1. Metabolic Enzyme/Protease
  2. Carbonic Anhydrase
  3. NCX-278

NCX-278 is a human carbonic anhydrase inhibitor with a 13 nM Ki for hCA II, 410 nM Ki for hCA I, 181 nM Ki for hCA IV, and selective inhibition of hCA II over hCA IV. NCX-278 is a potent and effective stimulator of NO/sGC/cGMP signaling with an EC50 of 2.05 lM. NCX-278 exerts NO-mediated vascular relaxant effects. NCX-278 lowers intraocular pressure in normotensive rabbits. NCX-278 can be used for the research of open-angle glaucoma.

For research use only. We do not sell to patients.

NCX-278

NCX-278 Chemical Structure

CAS No. : 1202697-61-7

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Description

NCX-278 is a human carbonic anhydrase inhibitor with a 13 nM Ki for hCA II, 410 nM Ki for hCA I, 181 nM Ki for hCA IV, and selective inhibition of hCA II over hCA IV. NCX-278 is a potent and effective stimulator of NO/sGC/cGMP signaling with an EC50 of 2.05 lM. NCX-278 exerts NO-mediated vascular relaxant effects. NCX-278 lowers intraocular pressure in normotensive rabbits. NCX-278 can be used for the research of open-angle glaucoma[1].

IC50 & Target

hCA II

13 nM (Ki)

hCA I

410 nM (Ki)

In Vitro

NCX-278 potently inhibits recombinant human hCA II with a Ki of 13 nM, and shows 13.9-fold selectivity for hCA II over hCA IV, while inhibiting hCA I with a Ki of 410 nM[1].

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

Parmacokinetics
Species Dose Route Tmax
Rat[1] 55 mM o.a. 120 min
In Vivo

NCX-278 (55 mM; o.a.; single dose) produces a statistically significant maximal intraocular pressure reduction of -3.7 mmHg in normotensive New Zealand white rabbits, with peak effect at 120 minutes post-dose[1].

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

Animal Model: New Zealand white rabbits[1]
Dosage: 55 mM
Administration: o.a.; single dose
Result: Reduced intraocular pressure to a maximal effect of -3.7 mmHg.
Reached peak effect at 120 minutes post-dosing.
Returned to basal intraocular pressure levels at 360 minutes post-dosing.
Molecular Weight

471.53

Formula

C14H21N3O9S3

CAS No.
SMILES

O=C(OCCCO[N+]([O-])=O)N([C@@H]1C2=C(S(=O)([C@H](C1)C)=O)SC(S(N)(=O)=O)=C2)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
NCX-278
Cat. No.:
HY-182426
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