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Antidiabetic Agents / Related Products
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Items 11 of 11
ALX-270-255 Revised 14-Sep-07
Ciglitazone
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SYNONYMS (±)-5-[4-(1-Methylcyclohexylmethoxy)benzyl]-thiazolidine-2,4-dione
U-63287
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-255-M001   1 mg 30.00 USD Add To Cart
ALX-270-255-M005   5 mg 80.00 USD Add To Cart
ALX-270-255-M025   25 mg 310.00 USD Add To Cart
Product Specification
FORMULA: C18H23NO3S
MW: 333.5
CAS NUMBER: 74772-77-3
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.

Product Description
Selective PPARγ agonist.
Product Specific Literature References
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones: T.M. Willson, et al.; J. Med. Chem. 39, 665 (1996) Abstract; Full Text
Detection and functional characterisation of the transcription factor peroxisome proliferator-activated receptor gamma in lutein cells: B. Löhrke, et al.; J. Endocrinol. 159, 429 (1998) Abstract; Full Text
Peroxisome proliferator-activated receptor gamma ligands are potent inhibitors of angiogenesis in vitro and in vivo: X. Xin, et al.; J. Biol. Chem. 274, 9116 (1999) Abstract; Full Text
Thiazolidinediones--the new insulin enhancers: R.J. Jha; Clin. Exp. Hypertens. 21, 157 (1999), (Review) Abstract
The nuclear receptor PPAR gamma and immunoregulation: PPAR gamma mediates inhibition of helper T cell responses: R.B. Clark, et al.; J. Immunol. 164, 1364 (2000) Abstract; Full Text
Further Categories Containing This Product:
Antidiabetic Agents / Related Products
 
 
ALX-270-355 Revised 14-Sep-07
Troglitazone
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SYNONYMS 5-[[4-[(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)methoxy]phenyl]methyl]-2,4-thiazolidinedione
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-270-355-M001   1 mg 20.00 USD Add To Cart
ALX-270-355-M005   5 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C24H27NO5S
MW: 441.5
CAS NUMBER: 97322-87-7
MERCK INDEX: 14: 9769
RTECS: XJ5813130
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: White to beige solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in 100% ethanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C

Product Description
Potent and selective PPARγ ligand. Binds to the PPARγ ligand-binding domain and recruits ligand-specific transcriptional coactivators at 1µM [1]. In skeletal muscle and adipocyte cell cultures, the EC50 of troglitazone is about 10µM [2].
Product Specific Literature References
[1] Ligand type-specific interactions of peroxisome proliferator-activated receptor gamma with transcriptional coactivators: Y. Kodera, et al.; J. Biol. Chem. 275, 33201 (2000) Abstract; Full Text
[2] Enhancing effect of troglitazone on porcine adipocyte differentiation in primary culture: a comparison with dexamethasone: Y.D. Tchoukalova, et al.; Obes. Res. 8, 664 (2000) Abstract
[3] 15-Deoxy-{delta}12,14-prostaglandin j2 inhibits interleukin-1{beta}-induced nuclear factor-{kappa}b in human amnion and myometrial cells: mechanisms and implications: T.M. Lindström & P.R. Bennett; J. Clin. Endocrinol. Metab. 90, 3534 (2005) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION Troglitazone is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, troglitazone should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. Troglitazone has a solubility of 100µg/ml in a 1:6 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.
General Literature References
[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents: B.C. Cantello, et al.; J. Med. Chem. 37, 3977 (1994) Abstract
An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma): J.M. Lehmann, et al.; J. Biol. Chem. 270, 12953 (1995) Abstract; Full Text
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones: T.M. Willson, et al.; J. Med. Chem. 39, 665 (1996) Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products • Antidiabetic Agents / Related Products
 
 
ALX-270-367 Revised 25-Jul-07
Pioglitazone
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SYNONYMS 5-[[4-[2-(5-Ethyl-2-pyridinyl)ethoxy]phenyl]methyl-2,4-thiazolidinedione
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-270-367-M001   1 mg 48.00 USD Add To Cart
ALX-270-367-M005   5 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C19H20N2O3S
MW: 356.4
CAS NUMBER: 111025-46-8
MERCK INDEX: 14: 7452
PURITY: ≥98% (1H-NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (2.5mg/ml) or dimethyl formamide (2.5mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C

Product Description
Pioglitazone selectively activates PPARγ-1. It is about one tenth as potent as rosiglitazone (EC50~500nM for human and mouse PPARγ). In a transactivation assay using COS-1 cells transfected with full length human PPARα and RXRα, pioglitazone and rosiglitazone exhibit low level activation of PPARα at 1µM and 5.4- and 4.2-fold activation, respectively, at a concentration of 10µM.

