CAXII-IN-3
CAXII-IN-3 is an effective carbonic anhydrase (CA XII) inhibitor with a Ki of 53 nM. CAXII-IN-3 exhibits selective inhibition against multiple human CA subtypes with Kis 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.
For research use only. We do not sell to patients.
- Formula: C26H25N3O3S
- Molecular Weight:459.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adrenergic Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
hCA XII 53 nM (Ki) |
hCA II 75 nM (Ki) |
hCA I 5.3 μM (Ki) |
hCA IX > 10 μM (Ki) |
Beta-1 adrenergic receptor |
Beta-2 adrenergic receptor |
Beta-3 adrenergic receptor |
In Vitro
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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Instantaneous high intraocular pressure model established in New Zealand White (NZW) rabbits[1]
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Dosage:30 μL of 1% solution
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Administration:Eye drip, single dose
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Result:Produced the greatest and most sustained effect.
Chemical Information
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Molecular Weight 459.56
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Formula C26H25N3O3S
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SMILES
NC1=CC=C(C=C1)CCNC[C@@H](C2=CC=CC=C2)OC(NC3=CC(C=C4)=C(C=C3)OC4=O)=S
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)