1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. MK-0343

MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.

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MK-0343

MK-0343 화학구조

CAS No. : 233275-76-8

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg   견적 받기  
200 mg   견적 받기  

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고객리뷰

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Other Forms of MK-0343:

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제품 설명

MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic[1].

IC50 & Target

Ki: 0.22 nM (rGABAA α1), 0.4 nM (rGABAAα2) , 0.21 nM (rGABAAα3), 78 nM (rGABAAα4), 0.23 nM (rGABAAα5), 980 nM (rGABAAα6)[1]

In Vivo

MK0343 readily penetrates the brain in rats and occupies the benzodiazepine site of GABAA receptors, measured using an in vivo [3H]flumazenil binding assay, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL[1].

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

Animal Model: Male Sprague-Dawley rats (approximately 250–300g) (pharmacokinetics)[1]
Dosage: 1, 2 or 3 mg/kg
Administration: Oral administration
Result: Readily penetrated the brain in rats and occupies the benzodiazepine site of GABAA receptors, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL.
분자량

397.38

화학식

C19H17F2N7O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1N=CN=C1COC2=NN3C(C=C2C4CCC4)=NN=C3C5=C(F)C=CC=C5F

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

DMSO : 250 mg/mL (629.12 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 2.5165 mL 12.5824 mL 25.1648 mL
5 mM 0.5033 mL 2.5165 mL 5.0330 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
순도&문서

Purity: 99.69%

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 2.5165 mL 12.5824 mL 25.1648 mL 62.9121 mL
5 mM 0.5033 mL 2.5165 mL 5.0330 mL 12.5824 mL
10 mM 0.2516 mL 1.2582 mL 2.5165 mL 6.2912 mL
15 mM 0.1678 mL 0.8388 mL 1.6777 mL 4.1941 mL
20 mM 0.1258 mL 0.6291 mL 1.2582 mL 3.1456 mL
25 mM 0.1007 mL 0.5033 mL 1.0066 mL 2.5165 mL
30 mM 0.0839 mL 0.4194 mL 0.8388 mL 2.0971 mL
40 mM 0.0629 mL 0.3146 mL 0.6291 mL 1.5728 mL
50 mM 0.0503 mL 0.2516 mL 0.5033 mL 1.2582 mL
60 mM 0.0419 mL 0.2097 mL 0.4194 mL 1.0485 mL
80 mM 0.0315 mL 0.1573 mL 0.3146 mL 0.7864 mL
100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6291 mL
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  • 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.

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Inquiry Information

상품명:
MK-0343
Cat. No.:
HY-101869
수량:
MCE Japan Authorized Agent: