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Saxagliptin hydrate

Saxagliptin hydrate Structure
CAS No.
945667-22-1
Chemical Name:
Saxagliptin hydrate
Synonyms
CS-1180;Onglyza hydrate;BMS477118 hydrate;BMS-477118 hydrate;BMS 477118 hydrate;Saxagliptin hydrate;Shagliptin monohydrate;Saxagliptin hydrate Unii-9gb927lajw;Saxagliptin hydrate (BMS-477118 hydrate);BMS-477118 HYDRATE;BMS 477118 HYDRATE;BMS477118 HYDRATE
CBNumber:
CB92542796
Molecular Formula:
C18H27N3O3
Molecular Weight:
333.43
MOL File:
945667-22-1.mol
MSDS File:
SDS
Modify Date:
2023/5/18 11:31:08
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Saxagliptin hydrate Properties

Melting point 106-108°C
storage temp. -20°C Freezer
solubility DMSO (Slightly), Methanol (Sparingly)
form Solid
color White to Off-White

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338

Saxagliptin hydrate Chemical Properties,Uses,Production

Description

While liraglutide targets the incretin system as a GLP-1 analog for therapeutic intervention in T2DM, saxagliptin enhances GLP-1 plasma concentrations by inhibiting the DPP-4 enzyme responsible for degradation of GLP-1 by cleavage of the two N-terminal amino acids adjacent to alanine (or proline), thereby rendering the hormone inactive. Similarto vildagliptin, saxagliptin is a cyanopyrrolidine substrate-based inhibitor. The proline mimetic occupies the small S1-pocket while the nitrile’s trajectory aligns with the scissile bond of the substrate. The slow dissociation kinetics of saxagliptin is attributed to a reversible, covalent reaction between the nitrile and the catalytically active serine hydroxyl (Ser630). The steric bulk provided by the adamantyl moiety and the constrained cyclopropyl ring stabilizes the trans-rotamer of the amide, thereby preventing the problematic intramolecular cyclization, via the amino group attacking the nitrile, which is favored in the cis-conformation.
Since metabolism of saxagliptin is primarily mediated by CYP3A4/5, there is a potential for drug interactions with concomitant administration of strong inducers or inhibitors of these cytochrome P450 enzymes. The most common adverse events (>5% of patients) included upper respiratory tract infection, urinary tract infection, and headache.

Uses

Saxagliptin Hydrate is a selective and reversible dipeptidyl peptidase-4 (DPP4) inhibitor that may be used to develop treatment for type 2 diabetes.

Definition

ChEBI: Saxagliptin hydrate is a hydrate that is the monohydrate form of anhydrous saxagliptin. Used for the treatment of Type II diabetes. It has a role as a hypoglycemic agent and an EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor. It contains a saxagliptin.

Biological Activity

Saxagliptin (BMS-477118) is an orally active, highly potent and long-acting dipeptidyl peptidase IV inhibitor (human DPP-IV Ki = 0.9 nM; plasma DDP-IV inhibition = 87% 0.5-4h post 4 μmol/kg po. in normal rats) with therapeutic efficacy against type 2 diabetes in vivo (plasma glucose clearance = 28/43/61% post 0.3/1.0/3.0 μmol/kg po. in Zucker fa/fa rats).

Solubility in organics

Saxagliptin hydrochloride is supplied as a crystalline solid. A stock solution may be made by dissolving the saxagliptin (hydrochloride)in the solvent of choice,which should be purged with an inert gas. Saxagliptin hydrochloride is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of saxagliptin hydrochloride in these solvents is approximately 10 mg/ml in ethanol and 20 mg/ml in DMSO and DMF. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of saxagliptin(hydrochloride)can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of saxagliptin (hydrochloride)in PBS(pH 7.2), is approximately 2 mg/ml. We do not recommend storing the aqueous solution for more than one day.

