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Chemical Structure| 106362-34-9 Chemical Structure| 106362-34-9

Structure of DAPTA
CAS No.: 106362-34-9

Chemical Structure| 106362-34-9

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DAPTA is a potent and selective CCR5 antagonist.

Synonyms: D-Ala-peptide T-amide; Adaptavir; Monomeric (D-Alanine-1) Peptide T amide

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Product Details of DAPTA

CAS No. :106362-34-9
Formula : C35H56N10O15
M.W : 856.88
SMILES Code : OC1=CC=C(C[C@H](NC([C@@H](NC([C@H]([C@H](O)C)NC([C@@H](NC([C@H]([C@H](O)C)NC([C@@H](NC([C@H](N)C)=O)CO)=O)=O)[C@H](O)C)=O)=O)CC(N)=O)=O)C(N[C@H](C(N)=O)[C@H](O)C)=O)C=C1
Synonyms :
D-Ala-peptide T-amide; Adaptavir; Monomeric (D-Alanine-1) Peptide T amide
MDL No. :MFCD00076838
InChI Key :AKWRNBWMGFUAMF-ZESMOPTKSA-N
Pubchem ID :184644

Safety of DAPTA

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

Related Pathways of DAPTA

GPCR

Isoform Comparison

Biological Activity

Target
  • CCR

    CM235-CCR5, IC50:0.32 nM

    gp120 Bal-CCR5, IC50:0.06 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 0.1 mM 6 hours DAPTA significantly reduced CSE-induced tight junction injury and inhibited the downregulation of ZO-1, occludin, CCL3, and CCR5 expression by CSE. PMC8089484
16-HBE cells 0.1 mM 6 hours DAPTA significantly reduced CSE-induced tight junction injury and inhibited the downregulation of ZO-1, occludin, CCL3, and CCR5 expression by CSE. PMC8089484

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice CSE-induced COPD Mice model Subcutaneous injection 10 μg/kg Once daily for 6 weeks DAPTA partially reversed the negative effects of CSE on lung function and tight junction protein expression in mice, reducing alveolar space enlargement and inflammatory responses. PMC8089484
ApoE−/− mice Atherosclerosis model Tail vein injection 370 kBq 1, 4, and 24 hours To evaluate the pharmacokinetics and targeting efficiency of DAPTA-Comb nanoparticles in an atherosclerosis model. Results showed extended blood circulation of 10%, 25%, and 40% DAPTA-Comb, with 40% DAPTA-Comb demonstrating higher plaque targeting efficiency. PMC8737066
Sprague-Dawley rats Conscious adult and juvenile rats Intracerebroventricular (ICV) administration 400 ng (acute), 2 ng (chronic) Acute: single injection; chronic: twice daily for 5 days To investigate the effect of gp120 on GH release and body weight, results showed gp120 significantly suppressed GH release and caused weight loss PMC19215
SJL/J mice Experimental autoimmune encephalomyelitis (EAE) model Intraperitoneal injection 0.01 mg/kg Once daily from day 14 to day 42 after immunization To evaluate the therapeutic potential of DAPTA in EAE mice, results showed that DAPTA significantly reduced the expression of NF-κB p65, Notch-1, Notch-3, GM-CSF, MCP-1, iNOS, and TNF-α, while increasing the expression of IκBα. PMC10294823
SJL/J mice Experimental autoimmune encephalomyelitis (EAE) model Intraperitoneal injection 0.01 mg/kg Once daily from day 14 to day 42 DAPTA treatment significantly reduced the expression of NF-κB p65, Notch-1, Notch-3, GM-CSF, MCP-1, iNOS, and TNF-α in EAE mice, while increasing the expression of IκBα. PMC10294823

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00951743 HIV Infections Phase 2 Unknown July 2010 United States, District of Col... More >>umbia Whitman Walker Clinic Recruiting Washington, District of Columbia, United States, 20009 Principal Investigator: Richard Elion, MD Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.17mL

0.23mL

0.12mL

5.84mL

1.17mL

0.58mL

11.67mL

2.33mL

1.17mL

References

 

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