Cat. No.: HY-14277A

Levocabastine hydrochloride

(Synonyms: R 50547 hydrochloride)

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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).

For research use only. We do not sell to patients.

Purity: 99.37%
CAS No.: 79547-78-7
Formula: C₂₆H₃₀ClFN₂O₂
Molecular Weight:456.98

Storage:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Levocabastine hydrochloride Chemical Structure

CAS No.: 79547-78-7

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

H₁ Receptor

NTR2

17 nM (Ki)

All Histamine Receptor Isoforms :

All Neurotensin Receptor Isoforms :

NTR1
NTR2

All Integrin Isoforms :

In Vitro

Levocabastine (0-1000 μM; HEK-293 cells) hydrochloride causes inhibition of ¹²⁵I-FN binding to the SPA bead-associated α4β1 integrin in a concentration-dependent manner with an IC₅₀ 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 IC₅₀ of 395.6 μM, and the adhesion of EoL-1 cells with an IC₅₀ of 403.6 μM. Moreover, Levocabastine inhibits adhesion of human eosinophils to VCAM-1-coated wells (IC₅₀=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.

Chemical Information

CAS No. 79547-78-7
Appearance Solid
Molecular Weight 456.98
Formula C₂₆H₃₀ClFN₂O₂
Color White to off-white
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
Synonyms

R 50547 hydrochloride
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)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[2]. Yamauchi R, et, al. Effect of beta-lactotensin on acute stress and fear memory. Peptides. 2006 Dec;27(12):3176-82. [Content Brief]

[3]. Qasem AR, et, al. Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine. Biochem Pharmacol. 2008 Sep 15;76(6):751-62. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Levocabastine hydrochloride

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All Histamine Receptor Isoforms

All Neurotensin Receptor Isoforms

All Integrin Isoforms

Biological Activity

Chemical Information

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References

Calculators

Help & FAQs

Levocabastine hydrochloride Related Classifications

HY-14277A Related Classifications