[CAS NO. 166038-00-2] BrBzGCp2

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PRODUCTS SPECIFICATIONS [166038-00-2]

Catalog

HY-136684

Brand

MCE

CAS

166038-00-2

DESCRIPTION [166038-00-2]

Overview

MDL	-
Molecular Weight	612.58
Molecular Formula	C27H38BrN3O6S
SMILES	O=C(NCC(OC1CCCC1)=O)[C@@H](NC(CC[C@H](N)C(OC2CCCC2)=O)=O)CSCC(C=C3)=CC=C3Br

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

Summary

BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor, with a GC ₅₀ of 4.23 μM in HL-60 cells. BrBzGCp2 possesses antitumor and neuroprotective activity ^[1] ^[2] .

IC50 & Target

GC50: 4.23 μM (GLO1) ^[1] .

In Vivo

GLO1 inhibition by BrBzGCp2 increases center time in the OF test, without changing distance traveled. GLO1 inhibition increases MG (methylglyoxal) concentration, thus reducing anxiety-like behavior ^[2] .
BrBzGCp2 pre-treatment decreases seizure duration ^[3] .
BrBzGCp2 injection alleviates the level of anxiety in mice, and mice with less anxiety and fear were more likely to explore the unknown area, implying that inhibition of GLO1 activity mitigated anxiety levels ^[4] .
BrBzGCp2 treatment restores the VPA-induced inhibition effect on GABA _A receptor activation ^[4] .
BrBzGCp2 significantly lowers the blood pressure and ameliorated endothelial dysfunction in diabetic mice ^[5] .

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

Animal Model:	Male CD-1 mice ^[2] .
Dosage:	50 mg/kg.
Administration:	IP once (Two hours post-injection, mice were sacrificed, and brains were rapidly dissected and flash-frozen on dry ice. MG concentration was measured)
Result:	Allowed MG levels to accumulate for 2 hours

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 408.11 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6324 mL	8.1622 mL	16.3244 mL
5 mM	0.3265 mL	1.6324 mL	3.2649 mL
10 mM	0.1632 mL	0.8162 mL	1.6324 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 8% DMSO >> 18% Tween-80 >> 74% saline

Solubility: 20 mg/mL (32.65 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.40 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.40 mM); Clear solution

* All of the co-solvents are available by MCE.