Successful, we will reply to you quickly.

OK

Please select the quantity.

OK

Your message is being sent, please wait.

Close

test

Close

Send mail failed, please send again!

Close

Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

LY-411575

HY-50752

(LY411575; LY 411575)

LY-411575

LY-411575 Chemical Structure

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $198 In-stock
50 mg $590 In-stock
100 mg $960 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €119 In-stock
5 mg €108 In-stock
10 mg €194 In-stock
50 mg €578 In-stock
100 mg €941 In-stock
200 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Bulk Inquiry

Inquiry Information
Product name: LY-411575
Cat. No.: HY-50752

LY-411575 Data Sheet

  • View current batch:

    Purity: 98.96%

  • Network Version

    DataSheet

    Pdf Version Network Version

    MSDS

    Pdf Version

    COA

Customer View

Related Compound Libraries

Biological Activity of LY-411575

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with IC50 of 0.39 nM.
IC50 value:  0.078 nM/0.082 nM (membrane/cell-based) [1]
Target: γ-secretase
in vitro: LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage [1]. LY-411575, which blocks Notch activation, results in apoptosis in primary and immortalized KS cells [2].
in vivo: 10 mg/kg oral dose of LY-411575 decreases brain and plasma Aβ40 and -42 dose-dependently. [1] LY-411575 reduces cortical Aβ40 in young (preplaque) transgenic CRND8 mice (ED50 ≈ 0.6 mg/kg) and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg). The therapeutic window is similar after oral and subcutaneous administration and in young and aged CRND8 mice. Both the thymus and intestinal side effects are reversible after a 2-week washout period. Three-week treatment with 1 mg/kg LY411575 reduces cortical Aβ40 by 69% without inducing intestinal effects, although a previously unreported change in coat color is observed [3].

Protocol (Extracted from published papers and Only for reference)

More

Chemical Information

M.Wt 479.48 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C26H23F2N3O4
CAS No 209984-57-6
Solvent & Solubility

DMSO: 95 mg/mL, H2O: <1 mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.0856 mL 10.4280 mL 20.8559 mL
5 mM 0.4171 mL 2.0856 mL 4.1712 mL
10 mM 0.2086 mL 1.0428 mL 2.0856 mL

Clinical Information of LY-411575

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
LY-411575 Eli Lilly & Co Alzheimers disease 31-DEC-09 30-APR-11 Phase 3 16-AUG-11
Eli Lilly & Co Alzheimers disease 31-MAR-08 31-MAY-11 Phase 3 04-OCT-13
Eli Lilly & Co Alzheimers disease 31-OCT-05 31-DEC-06 Phase 2 24-APR-12
Eli Lilly & Co Alzheimers disease 31-JUL-06 30-SEP-07 Phase 1 18-JUN-09
Eli Lilly & Co Alzheimers disease 30-SEP-08 30-APR-11 Phase 3 24-AUG-11

References on LY-411575

Other Forms

Inhibitor Kit

Related γ-secretase Products

  • BMS 299897

    BMS 299897 is a sulfonamide <b>(gamma)-secretase</b> inhibitor with an <b>IC<sub>50</sub></b> of 7 nM for A(beta) production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).

  • BMS-708163

    Avagacestat (BMS-708163) is a potent, selective, orally bioavailable (gamma)-secretase inhibitor of A(beta)40 and A(beta)42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch.

  • CHF5074

    CHF5074 is a novel (gamma)-secretase modulator, reduces A(beta)42 and A(beta)40 secretion, with an IC50 of 3.6 and 18.4 (mu)M, respectively.

  • DAPT

    DAPT(GSI-IX) is an inhibitor of (gamma)-secretase; DAPT causes a reduction in A(beta)40 and A(beta)42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total A(beta) and A(beta)42 respectively) and in brain extract, cerebrospinal fluid and plasma in vivo.

  • E 2012

    E 2012 is a potent (gamma)-secretase modulator.

  • gamma-secretase modulator 1

    (gamma)-secretase inhibitior-1 is a gamma-secretase modulator, (gamma)-secretase inhibitior-1 is useful for Alzheimer(acute)s disease.

  • gamma-secretase modulator 2

    gamma-secretase modulator 2 is a potent and selective (gamma)-secretase modulator for treatment of Alzheimer(acute)s disease.

  • gamma-secretase modulator 3

    gamma-secretase modulator 3 is a gamma-secretase modulator.

  • L-685458

    L-685458 is a potent inhibitor of Amyloid (beta)-Protein precursor (gamma)-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested.

  • RO4929097

    RO4929097 is a (gamma) secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of A(beta)40 and Notch with EC50 of 14 nM and 5 nM, respectively.

MORE