product name Brinzolamide
Description: Brinzolamide (also known as AL-4862) is a highly potent and selective carbonic anhydrase II inhibitor with IC50 of 3.19 nM. Brinzolamide is used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours.
References: Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29; Ophthalmol. 2000 Jan;44 Suppl 2:S147-53.
383.51
Formula
C12H21N3O5S3
CAS No.
138890-62-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 77 mg/mL (200.8 mM)
Water: < 1 mg/mL
Ethanol: < 1 mg/mL
Solubility (In vivo)
Synonyms
AL-4862
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404608
| In Vitro |
In vitro activity: Brinzolamide is the newest topical CAI to be successfully developed and marketed. It is a safe and efficacious glaucoma drug. In the in vitro assay, brinzolamide has its highest affinity (Ki of 0.13nM) and inhibitory potency (IC50 of 3.19 nM) for CA-II. It has much higher affinity and greater potency for CA-II than for CA-I and CAIV. In the in vivo models, administration of brinzolamide significantly reduces the intraocular pressure (IOP) both in the pigmented rabbits and cynomolgus monkeys with ocular hypertension induced by argon laser trabeculoplasty. Kinase Assay: Brinzolamide(AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM. Cell Assay: |
|---|---|
| In Vivo | Brinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1–2 hours. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice. Brinzolamide (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily. Brinzolamide significantly decreases intraocular pressure and arteriovenous passage time compared with placebo in healthy volunteers. Brinzolamide (2%) increases optic nerve head blood flow and decreases intraocular pressure in tranquilized Dutch-belted rabbits. Brinzolamide (1%) reduces intraocular pressure by reducing aqueous flow and not by affecting aqueous humor drainage in normotensive eyes of rabbits and hypertensive eyes of monkeys. |
| Animal model | |
| Formulation & Dosage | |
| References | Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29; Surv Ophthalmol. 2000 Jan;44 Suppl 2:S147-53. |
Related Posts
product name Brinzolamide
Description: Brinzolamide (also known as AL-4862) is a highly potent and selective carbonic anhydrase II inhibitor with IC50 of 3.19 nM. Brinzolamide is used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours.
References: Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29; Ophthalmol. 2000 Jan;44 Suppl 2:S147-53.
383.51
Formula
C12H21N3O5S3
CAS No.
138890-62-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 77 mg/mL (200.8 mM)
Water: < 1 mg/mL
Ethanol: < 1 mg/mL
Solubility (In vivo)
Synonyms
AL-4862
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404608
| In Vitro |
In vitro activity: Brinzolamide is the newest topical CAI to be successfully developed and marketed. It is a safe and efficacious glaucoma drug. In the in vitro assay, brinzolamide has its highest affinity (Ki of 0.13nM) and inhibitory potency (IC50 of 3.19 nM) for CA-II. It has much higher affinity and greater potency for CA-II than for CA-I and CAIV. In the in vivo models, administration of brinzolamide significantly reduces the intraocular pressure (IOP) both in the pigmented rabbits and cynomolgus monkeys with ocular hypertension induced by argon laser trabeculoplasty. Kinase Assay: Brinzolamide(AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM. Cell Assay: |
|---|---|
| In Vivo | Brinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1–2 hours. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice. Brinzolamide (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily. Brinzolamide significantly decreases intraocular pressure and arteriovenous passage time compared with placebo in healthy volunteers. Brinzolamide (2%) increases optic nerve head blood flow and decreases intraocular pressure in tranquilized Dutch-belted rabbits. Brinzolamide (1%) reduces intraocular pressure by reducing aqueous flow and not by affecting aqueous humor drainage in normotensive eyes of rabbits and hypertensive eyes of monkeys. |
| Animal model | |
| Formulation & Dosage | |
| References | Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29; Surv Ophthalmol. 2000 Jan;44 Suppl 2:S147-53. |