ALZ-801 (ALZ801; BLU-8499; NRM-8499) is an orally bioavailable, small-molecule inhibitor of beta amyloid (Aβ) oligomer formation with the potential for treating Alzheimer's disease (AD). ALZ-801 is a prodrug of tramiprosate with improved PK/pharmacokinetic properties and gastrointestinal tolerability.
Physicochemical Properties
| Molecular Formula | C8H18N2O4S |
| Molecular Weight | 238.3045 |
| Exact Mass | 238.098 |
| CAS # | 1034190-08-3 |
| Related CAS # | 3687-18-1; |
| PubChem CID | 25008296 |
| Appearance | White to off-white solid powder |
| LogP | -3 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 6 |
| Heavy Atom Count | 15 |
| Complexity | 294 |
| Defined Atom Stereocenter Count | 1 |
| SMILES | C(CCNC([C@H](C(C)C)N)=O)S(=O)(=O)O |
| InChi Key | NRZRFNYKMSAZBI-ZETCQYMHSA-N |
| InChi Code | InChI=1S/C8H18N2O4S/c1-6(2)7(9)8(11)10-4-3-5-15(12,13)14/h6-7H,3-5,9H2,1-2H3,(H,10,11)(H,12,13,14)/t7-/m0/s1 |
| Chemical Name | (S)-3-(2-Amino-3-methylbutanamido)propane-1-sulfonic acid |
| Synonyms | BLU 8499 ALZ 801 NRM8499 BLU8499ALZ-801 NRM-8499BLU-8499ALZ801 NRM 8499 |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vivo | The mean AUCt values of ALZ-801 (Alabama Drug; 172 mg/kg; single dose) were 58, 758, and 5841 ng/mL.h in plasma and brain, respectively. ALZ-801: The ratios of trimiprost in the waist and midbrain of CD-1 mice were 1.8 and 3.1, respectively [1]. |
| References |
[1]. Discovery and Identification of an Endogenous Metabolite of Tramiprosate and Its Prodrug ALZ-801 that Inhibits Beta Amyloid Oligomer Formation in the Human Brain. CNS Drugs. 2018; 32(9): 849–861. [2]. Clinical Pharmacokinetics and Safety of ALZ-801, a Novel Prodrug of Tramiprosate in Development for the Treatment of Alzheimer's Disease. Clin Pharmacokinet. 2018 Mar;57(3):315-333. |
Solubility Data
| Solubility (In Vitro) | H2O : ~30 mg/mL (~125.89 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (419.64 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1964 mL | 20.9820 mL | 41.9639 mL | |
| 5 mM | 0.8393 mL | 4.1964 mL | 8.3928 mL | |
| 10 mM | 0.4196 mL | 2.0982 mL | 4.1964 mL |