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DAPT (CAS 208255-80-5)

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Alternate Names:
Gamma-Secretase Inhibitor IX;N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-butyl ester
Application:
DAPT is a potent and specific inhibitor of γ-secretase
CAS Number:
208255-80-5
Purity:
≥95%
Molecular Weight:
432.46
Molecular Formula:
C23H26F2N2O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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DAPT is a potent and specific inhibitor of gamma-secretase. It may act to cause a reduction in Abeta40 and Abeta42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Abeta40 and Abeta42 respectively). There is evidence that DAPT does not effect APPalpha and APPbeta levels. It mimics notch signaling deficiencies at morphological, molecular and biochemical levels and may act to block notch signaling in hybrid human-mouse foetal thymus organ culture (FTOC).


DAPT (CAS 208255-80-5) References

  1. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain.  |  Dovey, HF., et al. 2001. J Neurochem. 76: 173-81. PMID: 11145990
  2. A gamma-secretase inhibitor blocks Notch signaling in vivo and causes a severe neurogenic phenotype in zebrafish.  |  Geling, A., et al. 2002. EMBO Rep. 3: 688-94. PMID: 12101103
  3. The gamma-secretase inhibitor N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester reduces A beta levels in vivo in plasma and cerebrospinal fluid in young (plaque-free) and aged (plaque-bearing) Tg2576 mice.  |  Lanz, TA., et al. 2003. J Pharmacol Exp Ther. 305: 864-71. PMID: 12626636
  4. Release of a membrane-bound death domain by gamma-secretase processing of the p75NTR homolog NRADD.  |  Gowrishankar, K., et al. 2004. J Cell Sci. 117: 4099-111. PMID: 15280425
  5. Different thresholds of Notch signaling bias human precursor cells toward B-, NK-, monocytic/dendritic-, or T-cell lineage in thymus microenvironment.  |  De Smedt, M., et al. 2005. Blood. 106: 3498-506. PMID: 16030192
  6. Reduction of Abeta levels in the Sprague Dawley rat after oral administration of the functional gamma-secretase inhibitor, DAPT: a novel non-transgenic model for Abeta production inhibitors.  |  El Mouedden, M., et al. 2006. Curr Pharm Des. 12: 671-6. PMID: 16472156
  7. Bleeding versus thrombosis: role of short DAPT in complex lesions.  |  Calcagno, S., et al. 2015. Minerva Cardioangiol. 63: 533-46. PMID: 26334115
  8. Short versus prolonged dual antiplatelet therapy (DAPT) duration after coronary stent implantation: A comparison between the DAPT study and 9 other trials evaluating DAPT duration.  |  Toyota, T., et al. 2017. PLoS One. 12: e0174502. PMID: 28931015
  9. ACC/AHA Versus ESC Guidelines on Dual Antiplatelet Therapy: JACC Guideline Comparison.  |  Capodanno, D., et al. 2018. J Am Coll Cardiol. 72: 2915-2931. PMID: 30522654
  10. Toward the Characterization of DAPT Interactions with γ-Secretase.  |  Aguayo-Ortiz, R., et al. 2019. ChemMedChem. 14: 1005-1010. PMID: 30925201
  11. Effect of 1-Month Dual Antiplatelet Therapy Followed by Clopidogrel vs 12-Month Dual Antiplatelet Therapy on Cardiovascular and Bleeding Events in Patients Receiving PCI: The STOPDAPT-2 Randomized Clinical Trial.  |  Watanabe, H., et al. 2019. JAMA. 321: 2414-2427. PMID: 31237644
  12. DAPT inhibits titanium particle-induced osteolysis by suppressing the RANKL/Notch2 signaling pathway.  |  Wei, X., et al. 2020. J Biomed Mater Res A. 108: 2150-2161. PMID: 32323420
  13. Dual Antiplatelet Therapy in Coronary Artery Disease.  |  Sharma, R., et al. 2020. Cardiol Ther. 9: 349-361. PMID: 32804330
  14. Validation of the 4-Item PRECISE-DAPT Score: A SWEDEHEART Study.  |  Wester, A., et al. 2021. J Am Heart Assoc. 10: e020974. PMID: 34612051
  15. DAPT Attenuates Cadmium-Induced Toxicity in Mice by Inhibiting Inflammation and the Notch/HES-1 Signaling Axis.  |  Yang, JY., et al. 2022. Front Pharmacol. 13: 902796. PMID: 35571137

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

DAPT, 5 mg

sc-201315
5 mg
$99.00

DAPT, 25 mg

sc-201315A
25 mg
$335.00

DAPT, 100 mg

sc-201315B
100 mg
$836.00

DAPT, 1 g

sc-201315C
1 g
$2099.00

Is this chemical cell permeable?

Asked by: Diniz
Yes, sc-201315/A is cell permeable. Please refer to the below below reference. Dovey, H F., et al., 2001. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. Journal of neurochemistry. 76(1): 173-81. PMID: 11145990 https://www.ncbi.nlm.nih.gov/pubmed/?term=11145990
Answered by: Technical Support
Date published: 2019-06-14

What are the shipping conditions?

Asked by: SCchem16
Thank you for your question. This chemical, DAPT: sc-201315, ships via ambient temperature.
Answered by: Chemical Support 2
Date published: 2017-03-06

Does this chemical inhibit any other targets besides y-secretase?

Asked by: SCchem16
Thank you for your question. This chemical, DAPT (CAS 208255-80-5), also indirectly inhibits Notch which is a γ-secretase substrate.
Answered by: Chemical Support 2
Date published: 2017-03-06
  • y_2025, m_11, d_13, h_10CST
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Rated 5 out of 5 by from Great results!It worked as expected. Would recommend. No complains.
Date published: 2022-06-28
Rated 5 out of 5 by from γ-secretase inhibitorA potent and specific inhibitor of γ-secretase. a good positive in γ-secretase research.
Date published: 2016-11-18
Rated 5 out of 5 by from Chen et alChen et al. (PubMed ID 20145246) used the -secretase inhibitor DAPT to elevate the level of -amyloid precursor protein (APP) C-terminal fragments (CTF). -SCBT Publication Review
Date published: 2015-01-03
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DAPT is rated 5.0 out of 5 by 3.
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