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Dipeptidyl Peptidase III (DPP-III) Inhibitor Fluostatin A, B

Date:April 14 2022Web Page No:95022

Fluostatin A (Sodium Salt) and Fluostatin B is a natural compound derived from actinomycetes, and thye are selective inhibitors for human placental dipeptidyl peptidase III (DPP-III, DPP3) 1, 2). Fluostatin A is reported to be about 50 times more active against human DPP III than its homologue Fluostatin B.

What is DPP III

Dipeptidyl peptidase III (DPP III), a zinc-dependent aminopeptidase, is an enzyme involved in cleaving dipeptides from the N-terminus of tetra- to decapeptides, thereby taking part in activation as well as degradation of signalling peptides critical in physiological and pathological processes such as blood pressure regulation, nociception, inflammation and cancer.
DPP III is said to function as a regulator of the cellular oxidative stress response pathways, such as the Keap1-Nrf2-mediated antioxidative respons, and as a key modulator of the renin-angiotensin system related to blood pressure regulation. In addition, since DPP III degrades enkephalin, it is also known as enkephalinase B, so it has been suggested to be involved in the regulation of pain, and has attracted attention as a drug discovery target.

Reference

  • Malovan, G., et al., FEBS J., Mar. 12 (2022) doi: 10.1111/febs.16429. [PMID:35278345]

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Specification

Name Fluostatin A (Sodium Salt) Fluostatin B
Code 15403 14683
Structure Fluostatin-A-Structure Fluostatin-B-Structure
Overview
  • Fluostatin A was prepared from fluostatin B by chemical dehydration and oxidation.

  • Inhibits human placental DPP-III selectively
    (IC50: 0.44 μg/mL) 1).

  • No toxicity after intraperitoneal injection in mice at a dose of 100 mg/kg. 1)
  • Fluostatin B is derived from Streptomyces sp. TA-3391.

  • Inhibits human placental DPP-III selectively
    (IC50: 24 ug/mL) 1).

  • No toxicity after intraperitoneal injection in mice at a dose of 100 mg/kg. 1)
Purity >98% (HPLC) >98% (HPLC)
CAS No. 160219-74-9 (salt free form) * 158906-40-2
Molecular Formula C18H9O5 Na (sodium salt) C18H14O6
Molecular Weight 328.225 326.304
Solubility Soluble in H2O, DMSO
Poorly soluble in MeOH
Soluble in DMSO, partially soluble in EtOAc, Acetone
Insoluble in H2O

* Fluostatin A is supplied as sodium salt.

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Inhibitory activity against DPP enzyme subtype

Name Fluostatin A (Sodium Salt) Fluostatin B
Code 15403 14683
IC50
(μg/ml)
DPPⅠ>100>100
DPPⅡ>100>100
DPPⅢ0.4424.00
DPPⅣ>100>100

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References

  1. Akiyama, T., et al., J. Antibiot., 51 (6), 553~559 (1998). [PMID:9711218]
  2. Akiyama, T., et al., J. Antibiot., 51 (6), 586~588 (1998). [PMID:9711223]

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[Date : June 20 2024 00:07]

Detail Product Name Product Code Supplier Size Price
Fluostatin A (sodium salt), Dipeptidyl Peptidase Ⅲ (DPP-Ⅲ) Inhibitor
DatasheetThis may not be the latest data sheet.
15403 IMCInstitute of Microbial Chemistry 1 mg $500

Description
Storage -20°C CAS 160219-74-9 (salt free form)
Link

Bioactive Compounds

Fluostatin B,Dipeptidyl Peptidase III (DPP-III) Inhibitor
DatasheetThis may not be the latest data sheet.
14683 IMCInstitute of Microbial Chemistry 1 mg $500

Description
Storage -20°C CAS 158906-40-2
Link

Bioactive Compounds

[Date : June 20 2024 00:07]

Fluostatin A (sodium salt), Dipeptidyl Peptidase Ⅲ (DPP-Ⅲ) Inhibitor


  • Product Code: 15403
  • Supplier: IMC
  • Size: 1mg
  • Price: $500

Description
Storage -20°C CAS 160219-74-9 (salt free form)
Link

Bioactive Compounds

Fluostatin B,Dipeptidyl Peptidase III (DPP-III) Inhibitor


  • Product Code: 14683
  • Supplier: IMC
  • Size: 1mg
  • Price: $500

Description
Storage -20°C CAS 158906-40-2
Link

Bioactive Compounds


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