β-LT It has an anti-anxiety effect and reduces the number of times you lower your head. Animal/Disease Models: Ovalbumin-sensitized guinea pigs [3] Doses: 500 µg/eye Route of Administration: One eye drop Experimental Results: Significant protective effect on allergic conjunctivitis (AC) and preventing the increase in conjunctival VLA-4 and conjunctival eosinophilic infiltration. In vivo animal studies are conducted in models of allergic conjunctivitis or allergic rhinitis. Levocabastine is administered topically as eye drops or intranasally. Efficacy endpoints include reduction in itching, rhinorrhea, conjunctival eosinophil infiltration, and VLA-4 levels. The compound's long-acting antihistaminic activity is evaluated. |
| ADME/Pharmacokinetics |
Levocabastine hydrochloride has a molecular weight of 456.98 and a molecular formula of C26H30ClFN2O2. It is also known as R 50547 hydrochloride. The compound is a potent and selective H1 receptor antagonist and a selective NTR2 antagonist with a Ki of 17 nM.
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| Toxicity/Toxicokinetics |
Levocabastine is generally well tolerated as a topical preparation. Common adverse effects include mild ocular irritation. No significant systemic toxicity has been reported at therapeutic doses. The compound is contraindicated in patients with known hypersensitivity.
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| References | |
| Additional Infomation |
Livorstin (TN) belongs to the piperidine class of drugs.
See also: Levocabastine hydrochloride (note moved to). Levocabastine hydrochloride is a synthetic piperidine derivative and a second-generation histamine-1 receptor antagonist. It is also a selective neurotensin receptor subtype 2 antagonist with a Ki of 17 nM. Levocabastine is used topically for allergic conjunctivitis and allergic rhinitis. |
| Molecular Formula |
C26H30CLFN2O2
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|---|---|
| Molecular Weight |
456.98
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| Exact Mass |
456.198
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| Elemental Analysis |
C, 68.34; H, 6.62; Cl, 7.76; F, 4.16; N, 6.13; O, 7.00
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| CAS # |
79547-78-7
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| Related CAS # |
Levocabastine;79516-68-0
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| PubChem CID |
54384
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| Appearance |
White to off-white solid powder
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| Boiling Point |
611ºC at 760 mmHg
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| Flash Point |
323.3ºC
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| LogP |
5.633
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
681
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@H]1CN(CC[C@@]1(C2=CC=CC=C2)C(=O)O)C3CCC(CC3)(C#N)C4=CC=C(C=C4)F.Cl
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| InChi Key |
OICFWWJHIMKBCD-VALQNVSPSA-N
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| InChi Code |
InChI=1S/C26H29FN2O2.ClH/c1-19-17-29(16-15-26(19,24(30)31)21-5-3-2-4-6-21)23-11-13-25(18-28,14-12-23)20-7-9-22(27)10-8-20/h2-10,19,23H,11-17H2,1H3,(H,30,31)1H/t19-,23-,25-,26-/m1./s1
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| Chemical Name |
(3S,4R)-1-((1s,4R)-4-cyano-4-(4-fluorophenyl)cyclohexyl)-3-methyl-4-phenylpiperidine-4-carboxylic acid hydrochloride
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| Synonyms |
R-50,547; R 50547; R-50547; R50547;Levocabastine hydrochloride; Livostin; R 50,547 Levocabastine HCl; R50,547
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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: 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1883 mL | 10.9414 mL | 21.8828 mL | |
| 5 mM | 0.4377 mL | 2.1883 mL | 4.3766 mL | |
| 10 mM | 0.2188 mL | 1.0941 mL | 2.1883 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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