Dutogliptin - CAS 852329-66-9
Catalog number:
852329-66-9
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C10-H20-B-N3-O3
Molecular Weight:
241.10
COA:
Inquire
Targets:
DPP4
Description:
Dutogliptin is a selective and orally active DPP4 inhibitor. It can improve glycaemic control in patients with type 2 diabetes. But phase III clinical trials for the treatment of type 2 diabetes were discontinued.
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Purity:
98%
Appearance:
Powder
Synonyms:
PHX 1149; (2R)-1-(((3R)-Pyrrolidin-3-ylamino)acetyl)pyrrolidin-2-yl)boronic acid;890402-81-0 (tartrate salt);
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Type 2 diabetes mellitus
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
DVJAMEIQRSHVKC-BDAKNGLRSA-N
InChI:
1S/C10H20BN3O3/c15-10(7-13-8-3-4-12-6-8)14-5-1-2-9(14)11(16)17/h8-9,12-13,16-17H,1-7H2/t8-,9+/m1/s1
Canonical SMILES:
B(C1CCCN1C(=O)CNC2CCNC2)(O)O
Current Developer:
Originator Phenomix Corporation
1.Population pharmacokinetic analysis of dutogliptin, a selective dipeptidyl peptidase-4 inhibitor.
Marier JF1, Mouksassi MS1, Gosselin NH1, Li J2,3. Clin Pharmacol Drug Dev. 2014 Jul;3(4):297-304. doi: 10.1002/cpdd.87. Epub 2014 Feb 10.
Dutogliptin is a selective dipeptidyl peptidase-4 inhibitor shown to be efficacious and safe in patients with type 2 diabetes mellitus (T2DM). Population pharmacokinetic (PK) analysis of dutogliptin was performed based on data collected in 561 healthy subjects and patients with T2DM enrolled in Phase I and II studies to assess sources of variability and support dosing rationale. The effect of extrinsic (formulations, fed/fasting conditions, potential drug-drug interaction with metformin) and intrinsic (baseline characteristics, markers of renal function, renal impairment category, and disease status) covariates was evaluated using non-linear mixed effect modeling. Plasma concentrations of dutogliptin were best fitted with a two-compartment model with a first-order rate constant of absorption (Ka) and a lag time. No differences were observed between healthy subjects and patients with T2DM. Apparent clearance (CL/F) and terminal elimination half-life of dutogliptin were 176 L/h and 12.
2.Evaluation of the potential for pharmacokinetic and pharmacodynamic interactions between dutogliptin, a novel DPP4 inhibitor, and metformin, in type 2 diabetic patients.
Li J1, Klemm K, O'Farrell AM, Guler HP, Cherrington JM, Schwartz S, Boyea T. Curr Med Res Opin. 2010 Aug;26(8):2003-10. doi: 10.1185/03007995.2010.491266.
OBJECTIVE: Dutogliptin is a novel, orally available, potent, and selective DPP4 inhibitor that improves glycemic control in type 2 diabetic patients. The objective of this study was to evaluate the potential pharmacokinetic and pharmacodynamic interactions, as well as the tolerability, of dutogliptin and metformin alone and in combination in type 2 diabetic patients.
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CAS 852329-66-9 Dutogliptin

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