Search Result
Results for "
fibroblast activation
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-145983
-
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FAP
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Cancer
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Suc-Gly-Pro-AMC is a fibroblast activation protein (FAP)-specific substrate. Suc-Gly-Pro-AMC can be used to study the activity of FAP .
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-
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- HY-147173
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FAP
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Cancer
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FAPI-74 is a PET (positron emission tomography) tracer targeting the fibroblast activation protein (FAP). FAPI-74 can be used for FAP-positive tumor research .
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- HY-147057A
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FAP
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Cancer
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FAP-2286 acetate is the conjugate of a fibroblast activation protein (FAP)-binding peptide. FAP-2286 acetate can be labeled with radionuclides for diagnostic applications. FAP-2286 acetate has antitumor activity .
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- HY-149860
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FAP
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Cancer
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FAP-IN-1 is a fibroblast activation protein (FAP) inhibitor with an IC50 value of 3.3 nM. FAP-IN-1 can be used for the research of cancer .
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- HY-162334
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Others
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Inflammation/Immunology
Cancer
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HYOU1-IN-1 (Compound 33) is an inhibitor of hypoxia-upregulated protein 1 (HYOU1) with anti-inflammatory activity. HYOU1-IN-1 can be used in research on the regulation of fibroblast activation, chronic inflammation, and fibrotic diseases .
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-
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- HY-128643
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FAP
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Cancer
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FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios .
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- HY-137331
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FAPI-46
1 Publications Verification
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FAP
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Cancer
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FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI-46 can be used for tumor imaging of a multitude of different cancers .
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- HY-153552A
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FAP
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Cancer
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NH2-UAMC1110 TFA is a UAMC1110 derivative that can be used in the synthesis of FAPI-QS. UAMC1110 is a fibroblast activation protein (FAP) inhibitor. FAPI-QS is a chelating agent that can be used to synthesize high tumor selectivity and high dose radiotracers for the diagnosis and treatment of tumors .
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- HY-146180
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FAP
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Cancer
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FSDD0I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD0I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging .
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- HY-146181
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FAP
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Cancer
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FSDD1I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD1I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging .
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- HY-146182
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FAP
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Cancer
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FSDD3I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD3I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging .
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- HY-P99902
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FAP-IL2v
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Interleukin Related
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Cancer
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Simlukafusp alfa (FAP-IL2v) is an immunocytokine comprising an antibody against fibroblast activation protein α (FAPα) and an IL-2 variant that only binds IL-2Rβγ. Isotype: human IgG1 .
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- HY-128642
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FAP
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Cancer
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FAPI-2 is a quinoline-based therapeutic ligand targeting fibroblast activator protein. FAPI-2, a ligand for the synthesis of 68Ga-FAPI-2, is a PET tracer. FAPI-2 is a fibroblast activating protein (FAP) inhibitor that can be used in cancer research .
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- HY-145938
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FAP
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Cancer
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OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
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- HY-128642A
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FAP
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Cancer
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FAPI-2 TFA is a fibroblast activation protein (FAP) inhibitor with potential use in cancer research .
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- HY-160289
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Proteasome
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Cancer
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ARI-3144 is an excellent substrate for fibroblast activation protein (FAP). ARI-3144 is a FAP-activated proteasome inhibitor that can be used for the research of solid tumors .
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- HY-139401
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FAP
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Cancer
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FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).
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- HY-161262
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FAP
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Cancer
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SB03178 is a fibroblast activation protein-alpha (FAP) inhibitor. SB03178 can be conjugated with DOTA and can be used for cancer research .
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- HY-47979
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FAP
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Others
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FAP-IN-2 is a derivative of 99mTc-labeled isonitrile-containing fibroblast activation protein (FAPI) inhibitor, that can be used for tumor imaging .
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-
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- HY-161074
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FAP
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Cancer
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PNT6555 is a fibroblast activation protein-α (FAP) inhibitor. PNT6555 has antitumor activity. PNT6555 can be used for imaging of FAP-positive tumors .
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- HY-160426
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Glucosidase
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Neurological Disease
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Gcase activator 3 (compound 9Q) is a glucosidase (Glucosidase, GCase) activator that can partially stabilize GCase and increase its activity. Gcase activator 3 reduces mutant GCase protein misfolding and degradation in fibroblasts and dopaminergic midbrain neurons. Gcase activator 3 can be used in the study of Parkinson's disease (PD) and related synucleinopathies .
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- HY-100684
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Others
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Cancer
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SP-13786 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM; also inhibits prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM.
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- HY-P99269
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BIBH 1; Anti-Human FAP Recombinant Antibody
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FAP
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Cancer
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Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC) .
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- HY-P10131
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FAP
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Cancer
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3BP-3940 is a highly potent fibroblast activation protein (FAP)-targeting peptide for theranostics. 3BP-3940 is often coupled with radionuclides for tumor diagnosis and treatment .
