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
100mg
Price
$567
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611536
Product name
Saxagliptin hydrate
Packaging
250mg
Price
$615.4
Updated
2021/12/16
Ark Pharm
Product number
P000018464
Product name
Saxagliptin hydrate
Purity
99+%
Packaging
50mg
Price
$349
Updated
2021/12/16
AK Scientific
Product number
Z6180
Product name
Saxagliptinhydrate
Packaging
50mg
Price
$385
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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Saxagliptin hydrate Suppliers

TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
19892
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58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6393
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
Country
United States
ProdList
19553
Advantage
58
Cato Research Chemicals Inc.
Tel
020-81215950 4000-868-328
Email
customer@uwalab.com
Country
United States
ProdList
10413
Advantage
58
Aladdin Scientific
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
57511
Advantage
58
Protheragen-ING
Tel
+16313385890
Email
info@protheragen-ing.com
Country
United States
ProdList
1091
Advantage
58
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View Lastest Price from Saxagliptin hydrate manufacturers

Hebei Duling International Trade Co. LTD
Product
Saxagliptin hydrate 945667-22-1
Price
US $70.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
20 tons
Release date
2023-03-24
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

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