Bepotastine Besilate

Research use only, not for human use.

Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.

Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.(In Vitro):Bepotastine besilate (10, 100, 1000 μM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 μM.Bepotastine besilate (50 μM; 1 h) suppresses the expression of NGF mRNA in NHEKs.(In Vivo):Bepotastine besilate (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration.Bepotastine besilate (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control.Bepotastine besilate (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash.

Bepotastine besilate (10, 100, 1000 μM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 μM.Bepotastine besilate (50 μM; 1 h) suppresses the expression of NGF mRNA in NHEKs.Cell Viability Assay Cell Line:NHEKs Concentration:50 μM (preincubation) Incubation Time:1 h Result:Suppressed the expression of NGF mRNA in NHEKs.Western Blot Analysis Cell Line:RPMCs Concentration:10, 100, 1000 μM Incubation Time:120 min (preincubate)Result:Decreased the release of histamine.

Bepotastine besilate (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration.Bepotastine besilate (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control.Bepotastine besilate (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash. Animal Model:Guinea pigs (6-week-old).Dosage:10 g/L (1.0% (w/v)) for 10 μL.Administration:Eye drop; 3 times at intervals of 20 min (in one eye).Result:Inhibited PAF-induced conjunctival eosinophil infiltration.Animal Model:Male BALB/c mice(12-week-old); NC/Nga mice.Dosage:3, 10 mg/kg Administration:Oral administration; once (1 h before induces scratching behavior of Male BALB/c mice).Result:Significantly inhibited histamine-mediated scratching behavior in male BALB/c mice.Significantly suppressed serum LTB 4 levels in NC/Nga mice with a rash.

Bepotastine besilate | TAU-284

GPCR/G Protein

Histamine Receptor

H1 receptor

Inflammation/Immunology

——

190786-44-8

547.06

C21H25ClN2O3·C6H6O3S

>98% (HPLC)

DMSO:109 mg/mL (199.24 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

C1CN(CCC1O[C@@H](C2=CC=C(C=C2)Cl)C3=CC=CC=N3)CCCC(=O)O.C1=CC=C(C=C1)S(=O)(=O)O

——

(-20℃)

With Ice Pack

≥ 2 years