Not sold in the US.
Product Specific Literature References
[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents: B.C. Cantello, et al.; J. Med. Chem. 37, 3977 (1994) Abstract
An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma): J.M. Lehmann, et al.; J. Biol. Chem. 270, 12953 (1995) Abstract; Full Text
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones: T.M. Willson, et al.; J. Med. Chem. 39, 665 (1996) Abstract
Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone: J. Sakamoto, et al.; BBRC 278, 704 (2000) Abstract
The PPARs: from orphan receptors to drug discovery: T.M. Willson, et al.; J. Med. Chem. 43, 527 (2000) Abstract
General Information
Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo. Rosiglitazone (Prod. No. ALX-350-103) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands.
Further Categories Containing This Product:
Antidiabetic Agents / Related Products
 
 
ALX-270-432 Revised 23-May-08
Metformin
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SYNONYMS 1,1-Dimethylbiguanide . hydrochloride
PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Antidiabetic Agents / Related Products
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ALX-270-432-G001   1 g 15.00 USD Add To Cart
ALX-270-432-G005   5 g 20.00 USD Add To Cart
Product Specification
FORMULA: C4H11N5 . HCl
MW: 129.2 . 36.5
CAS NUMBER: 1115-70-4
MERCK INDEX: 14: 5938
RTECS: DU1800000
PURITY: ≥97% (Assay)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING: Hygroscopic.
HAZARD: IRRITANT.

Product Description
Antidiabetic agent. Reduces the cardiovascular complications of diabetes. Does not induce hypoglycemia.
Product Specific Literature References
Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). UK Prospective Diabetes Study (UKPDS) Group: Lancet 352, 854 (1998) Abstract
Starting patients with type 2 diabetes on insulin therapy using once-daily injections of biphasic insulin aspart 70/30, biphasic human insulin 70/30, or NPH insulin in combination with metformin: C. Kilo, et al.; J. Diabetes Complications 17, 307 (2003) Abstract
Effects of metformin and thiazolidinediones on suppression of hepatic glucose production and stimulation of glucose uptake in type 2 diabetes: a systematic review: A. Natali and E. Ferrannini; Diabetologia 49, 434 (2006) Abstract
Insulin-lowering agents inhibit synthesis of testosterone in ovaries of DHEA-induced PCOS rats: T. Misugi, et al.; Gynecol. Obstet. Invest. 61, 208 (2006) Abstract
 
 
ALX-340-039 Revised 05-Feb-05
MEDICA 16
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SYNONYMS 3,3,14,14-Tetramethylhexadecanedioic acid
PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Cholesterol & Lipid Transport / Related Products
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ALX-340-039-M005   5 mg 92.00 USD Add To Cart
Product Specification
FORMULA: C20H38O4
MW: 342.5
CAS NUMBER: 87272-20-6
PURITY: ≥98%
APPEARANCE: Crystalline solid.
SOLUBILITY: 100mg/ml soluble in DMSO, dimethyl formamide or 100% ethanol. Slightly soluble in aqueous buffers.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C

Product Description
Hypolipidemic and antidiabetic agent, shown to reduce adiposity. Induces malic enzyme, mitochondrial glycerol-3-phosphate dehydrogenase, and carnitine palmitoyl transferase I. Inhibitor of citrate lyase and acetyl-CoA carboxylase, expected to disinhibit hepatic fatty acid oxidation while up-regulating electron shuttle mechanism, and thus should stimulate reverse electron transport. Exhibits thyromimetic properties with respect to the modulation of rat liver redox and phosphate potentials.
Product Specific Literature References
Inhibition of lipid synthesis by beta beta'-tetramethyl-substituted, C14-C22, alpha, omega-dicarboxylic acids in the rat in vivo: J. Bar-Tana, et al.; J. Biol. Chem. 260, 8404 (1985) Abstract; Full Text
The hypochylomicronemic effect of beta,beta'-methyl-substituted hexadecanedioic acid (MEDICA 16) is mediated by a decrease in apolipoprotein C-III: B. Frenkel, et al.; J. Biol. Chem. 263, 8491 (1988) Abstract; Full Text
Adipose reduction by beta,beta'-tetramethyl-substituted hexadecanedioic acid (MEDICA 16): R. Tzur, et al.; Int. J. Obes. 13, 313 (1989), Review Abstract
Inhibition of rat liver acetyl-CoA carboxylase by beta, beta'-tetramethyl-substituted hexadecanedioic acid (MEDICA 16): G. Rose-Kahn & J. Bar-Tana; Biochim. Biophys. Acta 1042, 259 (1990) Abstract
Hypolipidemic effect of beta, beta'-tetramethyl hexadecanedioic acid (MEDICA 16) in hyperlipidemic JCR:LA-corpulent rats: J.C. Russell, et al.; Arterioscler. Thromb. 11, 602 (1991) Abstract
Tissue selective modulation of redox and phosphate potentials by beta,beta'-methyl-substituted hexadecanedioic acid: B. Kalderon, et al.; Endocrinology 131, 1629 (1992) Abstract
Mode of action of peroxisome proliferators as hypolipidemic drugs. Suppression of apolipoprotein C-III: R. Hertz, et al.; J. Biol. Chem. 270, 13470 (1995) Abstract; Full Text
Sensitization to insulin induced by beta,beta'-methyl-substituted hexadecanedioic acid (MEDICA 16) in obese Zucker rats in vivo: N. Mayorek, et al.; Diabetes 46, 1958 (1997) Abstract
Mitochondria uncoupling by a long chain fatty acyl analogue: O. Hermesh, et al.; J. Biol. Chem. 273, 3937 (1998) Abstract; Full Text
Development of insulin resistance in the JCR:LA-cp rat: role of triacylglycerols and effects of MEDICA 16: J.C. Russell, et al.; Diabetes 47, 770 (1998) Abstract; Full Text
Peroxisome proliferators as adjuvants for the reverse-electron-transport therapy of obesity: an explanation for the large increase in metabolic rate of MEDICA 16-treated rats: M.F. McCarty; Med. Hypotheses 53, 272 (1999) Abstract
Mitochondrial protonophoric activity induced by a thyromimetic fatty acid analogue: O. Hermesh, et al.; Biochim. Biophys. Acta 1457, 166 (2000) Abstract
Fatty acid cycling in the fasting rat: B. Kalderon, et al.; Am. J. Physiol. Endocrinol. Metab. 279, E221 (2000) Abstract; Full Text
MEDICA 16 inhibits hepatic acetyl-CoA carboxylase and reduces plasma triacylglycerol levels in insulin-resistant JCR: LA-cp rats: L.L. Atkinson, et al.; Diabetes 51, 1548 (2002) Abstract
Genotoxicity of streptozotocin: A.D. Bolzan and M.S. Bianchi; Mutat. Res. 512, 121 (2002), (Review) Abstract
Further Categories Containing This Product:
Antidiabetic Agents / Related Products
 
