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Neuroscience

5-HT Receptor

(572)

AAK1 (AP2 associated kinase 1)

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(47)

iGluR

(118)

BACE

Beta-secretase 1 (BACE1), also known as beta-site amyloid precursor protein cleaving enzyme 1, beta-site APP cleaving enzyme 1, membrane-associated aspartic protease 2, memapsin-2, aspartyl protease 2, and ASP2, is an enzyme that in humans is encoded by the BACE1 gene. Expression of BACE1 is observed mainly in neurons.BACE1 is an aspartic-acid protease important in the formation of myelin sheaths in peripheral nerve cells: in mice the expression of BACE1 is high in the postnatal stages, when myelination occurs.

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Timosaponin BII

T3394136656-07-0

Timosaponin BII (Prototimosaponin A III) exhibits anti-dementia and antioxidant activities, with potential applications in treating type 2 diabetes. It can inhibit the up-regulation of BACE1 and reduce the over-production of β-CTF and Aβ in rat retina induced by FeCl.

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Atabecestat

T143381200493-78-2In house

Atabecestat (JNJ-54861911) is a potent, brain-penetrant, and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor that achieves robust and high CSF Aβ reduction, is well-tolerated, and displays sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment[1].

$132

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Umibecestat

T132531387560-01-1

Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), 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.

$175

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Epiberberine

T5S23616873-09-2

1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf MEK1 ERK1 2 and AMPKα Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.

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Epiberberine chloride

T8306889665-86-5

Epiberberine chloride, a natural pro-berberine from Coptis chinensis Franch. is an AChE, BChE, and BACE1 inhibitor with IC50 values of 1.07, 6.03, and 8.55 μM, respectively.Epiberberine chloride has antioxidant effects and inhibits the effects of Ca9-22 and Fa2R. Epiberberine chloride has antioxidant effects, inhibits the motility of Ca9-22 and FaDu cell lines, and can be used to study hyperlipidemia, Alzheimer's disease and diabetes.

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Loganin

T275918524-94-2

Loganin (Loganoside), an iridoid glucoside, has been reported to be an inhibitor of Cox-1 and also noted to suppress TNF-α formation. This compound also has displayed potent free-radical-scavenging activity and inhibitory effects on melanogenesis.

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Cited

Phytic acid potassium

T5075129832-03-7

Phytic acid dipotassium salt is an endogenous metabolite that inhibits β-secretase 1 (BACE1).

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Auraptene

T4115495-02-3

Auraptene is a coumarin derived from citrus plants that bears a geranyloxyl moiety at its C-7. It has anti-inflammatory, anti-carcinogenic, anti-bacterial, neuroprotective, and hepatoprotective activities. It inhibits leukocyte activation and induces phas

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Verubecestat

T70111286770-55-5

Verubecestat (MK-8931) (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.

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LY2811376

T26391194044-20-6

LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.

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NB-360

T121881262857-73-7

NB-360 is a potent and brain-penetrable inhibitor of BACE1 and BACE2 with IC50s of 5, 5, and 6 nM for mouse and human BACE1 and BACE2. NB-360 exhibits excellent selectivity over the related aspartyl proteases pepsin, cathepsin E, and cathepsin D.

$112

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Elenbecestat

T111751388651-30-6

Elenbecestat (E2609) is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.

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Anatabine

TN3410581-49-7

Anatabine shows anti-inflammatory activity in vitro and in vivo, which is mediated in part via an inhibition of STAT3 phosphorylation.Anatabine has anti-Alzheimer's disease effects, it inhibits BACE-1 transcription and reduces BACE-1 protein levels in hum

$308

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Aloeresin D

T8179105317-67-7

Aloeresin D, a natural chromone glycoside, inhibits β-Secretase (BACE1) activity (IC50: 39 μM).

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DSS30

T61439883027-32-5In house

DSS30 is a P25/CDK5 inhibitor.DSS30 acts by inhibiting the phosphorylation of amyloid precursor protein cleaving enzyme 1 (BACEl), which reduces the secretion of β-amyloid (Aβ).DSS30 can be used for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease.

