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Cat. No.: HY-175251

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GABAA receptor modulator-9

GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype GABA_A that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC₅₀: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC₅₀s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE).

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Formule: C₂₃H₁₇N₃OS₂
Masse moléculaire:415.53

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

GABAA receptor modulator-9 Chemical Structure

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Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

In Vitro

GABAA receptor modulator-9 (Compound (S)-9d) demonstrates the highest selectivity for the α1 subunit, may not exhibit β subunit selectivity and the γ2 subunit does not influence its allosteric activity on GABA_ARs^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-∞	MRT_0-∞	F
Mice^[1]	1 mg/kg	i.v.	1.9 h	0.08 h	1130.74 ng/mL	724.28 ng·h/mL	1.1 h	/
Mice^[1]	10 mg/kg	i.p.	3.0 h	0.75 h	715.02 ng/mL	2477.67 ng·h/mL	3.8 h	32 %

In Vivo

GABAA receptor modulator-9 (Compound (S)-9d) (5-30 mg/kg, i.p., single dose) prevents stage V seizures in 90% of mice and significantly delays the onset of clonic seizures in Pilocarpine (HY-B0726A)-induced SE model and Pentylenetetrazole-induced acute convulsive seizure model^[1].

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

Animal Model:

Pilocarpine-induced status epilepticus (SE) models established in male C57BL/6N mice (6−8 weeks old, 18-20 g)^[1]
Dosage:

5, 10 and 30 mg/kg
Administration:

Intraperitoneal injection (i.p.), single dose
Result:

Exhibited potent therapeutic efficacy, preventing 90% of Stage V seizure onset at 30 mg/kg.

Animal Model:

Pentylenetetrazole (PTZ)-induced acute convulsive seizures model established in male C57BL/6N mice (6−8 weeks old, 18-20 g)^[1]
Dosage:

5, 10 and 30 mg/kg
Administration:

Intraperitoneal injection (i.p.), single dose
Result:

Showed reduced seizure suppression compared to diazepam at equivalent doses during the acute 2 h SE phase at 5 mg/kg.
Achieved 90% prevention of Stage V seizures and significantly delayed the latency to Stage III seizure onset at 30 mg/kg.
Induced mild sedative side effects at doses above 20 mg/kg.

Chemical Information

Masse moléculaire 415.53
Formule C₂₃H₁₇N₃OS₂
SMILES

O=C1N(C(c2ccccc2)=NC3=C1SC(C4=CC=CS4)=N3)C5=CC=CC=C5CC
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Liao W, et al. Novel 2-(2-Thienyl)-thiazolo[4,5-d]pyrimidin-7(6H)-ones Binding β+/α- Subunit Interface as GABAAR Positive Allosteric Modulator for the Treatment of Status Epilepticus in Mouse. J Med Chem. 2025 Jul 10. [Content Brief]

Calculators

Calculateur de molarité

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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