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Purity: ≥98%
Lanabecestat camsylate (formerly known as AZD-3293; LY3314814), the camsylate salt of Lanabecestat, is a BACE inhibitor that inhibits beta-secretase 1 cleaving enzyme (BACE) with a Ki of 0.4 nM. AZD3293 displayed significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ. The in vitro potency of AZD3293 was demonstrated in several cellular models, including primary cortical neurons. In vivo in mice, guinea pigs, and dogs, AZD3293 displayed significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ. The in vitro potency of AZD3293 in mouse and guinea pig primary cortical neuronal cells was correlated to the in vivo potency expressed as free AZD3293 concentrations in mouse and guinea pig brains. In mice and dogs, the slow off-rate from BACE1 may have translated into a prolongation of the observed effect beyond the turnover rate of Aβ. The preclinical data strongly support the clinical development of AZD3293, and patients with AD are currently being recruited into a combined Phase 2/3 study to test the disease-modifying properties of AZD3293.
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| References |
J Alzheimers Dis.2016;50(4):1109-23.
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| Molecular Formula |
C36H44N4O5S
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| Molecular Weight |
644.83
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| CAS # |
1522418-41-2
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| Related CAS # |
1383986-31-9 (HCl);1383982-64-6;1628076-74-3 (deleted);1522418-41-2 (camsylate);
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| SMILES |
S(C([H])([H])C12C(C([H])([H])C([H])(C([H])([H])C1([H])[H])C2(C([H])([H])[H])C([H])([H])[H])=O)(=O)(=O)O[H].O(C([H])([H])[H])C1([H])C([H])([H])C([H])([H])C2(C([H])([H])C3C([H])=C([H])C(C4=C([H])N=C([H])C(C#CC([H])([H])[H])=C4[H])=C([H])C=3[C@@]32N=C(C(C([H])([H])[H])=N3)N([H])[H])C([H])([H])C1([H])[H]
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5508 mL | 7.7540 mL | 15.5080 mL | |
| 5 mM | 0.3102 mL | 1.5508 mL | 3.1016 mL | |
| 10 mM | 0.1551 mL | 0.7754 mL | 1.5508 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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