[CAS NO. 75144-12-6] Antitrypanosomal agent 1

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PRODUCTS SPECIFICATIONS [75144-12-6]

Catelog

HY-W052512

Brand

MCE

CAS

75144-12-6

DESCRIPTION [75144-12-6]

Overview

MDL	MFCD01220371
Molecular Weight	282.59
Molecular Formula	C11H14Cl3NO
SMILES	O=C(C1=CC=C(Cl)C(Cl)=C1)CCN(C)C.[H]Cl

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

Summary

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor with an IC ₅₀ of 3.3 μM. Antitrypanosomal agent 1 inhibits glutathione reductase (GR) ( IC ₅₀ =64.8 μM) and T. brucei ( EC ₅₀ =1 μM). Antitrypanosomal agent 1 has anti-trypanosomal activity ^[1] .

IC50 & Target

IC50: 3.3 μM (trypanothione reductase) and 64.8 μM (glutathione reductase) ^[1]
EC50: 1 μM ( T. brucei ) ^[1]

In Vitro

Antitrypanosomal agent 1 (compound 8a) has an selectivity for TR (GR IC50/TR IC50) of 20 ^[1] .

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 88.47 mM ; Need ultrasonic)

H ₂ O : 10 mg/mL ( 35.39 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5387 mL	17.6935 mL	35.3870 mL
5 mM	0.7077 mL	3.5387 mL	7.0774 mL
10 mM	0.3539 mL	1.7693 mL	3.5387 mL

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

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (8.85 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (8.85 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (8.85 mM); Clear solution

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

References

[1] Martyn DC, et al. High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1280-3.