2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. MRK-623

MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect.

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MRK-623

MRK-623 Chemical Structure

CAS No. : 461449-78-5

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Based on 1 publication(s) in Google Scholar

MRK-623 Related Antibodies

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Description

MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect[1].

In Vitro

MRK-623 shows efficacy at human GABAA receptor subtypes expressed in L(tk-) cells measured by whole cell patch-clamp electrophysiology[1].

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

MRK-623 Related Antibodies
In Vivo

MRK-623 (oral gavage; 0.3, 1, and 3 mg/kg; once) shows anxiolytic effects in the rat elevated plus maze assay[1].

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

Animal Model: Rat
Dosage: 0.3, 1, and 3 mg/kg
Administration: Oral gavage; 0.3, 1, and 3 mg/kg; once
Result: Showed 78% BZ site occupancy at 3 mg/kg, with an ID50 of 0.8 mg/kg.
Molecular Weight

348.37

Formula

C20H17FN4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(O)(C1=NC2=NC=C(C3=CC=C(F)C(C4=CC=CN=C4)=C3)N2C=C1)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (14.35 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 2.8705 mL 14.3526 mL 28.7051 mL
5 mM 0.5741 mL 2.8705 mL 5.7410 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. 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. 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 2.8705 mL 14.3526 mL 28.7051 mL 71.7628 mL
5 mM 0.5741 mL 2.8705 mL 5.7410 mL 14.3526 mL
10 mM 0.2871 mL 1.4353 mL 2.8705 mL 7.1763 mL
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MRK-623 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:

MRK-623461449-78-5MRK623MRK 623GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptororal activityhigh-affinityanxiolytic effectInhibitorinhibitorinhibit

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