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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P646348-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $390.90 | |
P646348-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $590.90 | |
P646348-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,200.90 | |
P646348-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,950.90 | |
P646348-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,750.90 |
Synonyms | PF-06751979|1818339-66-0|1Y0Y126GUG|2-Pyridinecarboxamide, N-[2-[(4aR,6S,8aR)-2-amino-4,4a,5,6-tetrahydro-6-methylpyrano[3,4-d][1,3]thiazin-8a(8H)-yl]-4-thiazolyl]-5-(difluoromethoxy)-|N-(2-((4aR,6S,8aR)-2-Amino-6-methyl-4a,5,6,8-tetrahydro-4H-pyrano(3,4- |
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Specifications & Purity | ≥99% |
Biochemical and Physiological Mechanisms | PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 ( BACE1 ) inhibitor with an IC 50 of 7.3 nM in BACE1 binding assay. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 ( BACE1 ) inhibitor with an IC 50 of 7.3 nM in BACE1 binding assay. In Vitro PF-06751979 shows improved selectivity over BACE2 (IC 50 =194 nM) in binding (27-fold) relative to the literature examples and across multiple chemical series in BACE1 program. PF-06751979 also inhibits BACE1 and BACE2 in a fluorescent polarization (FP) assay with IC 50 s of 26.9 nM and 238 nM, respectively. PF-06751979 has excellent potency at BACE1 in binding or FP assay formats along with cellular activity looking at production of sAPPβ in H4 cells with an IC 50 of 5 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PF-06751979 displays excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases including BACE2. Acute administration of PF-06751979 yields a robust dose-responsive and time-dependent reduction of cerebral spinal fluid (CSF) Aβx-40 with peak inhibition at 3 h of >77%. To determine if the reduction in brain and CSF Aβ is maintained during sustained exposure to PF-06751979, a 5 day subchronic study is executed, dosing once daily by subcutaneous (SC) administration (10 or 50 mg/kg/day). Brain and CSF samples are collected on day 5, following the last dose. PF-06751979 produces a dose-responsive and time-dependent inhibition of Aβ42 in mouse brain. At the 50 mg/kg/day dose, maximal brain lowering is 63% at 7 to 9 h. Administration of PF-06751979 (10 or 50 mg/kg/day for 5 days) produces a dose-responsive and time-dependent inhibition of Aβx-40 in mouse CSF resulting in 77% inhibition of CSF at 3 h post-final 50 mg/kg dose . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 7.3 nM (BACE1), 194 nM (BACE2) |
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IUPAC Name | N-[2-[(4aR,6S,8aR)-2-amino-6-methyl-4a,5,6,8-tetrahydro-4H-pyrano[3,4-d][1,3]thiazin-8a-yl]-1,3-thiazol-4-yl]-5-(difluoromethoxy)pyridine-2-carboxamide |
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INCHI | InChI=1S/C18H19F2N5O3S2/c1-9-4-10-6-30-17(21)25-18(10,8-27-9)15-24-13(7-29-15)23-14(26)12-3-2-11(5-22-12)28-16(19)20/h2-3,5,7,9-10,16H,4,6,8H2,1H3,(H2,21,25)(H,23,26)/t9-,10-,18-/m0/s1 |
InChi Key | ZLZUHACSRMOLLV-RAALSFIWSA-N |
Canonical SMILES | CC1CC2CSC(=NC2(CO1)C3=NC(=CS3)NC(=O)C4=NC=C(C=C4)OC(F)F)N |
Isomeric SMILES | C[C@H]1C[C@H]2CSC(=N[C@]2(CO1)C3=NC(=CS3)NC(=O)C4=NC=C(C=C4)OC(F)F)N |
Alternate CAS | 1818339-66-0 |
PubChem CID | 118435360 |
MeSH Entry Terms | 2-Pyridinecarboxamide, N-(2-((4aR,6S,8aR)-2-amino-4,4a,5,6-tetrahydro-6-methylpyrano(3,4-d)(1,3)thiazin-8a(8H)-yl)-4-thiazolyl)-5-(difluoromethoxy)-;N-(2-((4aR,6S,8aR)-2-Amino-6-methyl-4,4a,5,6-tetrahydropyrano(3,4-d)(1,3)thiazin-8a(8H)-yl)-1,3-thiazol-4- |
Molecular Weight | 455.50 |
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Solubility | DMSO : 150 mg/mL (329.31 mM; Need ultrasonic) Ethanol : 50 mg/mL (109.77 mM; Need ultrasonic) |
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