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Chemical Structure| 208255-80-5 Chemical Structure| 208255-80-5
Chemical Structure| 208255-80-5

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CAS No.: 208255-80-5

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DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor used as an auxiliary agent in cell therapy.

Synonyms: GSI-IX; LY-374973; N-(2FPhAc)Ala-phenyl-Gly t-butyl ester.

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Product Details of DAPT

CAS No. :208255-80-5
Formula : C23H26F2N2O4
M.W : 432.46
SMILES Code : O=C(OC(C)(C)C)[C@@H](NC([C@@H](NC(CC1=CC(F)=CC(F)=C1)=O)C)=O)C2=CC=CC=C2
Synonyms :
GSI-IX; LY-374973; N-(2FPhAc)Ala-phenyl-Gly t-butyl ester.
MDL No. :MFCD04974585
InChI Key :DWJXYEABWRJFSP-XOBRGWDASA-N
Pubchem ID :5311272

Safety of DAPT

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of DAPT

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Human induced pluripotent stem cell– and human embryonic stem cells–derived retinal organoids 50 μM 2 days DAPT did not drive significant differentiation PMC9513742
HEK293T cells 10 μM 12 h DAPT was used to inhibit γ-secretase activity to study the effect of H2O2 on γ-secretase activity. The results showed that pretreatment with DAPT significantly reduced the H2O2-induced luciferase activity, indicating that γ-secretase activity was inhibited. PMC2427353
SH-SY5Y cells 1-10 μM 3 h DAPT, as a γ-secretase inhibitor, was used to study the role of H2O2 in activating γ-secretase through the JNK-dependent pathway. The results showed that pretreatment with DAPT effectively reduced the H2O2-induced AICD level, indicating that γ-secretase activity was inhibited. PMC2427353
Non-differentiated embryonic multipotent mesenchymal progenitor cell line (10T1/2 cells) 10 μM overnight Inhibited Notch signaling and significantly downregulated Hes1, Acta2, and Cnn1 gene expression, suggesting these genes are downstream targets of Notch signaling. PMC8391929
Human coronary artery smooth muscle cells (HCASMCs) 10 μM overnight Inhibited Notch signaling and significantly attenuated the bead-bound Jagged1 induced gene response, suggesting a direct cause and effect of Notch signaling and gene expression. PMC8391929
C2C12 cells 10 μM 5 min, 15 min, 30 min, 1 h, 4 h To investigate the effect of the duration of Notch activation after DAPT removal on Hes1 and Hey1/L gene expression. The results showed that Hes1 responded strongly to brief pulses of Notch activation, while Hey1 and HeyL required sustained Notch activation. PMC6414217
Human Umbilical Vein Endothelial Cells (HUVEC) 10 μM 24 h To study the effect of DAPT on the cell cycle distribution of HUVEC, the results showed that DAPT treatment significantly reduced the proportion of cells in G1 phase and increased the proportion of cells in S/G2/M phase. PMC5732288
Human Umbilical Vein Endothelial Cells (HUVEC) 10 μM 1 h To verify whether fluid shear stress (FSS) induces NOTCH signaling, the results showed that FSS significantly increased the cleavage of the NOTCH intracellular domain (NICD), and this effect was blocked by pre-treatment with DAPT. PMC5732288

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice Wild-type and Gja4?/? mice Subcutaneous injection 100 mg/kg Injected once at 24 hours and once at 12 hours prior to killing To study the effect of DAPT on retinal vascular remodeling in mice, the results showed that DAPT treatment increased vascular density and reduced the expression of SMA and GJA5, indicating delayed arterial development. PMC5732288
Kunming mice Focal cerebral ischemia/reperfusion injury model Intraperitoneal injection 5 mL/kg Single dose, lasting 14 days DAPT significantly improved neurobehavioral scores and relieved neuronal morphological damage in mice with cerebral ischemia/reperfusion injury. DAPT decreased the number of glial fibrillary acidic protein- and Notch1-positive cells in the right prefrontal cortex, reduced the number of apoptotic cells, and downregulated Hes1 and Hes5 protein expression. PMC6334612
Mice Snail1 LOF mutant mice Subcutaneous injection 100 mg/kg Injected at E7.5, E8.5 and E9.5, embryos dissected at E10.5 To evaluate the rescue effect of DAPT on vascular defects in Snail1 LOF mutant mice. Results showed that DAPT partially restored vascular remodeling and branching in Snail1 LOF mutants. PMC4052376

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL

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