Cellagen Technology LLC
 
작성일 : 16-07-26
[Cellagen Technology LLC] Disease Area, Cardiovascular & Metabolic II
BMS-477118 (Saxagliptin) l DPP-IV & BMS-512148 (Dapagliflozin) l SGLT2 & CI-1011 (Avasimibe) l ACAT inhibitor / CDDO (Bardoxolone) l anti-inflammatory

 

Disease Area, Cardiovascular & Metabolic II

 

 

Product Name: BMS-477118 (Saxagliptin) | DPP-IV inhibitor

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Saxagliptin is an orally-available, adamantyl-based, reversible inhibitor of DPP-IV for the treatment of Type 2

diabetes with an IC50 of 26 nM and Ki of 0.6-1.3 nM [1, 2]. Saxagliptin is more selective than other approved

DPP-IV inhibitors (vildagliptin, sitagliptin) and is 400-fold and 75-fold selective over DPP-VIII and DPP-IX,

respectively. Once-daily administration of saxagliptin either as a monotherapy or in combination results in a

significant reductions in fasting and postprandial plasma glucose and HbA1c.

Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, improving b-cell

function and suppression of glucagon secretion.

 

Details

Chemical Formula:

 

C18H25N3O2

CAS No.:

 

361442-04-8

Molecular Weight:

 

315.41

Purity:

 

> 98%

Appearance:

 

White

Chemical Name:

 

 

(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl) acetyl]-2-azabicyclo

[3.1.0]hexane-3-carbonitrile

Solubility:

 

Up to 22 mM in DMSO

Synonyms:

 

BMS-477118, BMS 477118, BMS477118, Saxagliptin, Onglyza

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

Reference:

1. Tahrani et al., Saxagliptin: a new DPP-4 inhibitor for the treatment of type 2 diabetes mellitus. Adv. Ther.

   2009, 26(3), 249-262.

2. Deacon et al., Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Adv.

   Ther. 2009, 26(5), 488-499.

  

 

Product Name: BMS-512148 (Dapagliflozin) | SGLT2 inhibitor

 

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Dapagliflozin (BMS-512148) is an orally-available C-aryl glucoside diphenylmethanol inhibitor of SGLT2 (IC50

1.1 nM) for the treatment of Type 1 and Type 2 diabetes. It is the first approved SGLT2 inhibitor (European

Union as Forxiga) for the treatment of diabetes. Its excellent selectivity over SGLT1 (IC50 1390 nM) ensures

that it does not interfere with intestinal glucose absorption. Dapagliflozin minimally inhibits glucose

transporters GLUT1 and GLUT2 and modestly inhibits GLUT4.

Dapagliflozin removes excess glucose and its associated calories in urine, which in turn reduces blood

sugar levels. Clinical studies have shown concurrent reductions in weight and blood pressure. In

combination with metformin, the weight loss was statistically significant, dose-dependent, and persisted for

over two years.

 

Details

Chemical Formula:

 

C21H25ClO6

CAS No.:

 

461432-26-8

Molecular Weight:

 

408.87

Purity:

 

> 98%

Appearance:

 

White

Chemical Name:

 

 

(2S,3R,4R,5S,6R)-2-(3-(4-ethoxybenzyl)-4-chlorophenyl)-6-(hydroxymethyl)-

tetrahydro-2H-pyran-3,4,5-triol

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

 

BMS-512148, BMS 512148, BMS512148, Dapagliflozin

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

Reference:

1. Shah et al., Dapagliflozin: a novel sodium-glucose cotransporter type 2 inhibitor for the treatment of type 2

   diabetes mellitus. Pharmacotherapy 2012, 32(1), 80-94.

2. AstraZeneca website: http://www.astrazeneca.com/Media/Press-releases/Article/20121114--forxiga-eu-

   approval-type-2-diabetes

3.Chao et al., Dapagliflozin: an evidence-based review of its potential in the treatment of type-2 diabetes.

   Core Evidence 2012, 7, 21-28.

