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Details

Stereochemistry RACEMIC
Molecular Formula C26H28N4O2.C4H4O4
Molecular Weight 544.5983
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of ZALDARIDE MALEATE

SMILES

OC(=O)\C=C/C(O)=O.CC4(CN1CCC(CC1)N2C(=O)NC3=CC=CC=C23)OCC5=C(C=CC=C5)N6C=CC=C46

InChI

InChIKey=NGODOSILXOFQPH-BTJKTKAUSA-N
InChI=1S/C26H28N4O2.C4H4O4/c1-26(24-11-6-14-29(24)22-9-4-2-7-19(22)17-32-26)18-28-15-12-20(13-16-28)30-23-10-5-3-8-21(23)27-25(30)31;5-3(6)1-2-4(7)8/h2-11,14,20H,12-13,15-18H2,1H3,(H,27,31);1-2H,(H,5,6)(H,7,8)/b;2-1-

HIDE SMILES / InChI

Description

Zaldaride is a calmodulin antagonist known to produce inhibition of calmodulin-dependent voltage-gated ion channels including those of Ca2+, Na+, and K+. Zaldaride was also observed to inhibit nicotinic acetylcholine receptor (nAChR) channel currents. Zaldaride has been studied in clinical trials as a potential treatment for travelers diarrhea.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
3.3 µM [IC50]
0.81 µM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Unknown

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
Treatment of traveler's diarrhea: 20 mg zaldaride maleate four times per day
Route of Administration: Oral
In Vitro Use Guide
Zaldaride (CGS 9343B) inhibited Kv currents in rabbit coronary arterial smooth muscle cells in a concentration-dependent manner, with a half-maximal inhibitory concentration (IC50) value of 0.81uM.