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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Based on 1 publication(s) in Google Scholar

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
Species Dose Route CL Vd T1/2 AUC Cmax Tmax F
Rat[1] 1 mg/kg i.v. 9.3 mL/min/kg 1.8 L/kg 2.8 h / / / /
Rat[1] 10 mg/kg p.o. / / / 10300 ng·h/mL 1100 ng/mL 0.17 h 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.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1=CC=CC(C(F)(F)F)=C1)NC2(C3)CC3(C(F)F)C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (299.15 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 2.9915 mL 14.9575 mL 29.9150 mL
5 mM 0.5983 mL 2.9915 mL 5.9830 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, stored under nitrogen). 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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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, stored under nitrogen). 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 2.9915 mL 14.9575 mL 29.9150 mL 74.7876 mL
5 mM 0.5983 mL 2.9915 mL 5.9830 mL 14.9575 mL
10 mM 0.2992 mL 1.4958 mL 2.9915 mL 7.4788 mL
15 mM 0.1994 mL 0.9972 mL 1.9943 mL 4.9858 mL
20 mM 0.1496 mL 0.7479 mL 1.4958 mL 3.7394 mL
25 mM 0.1197 mL 0.5983 mL 1.1966 mL 2.9915 mL
30 mM 0.0997 mL 0.4986 mL 0.9972 mL 2.4929 mL
40 mM 0.0748 mL 0.3739 mL 0.7479 mL 1.8697 mL
50 mM 0.0598 mL 0.2992 mL 0.5983 mL 1.4958 mL
60 mM 0.0499 mL 0.2493 mL 0.4986 mL 1.2465 mL
80 mM 0.0374 mL 0.1870 mL 0.3739 mL 0.9348 mL
100 mM 0.0299 mL 0.1496 mL 0.2992 mL 0.7479 mL
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IDOR-1104-0086 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:

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

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