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K4264
KR-62436 hydrate
≥95%, powder
Synonym(e):
6-{2-[(5-Cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile dihydrochloride hydrate
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Empirische Formel (Hill-System):
C14H15N7O·2HCl · xH2O
CAS-Nummer:
Molekulargewicht:
370.24 (anhydrous basis)
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
Assay:
≥95%
Form:
powder
assay
≥95%
form
powder
color
white to beige
solubility
H2O: 5 mg/mL, clear
storage temp.
2-8°C
SMILES string
O.Cl.Cl.O=C(CNCCNc1ccc(cn1)C#N)N2N=CCC2C#N
InChI
1S/C14H15N7O.2ClH.H2O/c15-7-11-1-2-13(19-9-11)18-6-5-17-10-14(22)21-12(8-16)3-4-20-21;;;/h1-2,4,9,12,17H,3,5-6,10H2,(H,18,19);2*1H;1H2
InChI key
FQZOFSJMRKZMSV-UHFFFAOYSA-N
Biochem/physiol Actions
KR-62436 is a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV). DPP-IV is a serine protease which inactivates glucagon-like peptide (GLP-1); IC50 0.1-0.8 μM; GLP-1 is a potent stimulus for insulin secretion and inducer of satiety after food intake, but it has a very short action (1 min) because it is rapidly degraded by DPP-IV; blocking DPP-IV increases GLP-1 action and increases plasma insulin levels; DPP-IV inhibitors and KR-62436 have clinical potential as anti-diabetic agents
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Lagerklasse
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
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Kwang-Rok Kim et al.
European journal of pharmacology, 518(1), 63-70 (2005-08-18)
Dipeptidyl peptidase-IV (DPP-IV) is involved in the inactivation of glucagon-like peptide-1 (GLP-1), a potent insulinotropic peptide. Thus, DPP-IV inhibition can be an effective approach to treat type 2 diabetes mellitus by potentiating insulin secretion. This study describes the biological effects
Emi Kawakita et al.
Molecular cancer research : MCR, 19(1), 61-73 (2020-10-01)
The biological influence of antidiabetic drugs on cancer cells and diabetic cancer patients has not yet been completely elucidated. We reported that a dipeptidyl peptidase (DPP)-4 inhibitor accelerates mammary cancer metastasis by inducing epithelial-mesenchymal transition (EMT) through the CXCL12/CXCR4/mTOR axis.
Fan Yang et al.
Cancer research, 79(4), 735-746 (2018-12-26)
Dipeptidyl peptidase (DPP)-4 is a multifunctional glycoprotein involved in various biological and pathologic processes. DPP-4 has been widely recognized as a therapeutic target for type 2 diabetes mellitus but is also implicated in the development of human malignancies. Here, we