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Cat. No.: HY-168834

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Flubrotizolam

Name: Flubrotizolam
Brand: MedChemExpress
SKU: HY-168834
Price: 409.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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Flubrotizolam is a GABA-A receptor modulator. Flubrotizolam allosterically enhances GABA-induced chloride currents at α1β2γ2 GABA-A receptors through the benzodiazepine binding interface, an effect that is abolished by Flumazenil (HY-B0009). Flubrotizolam undergoes limited metabolism in human hepatocytes, primarily generating metabolites via hydroxylation and glucuronidation.

For research use only. We do not sell to patients.

Purity : 98.64%
CAS No.: 57801-95-3
Formula: C₁₅H₁₀BrFN₄S
Molecular Weight:377.23

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Flubrotizolam Chemical Structure

CAS No.: 57801-95-3

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
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- Cellular Effect
- In Vitro
Chemical Information
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Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC50	3.34 nM	Positive allosteric modulation of human α1β2γ2 GABAA receptor in CHO cells assessed as potentiation of 2 μM GABA-induced currents by automated planar patch-clamp (QPatch II) with pre-incubation prior to GABA application. Positive allosteric modulation of human α1β2γ2 GABAA receptor in CHO cells assessed as potentiation of 2 μM GABA-induced currents by automated planar patch-clamp (QPatch II) with pre-incubation prior to GABA application.	41946818

In Vitro

Flubrotizolam (20 µM; 3 h) remains largely unmetabolized in pooled human hepatocytes from ten donors (peak area 1.3×10⁹) and can be converted to generate 6 metabolites^[1].
Flubrotizolam 3 h hepatocyte incubate hydrolyzed with β-glucuronidase (50 µL; 90 min) shows complete cleavage of M3 and M4 together with elevated M6 levels, confirming that M3/M4 are 6-hydroxy-glucuronides, M1 is a direct N-glucuronide, and M2 is a reduced hydroxy-N-glucuronide^[1].

Flubrotizolam (compound 45) (0.96-3000 nM) is a positive allosteric modulator of the α1β2γ2 GABA_A receptor expressed in CHO cells, with an EC₅₀ of 3.34 nM and an E_max of 2.68, and its potentiating effect is completely blocked by Flumazenil^[2].

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

Chemical Information

CAS No. 57801-95-3
Appearance Solid
Molecular Weight 377.23
Formula C₁₅H₁₀BrFN₄S
Color Light brown to brown
SMILES

FC1=C(C2=NCC3=NN=C(C)N3C4=C2C=C(Br)S4)C=CC=C1
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

References

[1]. Gameli PS, et al. Exploring the Metabolism of Flubrotizolam, a Potent Thieno-Triazolo Diazepine, Using Human Hepatocytes and High-Resolution Mass Spectrometry. Metabolites. 2024 Sep 19;14(9):506.

[2]. Norman C, et al. In vitro γ-aminobutyric acid A (GABA) receptor activity and binding interactions at the α/γ interface of 53 prescription and designer benzodiazepines. Communications chemistry. 2026 Apr 07;9(1):155.

[3]. Catalani V, et al. In silico studies on recreational drugs: 3D quantitative structure activity relationship prediction of classified and de novo designer benzodiazepines. Chemical biology & drug design. 2023 Jan;101(1):40-51. [Content Brief]

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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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