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.
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- Formule: C26H25N3O3S
- Masse moléculaire:459.56
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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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Masse moléculaire 459.56
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CAXII-IN-3 Related Classifications
HY-178030 Related Classifications
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