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Lanabecestat camsylate

Alias: O=S(C[C@@]1(C2(C)C)C(C[C@@]2([H])CC1)=O)(O)=O.NC(C(C)=N3)=NC43C5=C(C=CC(C6=CC(C#CC)=CN=C6)=C5)C[C@]74CCC(OC)CC7
Cat No.:V2719 Purity: ≥98%
Lanabecestat camsylate (formerly known as AZD-3293; LY3314814), the camsylate salt ofLanabecestat, is a BACE inhibitor that inhibits beta-secretase 1 cleaving enzyme (BACE) with aKiof 0.4 nM.
Lanabecestat camsylate
Lanabecestat camsylate Chemical Structure CAS No.: 1522418-41-2
Product category: Others 3
This product is for research use only, not for human use. We do not sell to patients.
Size Price
500mg
1g
Other Sizes

Other Forms of Lanabecestat camsylate:

  • Lanabecestat HCl
  • AZD3293 (Lanabecestat)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: AZD3293 is a potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, BACE1 inhibitor with unique slow off-rate kinetics. When the potency of AZD3293 with respect to secretion of Aβ40 and sAβPPβ is studied in a range of cellular models, the compound displays pM potency in primary neuron cultures from mice and guinea pigs and in SH-SY5Y cells over-expressing AβPP (IC50 = 610 pM, 310 pM, and 80 pM, respectively). AZD3293 is also tested in a panel of more than 350 in vitro radioligand binding and enzyme activity assays, covering a diverse range of receptors, ion channels, transporters, kinases, and enzymes, up to a concentration of 10μM of AZD3293. A few significant responses are observed, but these had at least a 1,000-fold selectivity against BACE1, thus indicating specificity to BACE1. The off-rate of AZD3293 has an estimated t1/2 of approximately 9 h.


Kinase Assay: Lanabecestat (formerly known as AZD3293 and LY3314814), is a novel potent, orally bioactive, highly permeable, brain-penetreable inhibitor of 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.


Cell Assay: The cells [SH-SY5Y, SH-SY5Y overexpressing wild type AβPP, HEK293 cells overexpressing AβPP with the Swedish mutation (K595N/M596L), N2A cells, and primary cortical neurons isolated from fetal C57BL/6 mice (E16) or Dunkin-Hartley guinea pigs (E25-27)] are incubated with different AZD3293 concentrations for 5 to 16 h, and the release of sAβPPβ, Aβ1-40, Aβ1-42, or sAβPPα into the medium is analyzed using specific commercial ELISA or kits from Meso Scale Discovery.

ln Vivo
In vivo in mice, guinea pigs, and dogs, AZD3293 displays significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ. In the dog PK study, the bioavailability of AZD3293 is determined to be 80% (F = 0.8). 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.
Animal Protocol
Formulated in 5% dimethylacetamide in 0.3 M gluconic acid, pH 3; 50, 100, or 200μmol/kg; p.o.
C57BL/6 mice
References
J Alzheimers Dis.2016;50(4):1109-23.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C36H44N4O5S
Molecular Weight
644.83
Exact Mass
644.303
CAS #
1522418-41-2
Related CAS #
1383986-31-9 (HCl);1383982-64-6;1628076-74-3 (deleted);1522418-41-2 (camsylate);
PubChem CID
137091139
Appearance
Typically exists as solid at room temperature
LogP
6.157
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
5
Heavy Atom Count
46
Complexity
1230
Defined Atom Stereocenter Count
2
SMILES
S(CC12C(CC(CC1)C2(C)C)=O)(=O)(=O)O.O(C)C1CCC2(CC3C=CC(C4C=NC=C(C#CC)C=4)=CC=3[C@@]32N=C(C(C)=N3)N)CC1
InChi Key
PEOILZBROWEGCC-GWKIJFMESA-N
InChi Code
InChI=1S/C26H28N4O.C10H16O4S/c1-4-5-18-12-21(16-28-15-18)19-6-7-20-14-25(10-8-22(31-3)9-11-25)26(23(20)13-19)29-17(2)24(27)30-26;1-9(2)7-3-4-10(9,8(11)5-7)6-15(12,13)14/h6-7,12-13,15-16,22H,8-11,14H2,1-3H3,(H2,27,30);7H,3-6H2,1-2H3,(H,12,13,14)/t22?,25?,26-;7?,10-/m01/s1
Synonyms
O=S(C[C@@]1(C2(C)C)C(C[C@@]2([H])CC1)=O)(O)=O.NC(C(C)=N3)=NC43C5=C(C=CC(C6=CC(C#CC)=CN=C6)=C5)C[C@]74CCC(OC)CC7
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

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: > 80 mg/mL
Water:N/A
Ethanol:N/A
Solubility (In Vivo)
Lanabecestat camsylate; Lanabecestat;LY3314814; AZD3293 camsylate;LY-3314814 camsylate; AZD-3293;LY 3314814; AZD 3293
 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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