[CAS NO. 50264-69-2] Lonidamine

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PRODUCTS SPECIFICATIONS [50264-69-2]

Catalog

HY-B0486

Brand

MCE

CAS

50264-69-2

DESCRIPTION [50264-69-2]

Overview

MDL	MFCD00866285
Molecular Weight	321.16
Molecular Formula	C15H10Cl2N2O2
SMILES	O=C(C1=NN(CC2=CC=C(Cl)C=C2Cl)C3=C1C=CC=C3)O

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

5 Publications Citing Use of MCE

Summary

Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor ( K _i : 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis ^[1] ^[2] ^[3] .

IC50 & Target

Ki: 2.5 μM (Mitochondrial pyruvate carrier) ^[2]

In Vitro

Lonidamine (100 μM, 24 h) inhibits TGF-β-stimulated lactate production and oxygen consumption rate in AKR-2B and TIG-1 cells ^[3] .
Lonidamine (100 μM, 24/48 h) inhibits H2030BrM3 and A549 cell proliferation ^[4] .
Lonidamine (100-200 μM, 24 h) inhibits H2030BrM3 and A549 cell invasion ^[4] .
Lonidamine (100-1000 μM, 24 h) inhibits mitochondrial complex I and II activities ^[4] .
Lonidamine (200 μM, 24 h) increases ROS generation in H2030BrM3 lung cancer cells ^[4] .

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

In Vivo

Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model ^[3] .

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

Animal Model:	Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model ^[3] .
Dosage:	10, 30, 100 mg/kg/day
Administration:	Oral administration, daily, d10 to d20 after BLM treatment.
Result:	Partially or completely reversed the increases in HK2 and lactate induced by BLM and reduced the expression of 10 profibrotic mediators.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00435448	Threshold Pharmaceuticals\|PRA Health Sciences	Benign Prostatic Hyperplasia\|Enlarged Prostate	June 2005	Phase 3
NCT00237536	Threshold Pharmaceuticals	Benign Prostatic Hyperplasia	June 2005	Phase 2

Appearance

Solid

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 155.69 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1137 mL	15.5686 mL	31.1371 mL
5 mM	0.6227 mL	3.1137 mL	6.2274 mL
10 mM	0.3114 mL	1.5569 mL	3.1137 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: ≥ 2.08 mg/mL (6.48 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (6.48 mM); Clear solution

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

References

Synonyms

1H-Indazole-3-carboxylic acid, 1-[(2,4-dichlorophenyl)methyl]-

1-[(2,4-Dichlorophenyl)methyl]-1H-indazole-3-carboxylic acid

1-(2,4-Dichlorobenzyl)-1H-indazole-3-carboxylic acid

Diclondazolic acid

DICA

AF 1890

Lonidamine

1-[(2,4-Dichlorophenyl)methyl]indazole-3-carboxylic acid