1. Immunology/Inflammation
  2. Complement System
  3. (Z)-Leukadherin-1

(Z)-Leukadherin-1 (Synonyms: ADH-503 free base)

Cat. No.: HY-15701A Purity: >98.0%
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(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.

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(Z)-Leukadherin-1 Chemical Structure

(Z)-Leukadherin-1 Chemical Structure

CAS No. : 2055362-72-4

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Based on 1 publication(s) in Google Scholar

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Description

(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses[1].

IC50 & Target

CD11b[1]

In Vitro

(Z)-Leukadherin-1 (ADH-503 free base; 4 μM; 8 days) reduces the numbers of total tumor-infiltrating CD11b+ cells and subsets of CD11b+ monocytes, granulocytes, eosinophils, and macrophages[1].

In Vivo

(Z)-Leukadherin-1 (ADH-503 free base; oral gavage; 30, 60, or 120 mg/kg; twice a day for 60 days) delayes tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival[1].
(Z)-Leukadherin-1 (oral gavage; 30, 100 mg/kg; twice a day; on days 1 and 5) has the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/ml and AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively[1].

Animal Model: KPC mice [p48-CRE/Lox-stop-Lox(LSL)-KrasG12D/p53flox/flox][1]
Dosage: 30, 60, or 120 mg/kg
Administration: Oral gavage; 60 days
Result: Delayed tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival.
Animal Model: Male rats[1]
Dosage: 30, 100 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage twice a day; on days 1 and 5
Result: Had the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/ml and AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively.
Molecular Weight

421.49

Formula

C₂₂H₁₅NO₄S₂

CAS No.

2055362-72-4

SMILES

O=C(O)C1=CC=C(C2=CC=C(/C=C(SC(N3CC4=CC=CC=C4)=S)/C3=O)O2)C=C1.[(Z)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

(Z)-Leukadherin-1ADH-503ADH503ADH 503Complement SystemorallyallostericCD11brepolarizationtumorassociatedmacrophagestumor-infiltratingimmunosuppressivedendriticInhibitorinhibitorinhibit

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(Z)-Leukadherin-1
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