AR-13324 mesylate |
| カタログ番号GC19034 |
AR-13324は、低濃度で培養されたヒトとブタのトラバーシャルメッシュ細胞に形態学的変化を誘発することが示された、ROCK IとROCK IIの強力な阻害剤である。
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Cas No.: 1422144-42-0
Sample solution is provided at 25 µL, 10mM.
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AR-13324 is a potent inhibitor of ROCK I and ROCK II that has been shown to induce morphologic changes in cultured human and porcine TM cells at low concentration. AR-13324, a rho kinase inhibitor, and an inhibitor of the norepinephrine transporter, reduces intraocular pressure (IOP) in normotensive monkey eyes [1]. AR-13324 produces statistically significant lowering of EVP in DB rabbits [2].
The fixed-dose combination of AR-13324 0.02% and latanoprost 0.005% in PG324 Ophthalmic Solution provides clinically and statistically superior ocular hypotensive efficacy relative to its individual active components at the same concentrations [3]. AR-13324 0.02% was less effective than latanoprost by approximately 1 mmHg in patients with unmedicated IOPs in the range of 22 to 35 mmHg [4]
Six hours after a single dose of 0.04% AR-13324 to 7 normal monkey eyes, the IOP measured by pneumatonometer in treated eyes was reduced (P< 0.005) by 25% when compared with baseline measurements and by 24% when compared with contralateral vehicle-treated eyes [1]. At 3 h postdosing, the reduction in EVP caused by AR-13324 treatment accounted for 42% of the measured reduction in IOP [2].
References:
[1].Wang RF, et al. Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes. J Glaucoma. 2015 Jan;24(1):51-4.
[2].Kiel JW, Kopczynski CC. Effect of AR-13324 on episcleral venous pressure in Dutch belted rabbits. J Ocul Pharmacol Ther. 2015 Apr;31(3):146-51.
[3].Lewis RA, Levy B, Ramirez N, et alFixed-dose combination of AR-13324 and latanoprost: a double-masked, 28-day, randomised, controlled study in patients with open-angle glaucoma or ocular hypertensionBritish Journal of Ophthalmology 2016;100:339-344.
[4].Bacharach J, Dubiner HB, Levy B, Kopczynski CC, Novack GD; AR-13324-CS202 Study Group. Double-masked, randomized, dose-response study of AR-13324 versus latanoprost in patients with elevated intraocular pressure. Ophthalmology. 2015 Feb;122(2):302-7.
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