ICA 110381

Product NameICA 110381
CAS325457-99-6
MFC12H8Cl2N2O
MW267.11
EINECS
MOL File325457-99-6.mol

Chemical Properties

Boiling point	336.8±37.0 °C(Predicted)
Density	1.440±0.06 g/cm3(Predicted)
storage temp.	under inert gas (nitrogen or Argon) at 2-8°C
solubility	Soluble in DMSO (up to 26 mg/ml) or in Ethanol (up to 5 mg/ml).
form	solid
pka	11.34±0.70(Predicted)
color	White
Stability	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.

Usage And Synthesis

Description

ICA-110381 (325457-99-6) is a KCNQ2/Q3 (Kv7.2/7.3) activator, EC50=0.38 μM (KCNQ1 IC50=15 μM).1KCNQ3/Q5 heterodimers are not affected2. Potently dampens neuronal excitability and displays anticonvulsant activityin vivo.2

Uses

ICA 110381 was used to study the pharmacological activities as it selectively activated human KCNQ2 expressed in Chinese hamster ovary, damped neuronal excitability in rat hippocampal CA1 cell and showed anticonvulsant activity in amygdala-kindled rat.

in vivo

ICA 110381 (3-30 mg/kg; p.o.; once) elevates the threshold for induction of afterdischarges and reduced seizure severity and duration in fully amygdala-kindled rats^[2].

Animal Model:	Female Wistar rats (200-300 g)^[2]
Dosage:	3 mg/kg, 10 mg/kg and 30 mg/kg (suspended in 0.5% Hydroxyethyl Cellulose (HY-B2221B))
Administration:	Oral administration; once
Result:	Showed anticonvulsive properties in fully amygdala-kindled rats.

IC 50

KV7.1: 0.38 μM (EC₅₀); KV7.3: 0.38 μM (EC₅₀); KV7.1: 15 μM (IC₅₀)

storage

Store at +4°C

References

[1] GEORGE AMATO. N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy[J]. ACS Medicinal Chemistry Letters, 2011, 2 6: 481-484. DOI:10.1021/ml200053x
[2] A BOEHLEN. The new KCNQ2 activator 4-Chlor-N-(6-chlor-pyridin-3-yl)-benzamid displays anticonvulsant potential[J]. British Journal of Pharmacology, 2012, 168 5: 1182-1200. DOI:10.1111/bph.12065