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- HY-148127
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Drug-Linker Conjugates for ADC
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Cancer
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TAM558 is a payload molecule used for the synthesis of OMTX705. OMTX705 is a humanized anti-fibroblast-activating protein (FAP) antibody conjugated to the cytolysin TAM470 (HY-148128), with antitumor activity .
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- HY-136641
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FAP
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Cancer
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NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI can be used as a probe for FAP-targeted tumour imaging. NOTA-FAPI has good tumour detection efficacy and excellent imaging quality .
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- HY-110367A
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Src
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Others
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LCB 03-0110, a thienopyridine derivative, is a potent pan-discoidin domain receptor/c-Src family tyrosine kinase inhibitor. LCB 03-0110 suppresses scar formation by inhibiting fibroblast and macrophage activation .
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- HY-W404002
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Prolyl Endopeptidase (PREP)
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Metabolic Disease
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BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2
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- HY-N1419
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Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway .
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- HY-148859
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-
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- HY-P99010
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FGFR
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Cancer
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Bemarituzumab is a first-in-class, humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has the potential for cancer research .
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- HY-151955
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TGF-β Receptor
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Inflammation/Immunology
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TGFβ1-IN-3 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-3 can be used for idiopathic pulmonary fibrosis (IPF) research .
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- HY-151954
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TGF-β Receptor
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Inflammation/Immunology
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TGFβ1-IN-2 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-2 can be used for idiopathic pulmonary fibrosis (IPF) research .
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- HY-116084
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- HY-108915
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- HY-145358
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PI3K
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Cancer
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FAP-PI3KI1 is a fibroblast-activated protein (FAP)-targeted PI3K inhibitor that selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells and effectively inhibits collagen synthesis and reduces collagen deposition .
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- HY-B0636
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Glucocorticoid Receptor
FGFR
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Inflammation/Immunology
Endocrinology
Cancer
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Triamcinolone acetonide inhibits basic fibroblast growth factor (bFGF) induced proliferation of retinal endothelial cells. Triamcinolone acetonide reduces chondrocyte viability and leads to cartilage destruction. Triamcinolone acetonide activates macrophage with anti-inflammatory characteristics. Triamcinolone acetonide can be used in the study of diseases such as atopic dermatitis .
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- HY-D2281
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FAP
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Cancer
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[99m Tc]Tc-6-1, a 99mTc-labeled FAPI-46 derivative, is a specific fibroblast activation protein (FAP)-targeted radiotracer. [99m Tc]Tc-6-1 exhibits good tumor uptake and acts as a promising molecular tracer for FAP tumor imaging .
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- HY-116084S
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- HY-124514
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Ras
ERK
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Cancer
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UC-857993 is a selective SOS1-Ras inhibitor (Kd=14.7 μM, His6-SOS1cat), suppressing catalytic activity. UC-857993 also inhibits ERK and Ras activation, suppresses the growth of mouse embryonic fibroblasts (MEFs) .
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- HY-116084S1
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- HY-400687
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Others
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Cancer
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TAM558 intermediate-1 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
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- HY-400688
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Others
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Cancer
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TAM558 intermediate-24 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
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- HY-400689
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Others
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Cancer
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TAM558 intermediate-34 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
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- HY-400690
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Others
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Cancer
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TAM558 intermediate-4 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
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- HY-48564
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ADC Cytotoxin
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Cancer
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TAM558 intermediate-54 is an intermediate in the synthesis of TAM558 (HY-148127).TAM558 is the payload molecule used in the synthesis of OMTX705.OMTX705 is a humanized anti-fibroblast activation protein (FAP) antibody that binds to the cytolysin TAM470 (HY-148128) and has anti-tumor activity .
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- HY-142694
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E1/E2/E3 Enzyme
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Cardiovascular Disease
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DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation .
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- HY-156618
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ABSK011
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FGFR
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Cancer
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Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .
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- HY-13233A
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Val-boroPro mesylate; PT100 mesylate
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Dipeptidyl Peptidase
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Inflammation/Immunology
Cancer
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Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities .
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- HY-13233
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Val-boroPro; PT100
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Dipeptidyl Peptidase
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Inflammation/Immunology
Cancer
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Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities .
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- HY-B1121
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- HY-B1121A
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- HY-108933
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VEGFR
FGFR
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Cancer
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JK-P3 is a potent and pan VEGFR2 inhibitor, with IC50s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well as fibroblast growth factor receptor kinase activity in vitro. JK-P3 has anti-angiogenic activity .
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- HY-151483
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Histone Demethylase
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Cardiovascular Disease
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TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease .
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- HY-N2038
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Phosphodiesterase (PDE)
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Neurological Disease
Cancer
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3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma .
