ChemicalBook > CAS DataBase List > Saxagliptin hydrate

Saxagliptin hydrate

Product Name
Saxagliptin hydrate
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
Formula Weight
333.43
MOL File
945667-22-1.mol
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Saxagliptin hydrate Property

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

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

TRC
Product number
S143750
Product name
SaxagliptinHydrate
Packaging
500mg
Price
$525
Updated
2021/12/16
Ark Pharm
Product number
P000018464
Product name
Saxagliptin hydrate
Purity
99+%
Packaging
5mg
Price
$80
Updated
2021/12/16
Biosynth Carbosynth
Product number
FS44431
Product name
Saxagliptin monohydrate
Packaging
10mg
Price
$95
Updated
2021/12/16
Ark Pharm
Product number
P000018464
Product name
Saxagliptin hydrate
Purity
99+%
Packaging
10mg
Price
$115
Updated
2021/12/16
Ark Pharm
Product number
P000018464
Product name
Saxagliptin hydrate
Purity
99+%
Packaging
25mg
Price
$205
Updated
2021/12/16
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Saxagliptin hydrate Chemical Properties,Usage,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.

Originator

Bristol-Myers-Squibb (US)

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.

brand name

Onglyza

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

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View Lastest Price from Saxagliptin hydrate manufacturers

Henan Aochuang Chemical Co.,Ltd.
Product
Saxagliptin hydrate 945667-22-1
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1Ton
Release date
2022-09-22
Zhuozhou Wenxi import and Export Co., Ltd
Product
Saxagliptin hydrate 945667-22-1
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Saxagliptin hydrate 945667-22-1
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-08

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