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CAXII-IN-3 is a potent carbonic anhydrase (CA XII) inhibitor, with a Ki of 53 nM. It selectively inhibits various human CA isoforms, showing Ki values of 5.3 μM for CA I, 75 nM for CA II, 1.9 μM for CA IV, and > 10 μM for CA IX. Primarily targeting CA II and CA XII, CAXII-IN-3 reduces aqueous humor production. Additionally, it exhibits β3-AR agonist activity, leading to retinal blood vessel dilation and improved optic nerve perfusion. CAXII-IN-3 is applicable in the study of ocular diseases such as glaucoma.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | CAXII-IN-3 is a potent carbonic anhydrase (CA XII) inhibitor, with a Ki of 53 nM. It selectively inhibits various human CA isoforms, showing Ki values of 5.3 μM for CA I, 75 nM for CA II, 1.9 μM for CA IV, and > 10 μM for CA IX. Primarily targeting CA II and CA XII, CAXII-IN-3 reduces aqueous humor production. Additionally, it exhibits β3-AR agonist activity, leading to retinal blood vessel dilation and improved optic nerve perfusion. CAXII-IN-3 is applicable in the study of ocular diseases such as glaucoma. |
| Targets&IC50 | CA XII (human):53 nM (Ki) |
| In vitro | CAXII-IN-3 (Compound 14) enhances cAMP production in HEK293T cells expressing stable β1, β2, and β3 adrenergic receptor subtypes, with pEC50 values of 5.00, 5.29, and 4.98, respectively. It also induces complete vasodilation in porcine retinal arteriolar rings with an EC50 of 11 μM. Additionally, at a concentration of 4 μM for 2 hours, CAXII-IN-3 shows melanin accumulation in porcine retinal pigment epithelium (RPE) comparable to Propranolol. |
| In vivo | CAXII-IN-3 (Compound 14) administered as a single dose (30 μL of 1% solution, eye drops) reaches peak effectiveness 120 minutes post-administration, effectively reducing intraocular pressure (IOP) in rabbits. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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