[CAS NO. 79547-78-7] Levocabastine hydrochloride
PRODUCTS SPECIFICATIONS [79547-78-7]
DESCRIPTION [79547-78-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 456.98 |
| Molecular Formula | C26H30ClFN2O2 |
| SMILES | OC([C@@]1(C2=CC=CC=C2)[C@@H](CN([C@]3([H])CC[C@](CC3)(C4=CC=C(C=C4)F)C#N)CC1)C)=O.[H]Cl |
Summary
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a K i of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) [1] [2] [3] .
IC50 & Target
|
H 1 Receptor
|
NTR2 17 nM (Ki) |
In Vitro
Levocabastine (0-1000 μM; HEK-293 cells) hydrochloride causes inhibition of
125
I-FN binding to the SPA bead-associated
α4β1
integrin in a concentration-dependent manner with an IC
50
of 406.2μm
[3]
.
Levocabastine (0-1000 μM; 30 min; Jurkat cells and EoL-1 cells) hydrochloride inhibits
α4β1
integrin/VCAM-1-mediated cell adhesion in vitro. Levocabastine inhibits
α4β1
integrindependent adhesion of Jurkat cells to VCAM-1 with an IC
50
of 395.6 μM, and the adhesion of EoL-1 cells with an IC
50
of 403.6 μM. Moreover, Levocabastine inhibits adhesion of human eosinophils to VCAM-1-coated wells (IC
50
=443.7 μM)
[3]
.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Levocabastine (R 50547; 0.25 mg/kg; i.p.; twice a day for five days; guinea-pig with Parainfluenza-3 (PI-3) virus) hydrochloride inhibits the virus-induced airway hyperresponsiveness
[1]
.
Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) hydrochloride blocks anti-stress effect ofβ-LT on mouse behavior
[2]
.
Levocabastine (500 µg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) hydrochloride induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4
[3]
.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Guinea-pig with Parainfluenza-3 (PI-3) virus [1] |
| Dosage: | 0.25 mg/kg |
| Administration: | Intraperitoneal injection; twice a day for five days |
| Result: | Suppressed the influx of broncho-alveolar cells and increased in albumin content. |
| Animal Model: | Male C57BL/6J mice (8-9 weeks old) [2] |
| Dosage: | 0.05 mg/kg; 30 mg/kg (β-LT) |
| Administration: | Intraperitoneal injection; once |
| Result: | Blocked the anxiolytic effect ofβ-LT and decreased the number of head-dips. |
| Animal Model: | Ovalbumin-sensitized guinea pigs [3] |
| Dosage: | 500 µg/eye |
| Administration: | drops eye, once |
| Result: | Produced a noteworthy protection from allergic conjunctivitis (AC) and prevented the conjuctival elevation of VLA-4 as well as conjunctival eosinophil infiltration. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01957202 | GlaxoSmithKline |
Rhinitis, Allergic, Perennial and Seasonal
|
October 2013 | Phase 2 |
| NCT01949051 | GlaxoSmithKline |
Rhinitis, Allergic, Perennial and Seasonal
|
October 1, 2013 | Phase 2 |
| NCT04002349 | Beijing Tongren Hospital|Beijing Institute of Otolaryngology|Shanghai Johnson & Johnson Pharmaceuticals, Ltd. |
Determination of the Efficacy of Different Medications for Idiopathic Rhinitis|Impact of Different Medications on Biomarkers of Idiopathic Rhinitis|Safety and Tolerance of Different Medications for Idiopathic Rhinitis
|
July 1, 2019 | Not Applicable |
| NCT02498509 | Chong Kun Dang Pharmaceutical |
Rhinitis, Allergic, Perennial
|
May 2015 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
References
- [1] Folkerts G, et, al. Virus-induced airway hyperresponsiveness in the guinea-pig: possible involvement of histamine and inflammatory cells. Br J Pharmacol. 1993 Apr;108(4):1083-93.
- [2] Yamauchi R, et, al. Effect of beta-lactotensin on acute stress and fear memory. Peptides. 2006 Dec;27(12):3176-82.
- [3] Qasem AR, et, al. Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine. Biochem Pharmacol. 2008 Sep 15;76(6):751-62.