2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. IDOR-1104-0086

IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy.

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IDOR-1104-0086

IDOR-1104-0086 Chemical Structure

CAS No. : 2756581-81-2

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IDOR-1104-0086 Related Antibodies

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Description

IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy[1].

IC50 & Target[1]

Kv7

250 nM (EC50)

In Vitro

IDOR-1104-0086 (Compound 31) effectively inhibits pathological calcium oscillations in the primary cortical neuron-schizophrenia cell co-culture system of rats with IC50s of 188 nM ' and 228 nM (20 min)[1].

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

IDOR-1104-0086 Related Antibodies
Parmacokinetics[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. CL 9.3 mL/min/kg
Rat 10 mg/kg p.o. AUC 10300 ng·h/mL
Rat 1 mg/kg i.v. Vd 1.8 L/kg
Rat 10 mg/kg p.o. Cmax 1100 ng/mL
Rat 1 mg/kg i.v. T1/2 2.8 h
Rat 10 mg/kg p.o. Tmax 0.17 h
Rat 10 mg/kg p.o. F 19 %
In Vivo

IDOR-1104-0086 (Compound 31) (10-30 mg/kg, p.o., single dose) penetrates effectively the brain of rodents, with unbound brain-to-plasma ratio ([B/P]u) > 127% at 1 h post administration, induces almost full protection from the generalized tonic-clonic seizure in the AGS mouse model and causes a dose-dependent reduction in seizure intensity in the rat kindling model[1].

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

Animal Model: Audiogenic seizure-sensitive model of generalized convulsive seizures established in male juvenile DBA/2J mice (22-24 days old)[1]
Dosage: 10 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Induced almost full protection from the generalized tonic-clonic seizure in the AGS mouse model.
Animal Model: Amygdala-kindling rat Model established in adult male Wistar rats (body weight 300-350g)[1]
Dosage: 10 and 30 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Displayed the inhibition of the bilateral forelimb clonus and facial myoclonic twitches without behavioral side effects.
Molecular Weight

334.28

Formula

C15H15F5N2O
CAS No.
SMILES

O=C(NCC1=CC=CC(C(F)(F)F)=C1)NC2(C3)CC3(C(F)F)C2
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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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IDOR-1104-0086 Related Classifications

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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:

IDOR-1104-00862756581-81-2Potassium ChannelKcsAPhenotypic ScreeningCa2? Oscillation AssayEpilepsyMice modelRat modelInhibitorinhibitorinhibit

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