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ChemicalBook--->CAS DataBase List--->865759-25-7

865759-25-7

865759-25-7 Structure

865759-25-7 Structure
IdentificationBack Directory
[Name]

Trelagliptin
[CAS]

865759-25-7
[Synonyms]

YR-472
CS-926
Zafatek)
Trilagliptin
Trelagliplin
Trelagliptin
Glass acid trigram
Trelagliptin, >=98%
SYR472 Trelagliptin
Trelagliptin(syr472)
Trelagliptin free base
Trelagliptin impurity G
Trelagliptin Impurity 83
SYR-472; SYR472; SYR 472
Trelagliptin Isomer Impurity
TRELAGLIPTIN CAS 865759-25-7
Trelagliptin/Trelagliptin succinate
(R)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2
4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile(Trelagliptin)
1-(2-broMo-5-fluorobenzyl)-6-chloro-3-MethylpriMidine-2,4(1H, 3H)-dione
2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile
(S)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile
(R)-2-[[6-(3-AMinopiperidin-1-yl)-3-Methyl-2,4-dioxo-3,4-dihydropyriMidin-1(2H)-yl]Methyl]-4-fluorobenzonitrile
Benzonitrile, 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H) -pyrimidinyl]methyl]-4-fluoro-
(R)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile(Trelagliptin)
Trelagliptin (R)-2-[[6-(3-Aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]methyl]-4-fluorobenzonitrile
TrelagliptinQ: What is Trelagliptin Q: What is the CAS Number of Trelagliptin Q: What is the storage condition of Trelagliptin Q: What are the applications of Trelagliptin
[EINECS(EC#)]

1592732-453-0
[Molecular Formula]

C18H20FN5O2
[MDL Number]

MFCD22572746
[MOL File]

865759-25-7.mol
[Molecular Weight]

357.382
Chemical PropertiesBack Directory
[Boiling point ]

519.0±60.0 °C(Predicted)
[density ]

1.38±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

≥11.6 mg/mL in DMSO; ≥3.68 mg/mL in EtOH with gentle warming and ultrasonic; ≥93.8 mg/mL in H2O
[form ]

solid
[pka]

9.88±0.20(Predicted)
[color ]

White to off-white
[InChI]

InChI=1S/C18H20FN5O2/c1-22-17(25)8-16(23-6-2-3-15(21)11-23)24(18(22)26)10-13-7-14(19)5-4-12(13)9-20/h4-5,7-8,15H,2-3,6,10-11,21H2,1H3/t15-/m1/s1
[InChIKey]

IWYJYHUNXVAVAA-OAHLLOKOSA-N
[SMILES]

C(#N)C1=CC=C(F)C=C1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1
Hazard InformationBack Directory
[Uses]

Trelagliptin is a highly selective, long-acting dipeptidyl peptidase IV (DPP-4) inhibitor. This inhibitor provides sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes.
[Definition]

ChEBI: Trelagliptin is a member of benzenes and a nitrile.
[Biological Activity]

trelagliptin (syr-472) is a selective inhibitor of dpp-4 and is developed for the treatment of type 2 diabetes mellitus (t2dm) [1].dipeptidyl peptidase (dpp)-4 also known as adenosine deaminase complexing protein 2 or cd26 is an antigenic enzyme that expressed on the surface of most cell types and plays an important role in regulating immune system, signal transduction and apoptosis [2, 3].trelagliptin (syr-472) is a potent dpp-4 inhibitor and can be administered once weekly which unlike its other class approved agents that be taken once daily [1]. in japan,
[in vivo]

Trelagliptin (oral gavage; 7 mg/kg; single dose) shows sustained PD effect in dogs and gives >80% inhibition of DPP-4 activity even after 24h[1].Trelagliptin (oral gavage; 3 mg/kg; single dose; 60 min prior to oral glucose) significantly improves the glucose tolerance capacity by decreasing the AUC0?120min of 19.3% compared with the vehicle group in ob/ob mice[3]. Trelagliptin (oral gavage; 10 mg/kg; once a week; 8 weeks) caused significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 16.8% compared to the control.It also increases insulin level and raised it by 1.7-fold in AUC0?120min in ob/ob mice[3].

Animal Model:ICR ob/ob mice[3]
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg; once a week; 8 weeks
Result:Exerted chronic antidiabetic effects on type 2 diabetic db/db Mice.
[target]

DPP-4
[IC 50]

DPP-4
[References]

[1]. mckeage, k., trelagliptin: first global approval. drugs, 2015. 75(10): p. 1161-4.
[2]. inagaki, n., et al., once-weekly trelagliptin versus daily alogliptin in japanese patients with type 2 diabetes: a randomised, double-blind, phase 3, non-inferiority study. lancet diabetes endocrinol, 2015. 3(3): p. 191-7.
[3]. inagaki, n., et al., syr-472, a novel once-weekly dipeptidyl peptidase-4 (dpp-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. lancet diabetes endocrinol, 2014. 2(2): p. 125-32.
Spectrum DetailBack Directory
[Spectrum Detail]

Trelagliptin(865759-25-7)1HNMR
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