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HY-L088
-
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1984 compounds
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Angiogenesis is the physiological process through which new blood vessels are formed from pre-existing vessels. It occurs in various physiological processes e.g. embryonic development, menstrual cycle, exercise and wound healing etc. Angiogenesis is regulated by both endogenous activators and inhibitors. Some key activators of angiogenesis include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), angiogenin, TGF-β, etc. whereas angiogenesis inhibitors are angiostatin, endostatin, interferon, platelet factor 4, etc. The loss of balance between these opposing signals leads to life threatening diseases like cancer, cardiovascular and ischemic diseases etc. which are thus controlled by exogenous angiogenesis activators (for cardiovascular/ischemic disorders) and inhibitors (for cancer).
MCE offers a unique collection of 1984 compounds with validated angiogenesis targets modulating properties. MCE angiogenesis-related compound library is an effective tool for angiogenesis research and discovery of angiogenesis-related drugs.
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HY-L038
-
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1436 compounds
|
Stem cells, which are found in all multi-cellular organisms, can divide and differentiate into diverse special cell types and can self-renew to produce more stem cells. To be useful in therapy, stem cells must be converted into desired cell types as necessary which is called induced differentiation or directed differentiation. Understanding and using signaling pathways for differentiation is an important method in successful regenerative medicine. Small molecules or growth factors induce the conversion of stem cells into appropriate progenitor cells, which will later give rise to the desired cell type. There is a variety of signal molecules and molecular families that may affect the establishment of germ layers in vivo, such as fibroblast growth factors (FGFs); the wnt family or superfamily of transforming growth factors β (TGFβ) and bone morphogenetic proteins (BMP). Unfortunately, for now, a high cost of recombinant factors is likely to limit their use on a larger scale in medicine. The more promising technique focuses on the use of small molecules. These small molecules can be used for either activating or deactivating specific signaling pathways. They enhance reprogramming efficiency by creating cells that are compatible with the desired type of tissue. It is a cheaper and non-immunogenic method.
MCE Differentiation Inducing Compound Library contains a unique collection of 1436 compounds that act on signaling pathways for differentiation. These compounds are potential stimulators for induced differentiation. This library is a useful tool for researching directed differentiation and regenerative medicine.
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Cat. No. |
Product Name |
Type |
-
- HY-D2281
-
|
Dyes
|
[99m Tc]Tc-6-1, a 99mTc-labeled FAPI-46 derivative, is a specific fibroblast activation protein (FAP)-targeted radiotracer. [99m Tc]Tc-6-1 exhibits good tumor uptake and acts as a promising molecular tracer for FAP tumor imaging .
|
Cat. No. |
Product Name |
Type |
-
- HY-148859
-
|
Drug Delivery
|
AA-T3A-C12 is an anisamide ligand-tethered lipidoid (AA-lipidoid). AA-T3A-C12 mediates great RNA delivery and transfection of activated fibroblasts .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P4448
-
|
Peptides
|
Others
|
Ac-Gly-Pro-AFC is a fluorogenic substrate for the determination of fibroblast activation protein (FAP) endopeptidase activity .
|
-
- HY-P10131
-
|
FAP
|
Cancer
|
3BP-3940 is a highly potent fibroblast activation protein (FAP)-targeting peptide for theranostics. 3BP-3940 is often coupled with radionuclides for tumor diagnosis and treatment .
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- HY-P5452
-
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Peptides
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Others
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PKCd (8-17) is a biological active peptide. (This peptide is derived from the V1 domain of protein kinase C (PKC)d. It inhibits phorbol 12-myristate 13-acetate (PMA)-induced PKCd translocation and activation. Inhibition of PKCd reduces ischemia damage in cardiac and cerebral cells, induces proliferation of fibroblasts, and inhibits graft coronary artery disease in mice.)
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99902
-
FAP-IL2v
|
Interleukin Related
|
Cancer
|
Simlukafusp alfa (FAP-IL2v) is an immunocytokine comprising an antibody against fibroblast activation protein α (FAPα) and an IL-2 variant that only binds IL-2Rβγ. Isotype: human IgG1 .
|
-
- HY-P99269
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BIBH 1; Anti-Human FAP Recombinant Antibody
|
FAP
|
Cancer
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Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC) .
|
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- HY-P99010
-
|
FGFR
|
Cancer
|
Bemarituzumab is a first-in-class, humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has the potential for cancer research .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-116084
-
-
-
- HY-108915
-
-
-
- HY-N2038
-
|
Structural Classification
Flavonols
Flavonoids
Rutaceae
Plants
Citrus reticulata Blanco
|
Phosphodiesterase (PDE)
|
3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-116084S
-
|
Trimethylamine N-oxide-d9 is the deuterium labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway[1][2][3].
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- HY-116084S1
-
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Trimethylamine-N-oxide- 13C3 is the 13C-labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway[1][2][3].
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Cat. No. |
Product Name |
Application |
Reactivity |
-
- HY-P81345
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FAP; Seprase; 170 kDa melanoma membrane-bound gelatinase; fibroblast activation protein alpha; Integral membrane serine protease
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IHC-P
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Human |
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- HY-P81697
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FAP; Seprase; 170 kDa melanoma membrane-bound gelatinase; fibroblast activation protein alpha; Integral membrane serine protease
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FC, ELISA
|
Human |
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