Saxagliptin hydrate Preparation Products And Raw materials

Raw materials

Preparation Products

Saxagliptin hydrate Suppliers

Global( 179)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Morepen Laboratories Ltd +91-7017029282 +91-9818305894 Haryana, India 34 58 Inquiry
Aurobindo Pharma Limited +914066725000 Telangana, India 112 58 Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Pharmaffiliates Analytics and Synthetics P. Ltd +91-172-5066494 Haryana, India 6773 58 Inquiry
SynZeal Research Pvt Ltd +1 226-802-2078 Gujarat, India 6522 58 Inquiry
Henan Tianfu Chemical Co.,Ltd. +86-0371-55170693 +86-19937530512 China 21669 55 Inquiry
Shanghai Time Chemicals CO., Ltd. +86-021-57951555 +8617317452075 China 1807 55 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32760 60 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29897 58 Inquiry
Supplier Advantage
Morepen Laboratories Ltd 58
Aurobindo Pharma Limited 58
A.J Chemicals 58
CLEARSYNTH LABS LTD. 58
Pharmaffiliates Analytics and Synthetics P. Ltd 58
SynZeal Research Pvt Ltd 58
Henan Tianfu Chemical Co.,Ltd. 55
Shanghai Time Chemicals CO., Ltd. 55
ATK CHEMICAL COMPANY LIMITED 60
career henan chemical co 58

Saxagliptin hydrate Spectrum

Saxagliptin hydrate(945667-22-1)1HNMR

945667-22-1(Saxagliptin hydrate)Related Search:

Saxagliptin 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-aMino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1R,3R,5R)- (1R, 3R, 5R, 2R)-Saxagliptin (1S, 3R, 5R, 2'S)-Saxagliptin (1R, 3S, 5S, 2'S)-Saxagliptin
2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2R)-2-aMino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3S,5S)- 1H-Pyrrole-1-carboxylic acid, 2-(aMinocarbonyl)-2,3-dihydro-, 1,1-diMethylethyl ester, (2S)- (S) - N- Boc- adamantylglycine (S)-1-Boc-2,3-dihydro-2-pyrrolecarboxylic acid ethyl ester 2-Azabicyclo[3.1.0]hexane-2,3-dicarboxylic acid, 2-(1,1-dimethylethyl) 3-ethyl ester, (1S,3S,5S)-
N-Boc-L-trans-4,5-Methanoproline (2R)-1,2-Pyrrolidinedicarboxylic acid 1-tert-butyl 2-ethyl ester (1S,3S,5S)-2-(TERT-BUTOXYCARBONYL)-2-AZABICYCLO[3.1.0]HEXANE-3-CARBOXYLIC ACID DSLXQSYLYSTVKT-ONZQNKQFSA-N 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2R)-2-aMino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3R,5S)-
AcetaMide, N-[(1S)-2-[(1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hex-2-yl]-1-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)-2-oxoethyl]-2,2,2-trifluoro- [15N,2H2]-Saxagliptin Hydrochloride Saxagliptin hydrochloride
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2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, hydrate (1:1), (1S,3S,5S)- Saxagliptin hydrate Saxagliptin hydrate Unii-9gb927lajw (1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate Saxagliptin hydrate (1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate CS-1180 BMS 477118 hydrate BMS477118 hydrate BMS-477118 hydrate BMS-477118 HYDRATE;BMS 477118 HYDRATE;BMS477118 HYDRATE Saxagliptin hydrate (BMS-477118 hydrate) Onglyza hydrate (1S,3S,5S)-2-((2S)-2-amino-2-(3-hydroxyadamantan-1-yl)acetyl)-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile Saxagliptin MonohydrateQ: What is Saxagliptin Monohydrate Q: What is the CAS Number of Saxagliptin Monohydrate Q: What is the storage condition of Saxagliptin Monohydrate Q: What are the applications of Saxagliptin Monohydrate (1S,3S,5S)-2-((2S)-2-Amino-2-(3-hydroxyadamantan-1-yl)acetyl)-2-azabicyclo[3.1.0]hexane-3-carbonitrile monohydrate 4-trifluorosulfoyl-3'-trifluoroacetamino-4-demethyldaunorubicin Shagliptin monohydrate 945667-22-1 C18H25N3O2H2O Saxagliptin hydrate API