2. Neuronal Signaling
  3. Beta-secretase
  4. Umibecestat

Umibecestat  (Synonyms: CNP520)

Cat. No.: HY-119689 Purity: 99.88%
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Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease.

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

Umibecestat Chemical Structure

Umibecestat Chemical Structure

CAS No. : 1387560-01-1

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1 mg USD 214 In-stock
5 mg USD 450 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2550 In-stock
100 mg USD 3800 In-stock
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Based on 1 publication(s) in Google Scholar

Umibecestat Related Antibodies

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Description

Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively[1]. Umibecestat can be used for the research of alzheimer's disease.

IC50 & Target

IC50: 11 nM (human BACE-1), 10 nM (mouse BACE-1)[1]
In Vitro

Umibecestat (CNP520) is a potent BACE-1 inhibitor that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D[1].

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

Umibecestat Related Antibodies
In Vivo

Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows a dose-dependent effects on Aβ40 and a long duration of action in both rat brain and CSF[1].
Umibecestat (CNP520) (3.1 mg/kg; oral administration; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days[1].

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

Animal Model: Male rats (3-4 months old)[1]
Dosage: 1.5 mg/kg (3 μM/kg)-51.3 mg/kg (100 μM/kg)
Administration: Given by oral gavage; 72 hours
Result: Reduced 89.3±4.5% Aβ40 at the highest dose in brain tissue, and 50% lowering of rat brain Aβ40 (ED50) was 2.4±0.31 mg/kg. Reduced ~50% Aβ40 at a single oral 30 μM/kg (15.4 mg/kg) dose after 24 hours in both rat brain and CSF。
Animal Model: 3-month-old beagle dogs[1]
Dosage: 3.1 mg/kg (6 μM/kg)
Administration: Oral administration; 7 days
Result: Both Aβ40 and Aβ42 concentrations in CSF showed a > 75% reduction at 12-48 h after dosing and returned slowly to baseline over the next 7 days.
Clinical Trial
Molecular Weight

513.80

Formula

C19H15ClF7N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC([C@@]2(CO[C@](C)(C(N)=N2)C(F)(F)F)C)=C(C=C1)F)C3=NC=C(C=C3Cl)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (194.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9463 mL 9.7314 mL 19.4628 mL
5 mM 0.3893 mL 1.9463 mL 3.8926 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9463 mL 9.7314 mL 19.4628 mL 48.6571 mL
5 mM 0.3893 mL 1.9463 mL 3.8926 mL 9.7314 mL
10 mM 0.1946 mL 0.9731 mL 1.9463 mL 4.8657 mL
15 mM 0.1298 mL 0.6488 mL 1.2975 mL 3.2438 mL
20 mM 0.0973 mL 0.4866 mL 0.9731 mL 2.4329 mL
25 mM 0.0779 mL 0.3893 mL 0.7785 mL 1.9463 mL
30 mM 0.0649 mL 0.3244 mL 0.6488 mL 1.6219 mL
40 mM 0.0487 mL 0.2433 mL 0.4866 mL 1.2164 mL
50 mM 0.0389 mL 0.1946 mL 0.3893 mL 0.9731 mL
60 mM 0.0324 mL 0.1622 mL 0.3244 mL 0.8110 mL
80 mM 0.0243 mL 0.1216 mL 0.2433 mL 0.6082 mL
100 mM 0.0195 mL 0.0973 mL 0.1946 mL 0.4866 mL
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Umibecestat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Umibecestat1387560-01-1CNP520CNP 520CNP-520Beta-secretaseBACEβ-SecretaseInhibitorinhibitorinhibit

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