1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter
  3. AR-C117977

AR-C117977 is a potent monocarboxylate transporter (MCT1) inhibitor. AR-C117977 prolongs the survival of skin and heart sllograft. AR-C117977 inhibits the development of transplant arteriosclerosis in aortic allografts partially, but was unable to inhibit alloantibody production after transplantation. AR-C117977 shows potent immunosuppressive properties in vivo effectively preventing acute but not chronic allograft rejection in the mouse.

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AR-C117977

AR-C117977 Chemical Structure

CAS No. : 216685-07-3

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Description

AR-C117977 is a potent monocarboxylate transporter (MCT1) inhibitor. AR-C117977 prolongs the survival of skin and heart sllograft. AR-C117977 inhibits the development of transplant arteriosclerosis in aortic allografts partially, but was unable to inhibit alloantibody production after transplantation. AR-C117977 shows potent immunosuppressive properties in vivo effectively preventing acute but not chronic allograft rejection in the mouse[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
>1000 nM
Compound: 1
Antiproliferative activity against HEK293 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against HEK293 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
HEK293 IC50
>1 μM
Compound: 1
Antiproliferative activity against HEK293 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against HEK293 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
HT-29 IC50
>1000 nM
Compound: 1
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
HT-29 IC50
>1 μM
Compound: 1
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
HUVEC IC50
>1000 nM
Compound: 1
Antiproliferative activity against human HUVEC assessed as inhibition of acidic FGF-stimulated cell proliferation by fluorimetric assay
Antiproliferative activity against human HUVEC assessed as inhibition of acidic FGF-stimulated cell proliferation by fluorimetric assay
[PMID: 16370372]
HUVEC IC50
>1000 nM
Compound: 1
Antiproliferative activity against human HUVEC assessed as inhibition of basic FGF-stimulated cell proliferation by fluorimetric assay
Antiproliferative activity against human HUVEC assessed as inhibition of basic FGF-stimulated cell proliferation by fluorimetric assay
[PMID: 16370372]
HUVEC IC50
>1 μM
Compound: 1
Antiproliferative activity against human HUVEC assessed as inhibition of acidic FGF-stimulated cell proliferation by fluorimetric assay
Antiproliferative activity against human HUVEC assessed as inhibition of acidic FGF-stimulated cell proliferation by fluorimetric assay
[PMID: 16370372]
K562 IC50
>1000 nM
Compound: 1
Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
K562 IC50
>1 μM
Compound: 1
Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
Keratinocyte IC50
>1000 nM
Compound: 1
Antiproliferative activity against human primary epidermal keratinocytes assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human primary epidermal keratinocytes assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
Keratinocyte IC50
>1 μM
Compound: 1
Antiproliferative activity against human primary epidermal keratinocytes assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human primary epidermal keratinocytes assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
PANC-1 IC50
>1000 nM
Compound: 1
Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
PANC-1 IC50
>1 μM
Compound: 1
Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
SW480 IC50
>1000 nM
Compound: 1
Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
SW480 IC50
>1 μM
Compound: 1
Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
T-24 IC50
>1000 nM
Compound: 1
Antiproliferative activity against human T24 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human T24 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
T-24 IC50
>1 μM
Compound: 1
Antiproliferative activity against human T24 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human T24 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
THP-1 IC50
>1000 nM
Compound: 1
Antiproliferative activity against human THP1 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human THP1 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
THP-1 IC50
>1 μM
Compound: 1
Antiproliferative activity against human THP1 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human THP1 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
ZR-75-1 IC50
>1000 nM
Compound: 1
Antiproliferative activity against human ZR-75-1 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human ZR-75-1 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
ZR-75-1 IC50
>1 μM
Compound: 1
Antiproliferative activity against human ZR-75-1 cells assessed as inhibition of cell proliferation by fluorimetric assay
Antiproliferative activity against human ZR-75-1 cells assessed as inhibition of cell proliferation by fluorimetric assay
[PMID: 16370372]
Molecular Weight

468.63

Formula

C25H28N2O3S2

CAS No.
SMILES

O=C1N(CC(C)C)C2=C(C(SCCCO)=C(CC3=C4C=CC=CC4=CC=C3)S2)C(N1C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Molarity Calculator

  • Dilution Calculator

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AR-C117977
Cat. No.:
HY-114602
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