AR-13324 mesylate |
رقم الكتالوجGC19034 |
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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1422144-42-0
Sample solution is provided at 25 µL, 10mM.
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.
Animal experiment [1]: | |
Animal models | Seven adult female cynomolgus monkeys, each weighing 3 to 5 kg with normotensive IOP |
Preparation Method | 50 μL (25 μL×2) of 0.04% AR-13324 was topically applied to 1 eye of each monkey. An equal volume of vehicle was applied to the contralateral control eye. IOP was measured before drug administration and 6 hours after dosing with a calibrated neumatonometer in the sit ting position. IOP reading was taken 2 times on each eye and the average of 2 values was used to perform statistical analysis. |
Dosage form | 50 μL (25 μL×2) of 0.04% AR-13324 |
Applications | 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 |
Animal experiment [2]: | |
Animal models | Male DB rabbits (n=11, 2.15-0.09 kg) |
Preparation Method | The protocol entailed once per day—topical application of 1 drop of 0.04% AR-13324 for 2 days. Then, on the morning of the third day,the animals were anesthetized and surgically prepared, and then, measurements were obtained before dosing with AR-13324 or vehicle (baseline measurements) and for 3 h after dosing. |
Dosage form | 1 drop of 0.04% AR-13324 for 2 days |
Applications | At 3 h postdosing, the reduction in EVP caused by AR-13324 treatment accounted for 42% of the measured reduction in IOP. |
References: |
Cas No. | 1422144-42-0 | SDF | |
Canonical SMILES | CC1=CC(C)=C(C(OCC2=CC=C([C@@H](CN)C(NC3=CC(C=CN=C4)=C4C=C3)=O)C=C2)=O)C=C1.CS(=O)(O)=O.CS(=O)(O)=O | ||
Formula | C30H35N3O9S2 | M.Wt | 645.74 |
الذوبان | DMSO : 100 mg/mL (154.86 mM; Need ultrasonic) | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 1.5486 mL | 7.7431 mL | 15.4861 mL |
5 mM | 0.3097 mL | 1.5486 mL | 3.0972 mL |
10 mM | 0.1549 mL | 0.7743 mL | 1.5486 mL |
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- Purity: >98.00%
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