SML3144

delta-Secretase inhibitor, CP11

≥95% (HPLC)

• Synonym(e): δ-Secretase inhibitor 11, δ-Secretase inhibitor, compound 11, δ-Secretase inhibitor, compound 11A, 7-(4-Morpholinyl)-2,1,3-benzoxadiazol-4-amine, 7-(Morpholin-4-yl)-2,1,3-benzoxadiazol-4-amine, 7-Morpholin-4-yl-benzo[1,2,5]oxadiazol-4-ylamine, CP11, CPA, delta-Secretase inhibitor, compound 11
• Empirische Formel (Hill-System): C₁₀H₁₂N₄O₂
• CAS-Nummer: 842964-18-5
• Molekulargewicht: 220.23
• UNSPSC Code: 12352200
• NACRES: NA.28
• MDL number: MFCD03422529
• Assay: ≥95% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: powder
• color: , Faint Brown to dark red
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: N3(CCOCC3)c1c2n[o]nc2c(cc1)N
• InChI: 1S/C10H12N4O2/c11-7-1-2-8(10-9(7)12-16-13-10)14-3-5-15-6-4-14/h1-2H,3-6,11H2
• InChI key: LWCSTSZSZFUHAT-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

Compound 11 (CP11) is an orally active and brain-penetrant delta-secretase (δ-secretase; AEP) inhibitor that selectively blocks AEP (IC50 = 710 nM) but not other related cysteine proteases (Caspase-3/-8 IC50 = 31.86/86.71 μM, Cathepsin-S/-L IC50 >200 μM) via a dual active site-directed and allosteric mode of inhibition. CP11 inhibits Pala cellular AEP activity in cultures (IC50 = 800 nM) and improves cognitive functions in murine models of Alzheimer′s disease (AD) in vivo (10 mg/kg tau P301S or 5xFAD mice via daily p.o.) by reducing tau and APP cleavage, ameliorating synapse loss and augmenting long-term potentiation.

Orally active, brain-penetrant, selective delta-secretase (δ-secretase; AEP) inhibitor that improves cognitive functions in murine models of Alzheimer′s disease (AD).

Sicherheitshinweise

• pictograms: GHS06
• signalword: Danger
• hcodes: H302,H311
• pcodes: P264 - P270 - P280 - P301 + P312 - P302 + P352 + P312 - P361 + P364
• Hazard Classifications: Acute Tox. 3 Dermal - Acute Tox. 4 Oral
• Lagerklasse: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable