Products

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.

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 4^oC desiccated, or store DMSO solution

at -20^oC.

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).

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.

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 4^oC desiccated, or store DMSO solution

at -20^oC.

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.

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.

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 4^oC desiccated, or store DMSO solution

at -20^oC.

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  

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.

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 4^oC desiccated, or store DMSO solution

at -20^oC.

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.