CAXII-IN-3 

CAXII-IN-3 is an effective carbonic anhydrase (CA XII) inhibitor with a K_i of 53 nM. CAXII-IN-3 exhibits selective inhibition against multiple human CA subtypes with K_is of 5.3 μM, 75 nM, 1.9 μM, > 10 μM against CA I, CA II, CA IV and CA IX. CAXII-IN-3 mainly inhibits CA II and XII, and reduces aqueous humor production. CAXII-IN-3 exhibits β3-AR agonistic activity, can dilate retinal blood vessels, and improve optic nerve perfusion. CAXII-IN-3 can be used in the research of ocular disorders such as glaucoma^[1].

CAXII-IN-3 (Compound 14) (0.1 pM-10 μM) increases cAMP production in HEK293T cells stably expressing β1, β2, and β3-adrenergic receptor subtypes with pEC₅₀ values of 5.00, 5.29 and 4.98^[1].
CAXII-IN-3 (1 nM-0.1 μM, 0-50 min) induces complete vasodilation in isolated porcine retinal artery rings with an EC₅₀ of 11 μM^[1].
CAXII-IN-3 (4 μM, 2 h) exhibits substantial melanosomal accumulation porcine retinal pigment epithelium (RPE) comparable to Propranolol (HY-B0573B)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CAXII-IN-3 (Compound 14) (30 μL of 1% solution, eye drip, single dose) exhibits the maximum effect at 120 min post-administration with reduction of intraocular pressure (IOP) in rabbits^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

459.56

C₂₆H₂₅N₃O₃S

NC1=CC=C(C=C1)CCNC[C@@H](C2=CC=CC=C2)OC(NC3=CC(C=C4)=C(C=C3)OC4=O)=S

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ammara A, et al. Repurposing Drug Metabolites into Dual β-Adrenergic Receptor-Carbonic Anhydrase Modulators as Potential Tools for Ocular Disorders. J Med Chem. 2025 Sep 11;68(17):18579-18596.  [Content Brief]