Amustaline dihydrochloride

Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products).

Product information

CAS Number: 210584-54-6

Molecular Weight: 507.28

Formula: C22H27Cl4N3O2

Chemical Name: 2-[bis(2-chloroethyl)amino]ethyl 3-[(acridin-9-yl)amino]propanoate dihydrochloride

Smiles: Cl.Cl.O=C(CCNC1C2=CC=CC=C2N=C2C=CC=CC2=1)OCCN(CCCl)CCCl

InChiKey: WEOLKSYHLNAIRH-UHFFFAOYSA-N

InChi: InChI=1S/C22H25Cl2N3O2.2ClH/c23-10-13-27(14-11-24)15-16-29-21(28)9-12-25-22-17-5-1-3-7-19(17)26-20-8-4-2-6-18(20)22;;/h1-8H,9-16H2,(H,25,26);2*1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

S‐303 (200 μM; 20 h) and glutathione (GSH; 20 mM) inactivates high titres of Chikungunya virus (CHIKV) in red blood cells (RBCs). S-303 (200 μM; 20 h) and GSH (2 mM) inactivates >6.5 logs of HIV, >5.7 logs of Bluetongue virus, >7.0 logs of Yersinia enterocolitica, 4.2 logs of Serratia marcescens, and 7.5 logs of Staphylococcus epidermidis in whole blood experiments. S-303 (200 μM; 20 h) and GSH (20 mM) inactivates approximately 5 logs or greater of Y. enterocolitica, E. coli, S. marcescens, S. aureus, HIV, bovine viral diarrhoea virus, bluetongue virus and human adenovirus 5 in RBC. S-303 (200 μM; 20 h) retains in vitro parameters of RBC function and physiology (including total ATP, extracellular potassium, hemolysis, glucose consumption, lactate production, and pH at 37 °C) compared to conventional RBC.

In Vivo:

S‐303 RBCs (a single transfusion) is well tolerated in rats (50 μmol/kg) and dogs (70 μmol/kg). S‐303 RBCs (repeated transfusions) is well tolerated in rats (10 μmol/kg) and dogs (10 μmol/kg) with no histopathologic evidence of organ toxicity.

Products are for research use only. Not for human use.