 

 

Product Name: CDDO (Bardoxolone) | anti-inflammatory

 

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CDDO is a synthetic oleanane triterpenoid. It is 400,000x more potent than natural product oleanolic acid in

inhibiting cellular iNOS production when stimulated by IFN-gamma, TNF-alpha, and IL-1. The mechanism of

action of CDDO remain elusive, despite its broad biological activities, including proliferation inhibition,

apoptosis induction, and oxidative stress and inflammation suppression.

CCDDO-methyl ester,an orally-available form of CDDO, is undergoing clinical development for the treatment

of advanced chronic kidney disease (CKD) in type 2 diabetes mellitus patients.

 

Details

Chemical Formula:

 

C31H41NO4

CAS No.:

 

218600-44-3

Molecular Weight:

 

491.66

Purity:

 

> 98%

Appearance:

 

Brown

Chemical Name:

 

2-cyano-3,12-dioxo-oleana-1,9(11)-dien-28-oic acid

Solubility:

 

Up to 10 mM in DMSO

Synonyms:

 

CDDO, RTA-401, RTA401, Bardoxolone

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

Reference:

1. Sporn MB, et al. New synthetic triterpenoids: potent agents for prevention and treatment of tissue injury

   caused by inflammatory and oxidative stress. J Nat Prod. 2011; 74(3):537-45.

2. Suh N, et al. A novel synthetic oleanane triterpenoid, 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid, with

   potent differentiating, antiproliferative, and anti-inflammatory activity. Cancer Res. 1999; 59(2):336-41.

 

 

Product Name: CI-1011 (Avasimibe) | ACAT inhibitor

 

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CI-1011 (Avasimibe) is an orally-available acylsulfamic acid inhibitor of Acyl Coenzyme A cholesterol

acyltransferase (ACAT), an enzyme that catalyzes the esterification of cholesterol. inhibition of ACAT by CI-

1011 presumably operates by modulating apoB synthesis and secretion, thereby lowering plasma

concentration of apoB-containing lipoproteins. [3] CI-1011 inhibits ACAT at 3.3 uM, though it has been shown

to be more potent dependent on microsome concentration. [1] CI-1011 also inhibits CYP450 enzymes 2C9,

1A2, and 2C19 at 2.9 uM, 13.9 uM, and 26.5 uM, respectively. [2] CI-1011 has been shown to be a PXR

activator and has CYP3A4 induction profile approximately 10 fold more potent than rifampin.

CI-1011 reduces plasma triglyceride levels in chow-fed rats, cholesterol-fed rats, sucrose-fed rats, and

hamsters. [1] In addition to inhibiting lipid accumulation in macrophages, and thus reducing atherosclerotic

lesion occurrence, CI-1011 also has plaque-stabilizing properties by inhibiting MMP expression and activity.

 

Details

Chemical Formula:

 

C29H43NO4S

CAS No.:

 

165518-60-1

Molecular Weight:

 

501.72

Purity:

 

> 98%

Appearance:

 

White

Chemical Name:

 

2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

 

CI-1011, CI1011, Avasimibe, PD-148515, PD148515

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

Reference:

1. Llaverias et al., Pharmacology of the ACAT inhibitor avasimibe (CI-1011). Cardiovascular Drug Rev.

   2006, 21(1), 33-50.

2. Sahi et al., Effects of avasimibe on cytochrome P450 2C9 expression in vitro and in vivo. Drug Metabolism

   and Disposition, 2004, 32(12), 1370-1376.

3. Burnett et al., Inhibition of ACAT by avasimibe decreases both VLDL and LDL apolipoprotein B production

   in miniature pigs. J. Lipid Res. 1999, 40, 1317-1327.

 

 

Ordering informations

Catalog No.

Product Name

Size

C2477-5

BMS-477118 (Saxagliptin) l DPP-IV inhibitor

5 mg, 25 mg & 100 mg

C2512-5

BMS-512148 (Dapagliflozin) l SGLT2 inhibitor

5 mg, 25 mg & 100 mg

C2336-5

CDDO (Bardoxolone) l anti-inflammatory

5 mg, 25 mg & 100 mg

C2410-10

CI-1011 (Avasimibe) l ACAT inhibitor

10 mg, 50 mg & 250 mg

 

 

 

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