$350

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SEW06622

T83616261349-28-4

SEW06622 is a potent inhibitor of acetylcholinesterase (AChE) and beta-secretase-1 (BACE-1) and is a potential candidate for the treatment of Alzheimer's disease.

$195

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8-Geranyloxypsoralen

TN13437437-55-0

8-Geranyloxypsoralen inhibits α2-secretase (BACE1) activity in non-competitive manner, with the IC(50) values <25.0 μM, it can induce vasorelaxation on rat arterial tissues. 8-Geranyloxypsoralen possesses nematicidal activities, the median lethal concentrations (LC(50)) is 188.3 mg L against B. xylophilus and is 117.5 mg L against P. redivivus.

$156

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LY2886721

T60581262036-50-9

LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.

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AZD3839 free base

T67721227163-84-9

AZD3839 free base is a potent and selective BACE1 inhibitor with a Ki of 26.1 nM, demonstrating approximately 14-fold selectivity over BACE2. [Phase 1]

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BACE-IN-1 acetate

T3161L

BACE-IN-1 acetate (BACE-IN-1 acetate (350228-37-4，Free base)) has been used as β-site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) inhibitor in BACE1 inhibitor assay. β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1), an aspartic protease belongs to the protease family of enzymes comprises of six luminal cysteine residues. These residues help in the formation of three intermolecular disulfide bonds and N-linked glycosylation sites.

$148

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LX2343

T4398333745-53-2

LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM and acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. Additionally, LX2343 stimulates autophagy, promoting Aβ clearance.

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Lanabecestat

TQ02381383982-64-6

Lanabecestat (AZD3293) is a highly potent and highly permeable, orally active BACE1 inhibitor (Ki: 0.4 nM) that crosses the blood-brain barrier, Lanabecestat can be used for the study of neurological diseases like Alzheimer's disease.

$149

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BACE1-IN-1

T104501310347-50-2

BACE1-IN-1 is a high brain penetrant BACE1 inhibitor (IC50s: 32 and 47 nM for human BACE1 and BACE2).

$1,650

8-10 weeks

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AM-6494

T102921874232-80-0

AM-6494, a potent and orally active BACE1 inhibitor (IC50: 0.4 nM), exhibits in vivo selectivity over BACE2 (IC50: 18.6 nM).

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10-14 weeks

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Sophoflavescenol

TN2217216450-65-6

Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , these effects might contribute to the antitumor activity without severe side effects. Sophoflaves

$657

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Putraflavone

TN486523624-21-7

Putraflavone possesses a good antioxidant activity via its DPPH free radical scavenging.

$1,960

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Questin

TN21313774-64-9

Questin is an antimicrobial agent derived from Aspergillus florescens with an antimicrobial activity profile that inhibits V. harveyi, V. anguillarum, V. cholerae and V. parahemolyticus with MIC values of 31.25 µg/mL, 62.5 µg/mL, 62.5 µg/mL and 125 µg/mL, respectively. Questin has good potential to inhibit AChE, BChE and BACE1 and may be used in the development of drugs for the treatment or prevention of Alzheimer's disease.

$813

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Kushenol C

TN439999119-73-0

Kushenol C is a good 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenger, and it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2). Kushenol C shows antimicrobial activity against Staphylococcus aureus and Streptococcus mutan

$1,329

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7-O-Methylaloeresin A

TN1332329361-25-3

7-O-Methylaloeresin A shows significant antioxidant activity, it also has moderate inhibitory active on BACE.

$290

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PF-06751979

T124291818339-66-0

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

$1,230

10-14 weeks

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BACE1-IN-5

T104532581114-83-0

BACE1-IN-5 (Compound 15), a potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, demonstrates significant efficacy with an IC50 of 9.1 nM for BACE1 inhibition and an impressive IC50 of 0.82 nM against cellular amyloid-β (Aβ) production. Additionally, it is engineered to enhance hERG inhibition and P-gp efflux, indicating its optimized medicinal chemistry profile [1].