2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. ICA 110381

ICA 110381 is an orally active Kv7.2/Kv7.3 (KCNQ2/3) potassium channel activator with anticonvulsive properties. ICA 110381 is a KCNQ2/Q3 activator (EC50=0.38 μM) as well as KCNQ1 antagonist (IC50=15 μM).

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

ICA 110381 Chemical Structure

ICA 110381 Chemical Structure

CAS No. : 325457-99-6

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Description

ICA 110381 is an orally active Kv7.2/Kv7.3 (KCNQ2/3) potassium channel activator with anticonvulsive properties. ICA 110381 is a KCNQ2/Q3 activator (EC50=0.38 μM) as well as KCNQ1 antagonist (IC50=15 μM)[1].

IC50 & Target[1]

KV7.1

0.38 μM (EC50)

KV7.3

0.38 μM (EC50)

KV7.1

15 μM (IC50)

In Vitro

ICA 110381 induces rubidium efflux in an agonist-induced rubidium efflux assay using CHO cells expressing KCNQ2 or KCNQ3 (EC50 = 0.38 µM). ICA 110381 inhibits rubidium efflux from CHO cells expressing KCNQ1 (EC50 = 15 µM)[1].
In CA1 pyramidal cells, the increase of M-currents (IM) in the presence of ICA 110381 resulted in a damping of neuronal excitability by reducing the input resistance and shifting the resting membrane potential in hyperpolarizing direction[2].

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

ICA 110381 Related Antibodies
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].

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

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.
Molecular Weight

267.11

Formula

C12H8Cl2N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(Cl)N=C1)C2=CC=C(Cl)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (467.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7438 mL 18.7189 mL 37.4378 mL
5 mM 0.7488 mL 3.7438 mL 7.4876 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7438 mL 18.7189 mL 37.4378 mL 93.5944 mL
5 mM 0.7488 mL 3.7438 mL 7.4876 mL 18.7189 mL
10 mM 0.3744 mL 1.8719 mL 3.7438 mL 9.3594 mL
15 mM 0.2496 mL 1.2479 mL 2.4959 mL 6.2396 mL
20 mM 0.1872 mL 0.9359 mL 1.8719 mL 4.6797 mL
25 mM 0.1498 mL 0.7488 mL 1.4975 mL 3.7438 mL
30 mM 0.1248 mL 0.6240 mL 1.2479 mL 3.1198 mL
40 mM 0.0936 mL 0.4680 mL 0.9359 mL 2.3399 mL
50 mM 0.0749 mL 0.3744 mL 0.7488 mL 1.8719 mL
60 mM 0.0624 mL 0.3120 mL 0.6240 mL 1.5599 mL
80 mM 0.0468 mL 0.2340 mL 0.4680 mL 1.1699 mL
100 mM 0.0374 mL 0.1872 mL 0.3744 mL 0.9359 mL
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ICA 110381 Related Classifications

Help & FAQs
  • 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.

Keywords:

ICA 110381325457-99-6ICA110381ICA-110381Potassium ChannelKcsAKv7.2/Kv7.3KCNQ2/3anticonvulsive propertiesInhibitorinhibitorinhibit

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