Cellagen Technology LLC
 
작성일 : 16-07-26
[Cellagen Technology LLC] Disease Area, Cardiovascular & Metabolic I
A769662 l AMPK & AlCAR l AMPK activator / Aliskiren l direct renin & BI-1356 (Linagliptin) l DPP-IV/DPP-4 inhibitor

 

Disease Area, Cardiovascular & Metabolic I

 

 

Product Name: A769662 l AMPK activator

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A769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator. It activates AMPK through the

β subunit carbohydrate-binding module and the γ subunit but not the AMP-binding sites.

A769662 stimulated partially purified rat liver AMPK with an EC50 of 0.8 µM and inhibited fatty acid synthesis

in primary rat hepatocytes with an IC50 of 3.2 µM. A769662 could be a useful tool compound for both cell

survival and cell proliferation.

 

Details

Chemical Formula:

 

C20H12N2O3S

CAS No.:

 

844499-71-4

Molecular Weight:

 

360.39

Purity:

 

> 98%

Appearance:

 

White solid or off white solid

Chemical Name:

 

 

4-hydroxy-3-(2'-hydroxy-[1,1'-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]

pyridine-5-carbonitrile

Solubility:

 

Up to 50 mM in DMSO

Storage:

 

 

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

at -20oC.

 

Reference:

1. Scott, J.W., et al. Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-

containing complexes. Chem. Biol. 15: 1220-1230 (2008).

2. Cool, B., et al. Identification and characterization of a small molecule AMPK activator that treats key

components of type 2 diabetes and the metabolic syndrome. Cell Metab. 3: 403-416 (2006).

3. Huang, X. et al. Important role of the LKB1-AMPK pathway in suppressing tumorigenesis in PTEN-deficient

mice. Biochem J. 412:211-221 (2008).

  

 

Product Name: AICAR | AMPK activator

 

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AICAR is a natural metabolic intermediate of the purine biosynthetic pathway. In its monophosphate form,

AICAR is a potent AMPK agonist, which at low concentrations, does not affect AMP, ADP, or ATP levels.

AICAR's interacts directly with AMPK, inducing a conformational change that favors phosphorylation of the

catalytic alpha subunit.

AMPK is also implicated in the modulation of enzymes such as glucokinase and glycogen phosphorylase.

Direct binding by AICAR to phosphofructokinase and fructose-1,6-bisphosphatase have been reported.

AICAR's interaction with HSP90 has also been studied and found to have antiproliferative effects in tumor cell

lines such as PC-3, MCF-7, C6 glioma, U87MG, K-562, and CEM.

 

Details

Chemical Formula:

 

C9H14N4O5

CAS No.:

 

2627-69-2

Molecular Weight:

 

258.23

Purity:

 

> 98%

Appearance:

 

White

Chemical Name:

 

 

5-amino-1-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1H-

imidazole-4-carboxamide

Solubility:

 

Up to 22 mM in DMSO

Synonyms:

 

Arasine, AICA-riboside, Protara, AIC-Riboside

Storage:

 

 

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

at -20oC.

 

Reference:

1. Daignan-Fornier et al., 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranosyl 5'-Monophosphate

(AICAR), a Highly Conserved Purine Intermediate with Multiple Effects Metabolites 2012, 2, 292-302.

2.Guo et al., The AMPK agonist AICAR inhibits the growth of EGFRvIII-expressing glioblastomas by inhibiting

lipogenesis. Proc. Natl. Acad. Sci. 2009, 106(31), 12932-12937.

 

 

Product Name: Aliskiren | direct renin inhibitor

 

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Aliskiren is an orally-available, nonpeptide piperidine-based inhibitor renin (IC50 0.6 nM) for the treatment of

hypertension. Despite it's 2.5% bioavailability in humans, the absorbed aliskiren is slowly cleared such that

the drug can accumulate to therapeutic levels within several doses.

Aliskiren is highly selective for the Renin-Angiotensin System (RAS) and therefore does not interfere with

bradykinin metabolism; therefore side effects often associated with ACE inhibitors are not likely to occur with

aliskiren. Aliskiren is effective in reducing blood pressure and is well tolerated, and has shown promising

target organ protection in animal models and clinical trials.

 

Details

Chemical Formula:

 

C30H53N3O6

CAS No.:

 

173334-57-1, 173334-58-2

Molecular Weight:

 

551.76

Purity:

 

> 98%

Appearance:

 

White

Chemical Name:

 

 

(2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-

[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide

Solubility:

 

Up to 22 mM in DMSO

Synonyms:

 

Aliskiren, Rasilez, Tekturna, CGP60536B

Storage:

 

 

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

at -20oC.

 

Reference:

1. Brown, M.J., Aliskiren. Circulation, 2008, 118, 773-784.

2. Allikmets, K., Aliskiren--an orally active renin inhibitor. Review of pharmacology, pharmacodynamics,

kinetics, and clinical potential in the treatment of hypertension.Vasc. Heatlh Risk Mgmt., 2007, 3(6), 809-815.

3. Gradman et al., Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive

efficacy and placebo-like tolerability in hypertensive patients. Circulation 2005, 111, 1012-1018. Pubmed ID:

15723979  

 

 

Product Name: BI-1356 (Linagliptin) | DPP-IV/DPP-4 inhibitor

 

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BI-1356 (Linagliptin) is a highly potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50 = 1 nM) for

treatment of type II diabetes. BI-1356 can increase incretin levels (GLP-1 and GIP), which increases insulin

secretion and inhibits glucagon release, decreases gastric emptying, and decreases blood glucose levels.

BI-1356 shows 10,000-fold more selectivity for DPP-4 against other protease/peptidases, including DPP-8,

DPP-9, trypsin, plasmin, and thrombin.

 

Details

Chemical Formula:

 

C25H28N8O2

CAS No.:

 

668270-12-0

Molecular Weight:

 

472.54

Purity:

 

> 98%

Appearance:

 

White

Chemical Name:

 

 

(R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)

methyl)-1H-purine-2,6(3H,7H)-dione

Solubility:

 

Up to 25 mM in DMSO

Synonyms:

 

BI-1356, BI1356, Linagliptin, Tradjenta, Trajenta

Storage:

 

 

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

at -20oC.

 

Reference:

1. Eckhardt M, et al. 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-

ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally

bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. J Med Chem. 2007; 50(26):6450-3.

2. Thomas L, et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-

ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor,

has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J

Pharmacol Exp Ther. 2008; 325(1):175-82.

 

 

Ordering informations

Catalog No.

Product Name

Size

C2769-5

A769662 l AMPK activator

5 mg, 25 mg & 100 mg

C2422-10

AlCAR l AMPK activator

10 mg, 50 mg & 250 mg

C2547-5

Aliskiren l direct renin inhibitor

5 mg, 25 mg & 100 mg

C2135-5

BI-1356 (Linagliptin) l DPP-IV/DPP-4 inhibitor

5 mg, 25 mg & 100 mg

 

 

 

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