[CAS NO. 550-99-2] Naphazolinehydrochloride
PRODUCTS SPECIFICATIONS [550-99-2]
DESCRIPTION [550-99-2]
Overview
| MDL | MFCD00012554 |
|---|---|
| Molecular Weight | 246.74 |
| Molecular Formula | C14H15ClN2 |
| SMILES | C1(CC2=NCCN2)=CC=CC3=CC=CC=C13.Cl |
Summary
Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE , GMCSF, and NGF。Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research [1] [2] .
IC50 & Target
|
IL-1β |
IL-6 |
IL-4 |
In Vivo
Naphazoline hydrochloride (0.2 mg/kg, 10 µl per eye; IP, once) reduces histamine or antigen-induced conjunctival vascular hyperpermeability in mice, and reduces conjunctivitis in mice via effects on inflammation, NGF and VEGF [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female wild-type BALB/c mice (4-5 weeks, 18 ± 2 g, n=8/group, allergic conjunctivitis mouse model established using histamine or an antigen (ovalbumin)) [1] |
| Dosage: | 0.2 mg/mL, 10 µl per eye |
| Administration: | Intraperitoneal injection (IP), once |
| Result: | Significantly suppressed conjunctival dye leakage in mice with histamine or antigen‑induced conjunctival vascular hyperpermeability. Reduced inflammatory reactions and the levels of IL-1β, IL-6, IFN-γ, and IL-4. Reduced the levels of IgE, GMCSF, NGF and VEGF in antigen-induced conjunctival vascular hyperpermeability mice. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00769886 | Bausch & Lomb Incorporated |
Allergic Conjunctivitis
|
October 2008 | Phase 3 |
| NCT00770133 | Bausch & Lomb Incorporated |
Allergic Conjunctivitis
|
February 2010 | Phase 3 |
| NCT05470868 | Laboratorios Sophia S.A de C.V. |
Hyperemia Eye
|
August 1, 2022 | Phase 1 |
| NCT01533220 | EMS |
Flu|Cold|Allergic Disorder of Respiratory System
|
January 1, 2013 | Phase 3 |
| NCT01390961 | Hom, Milton M., OD, FAAO|Allergan |
Allergic Conjunctivitis
|
August 2011 | Phase 4 |
| NCT03324113 | Sanofi |
Neoplasm Malignant
|
October 17, 2017 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 202.64 mM ; Need ultrasonic)
DMSO : ≥ 25 mg/mL ( 101.32 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.0528 mL | 20.2642 mL | 40.5285 mL |
| 5 mM | 0.8106 mL | 4.0528 mL | 8.1057 mL |
| 10 mM | 0.4053 mL | 2.0264 mL | 4.0528 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 75 mg/mL (303.96 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.13 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.13 mM); Suspended solution
References
- [1] Quan L, et, al. Treatment with olopatadine and naphazoline hydrochloride reduces allergic conjunctivitis in mice through alterations in inflammation, NGF and VEGF. Mol Med Rep. 2016 Apr;13(4):3319-25.
- [2] Yamaguchi I, et, al. Central and peripheral adrenergic mechanisms regulating gastric secretion in the rat. J Pharmacol Exp Ther. 1977 Oct;203(1):125-31.
Synonyms