 
ALX-350-094 Revised 24-Jul-08
Berberine . hemisulfate
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SYNONYMS Natural Yellow 18
5,6-Dihydro-9,10-dimethoxybenzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products with Antibiotic Activity
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ALX-350-094-G001   1 g 15.00 USD Add To Cart
Product Specification
FORMULA: C20H18NO4 . 0.5SO4
MW: 336.4 . 48.0
CAS NUMBER: 633-66-9
MERCK INDEX: 14: 1154
RTECS: DR9867000
PURITY: ≥98% (TLC)
APPEARANCE: Off-white to yellow powder.
SOLUBILITY: 50mg/ml soluble in methanol:water 2:1.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: TOXIC.
IDENTITY: Determined by IR: Identical to standard reference.

Product Description
Alkaloid which exhibits relatively weak antibiotic properties, because of its efflux by multidrug resistance pumps. The antimicrobial action of berberine is potentiated by 5’-methoxyhydnocarpin, a multidrug pump inhibitor. Lowers cholesterol levels through a mechanism different from that of statins. Upregulates the expression of liver low-density lipoprotein receptor (LDLR) resulting in improved clearance of plasma LDL cholesterol through receptor mediated endocytosis. Possesses anti-inflammatory, anti-diabetic and anti-angiogenic effects. Induces apoptosis.
Product Specific Literature References
Berberine sulfate: antimicrobial activity, bioassay, and mode of action: A.H. Amin, et al.; Can. J. Microbiol. 15, 1067 (1969) Abstract
Bacteria lacking a multidrug pump: a sensitive tool for drug discovery: P.C. Hsieh, et al.; PNAS 95, 6602 (1998) Abstract; Full Text
Synergy in a medicinal plant: antimicrobial action of berberine potentiated by 5’-methoxyhydnocarpin, a multidrug pump inhibitor: F.R. Stermitz, et al.; PNAS 97, 1433 (2000) Abstract; Full Text
Berberine is a novel cholesterol-lowering drug working through a unique mechanism distinct from statins: W. Kong, et al.; Nat. Med. 10, 1344 (2004) Abstract
The anti-inflammatory potential of berberine in vitro and in vivo: C.L. Kuo, et al.; Cancer Lett. 203, 127 (2004) Abstract
Therapeutic effects of berberine in impaired glucose tolerance rats and its influence on insulin secretion: S.H. Leng, et al.; Acta Pharmacol. Sin. 25, 496 (2004) Abstract
Berberine inhibits HIF-1alpha expression via enhanced proteolysis: S. Lin, et al.; Mol. Pharmacol. 66, 612 (2004) Abstract
Apoptosis of human leukemia HL-60 cells and murine leukemia WEHI-3 cells induced by berberine through the activation of caspase-3: C.C. Lin, et al.; Anticancer Res. 26, 227 (2006) Abstract
Berberine acutely inhibits insulin secretion from beta cells through cAMP signaling pathway: L. Zhou, et al.; Endocrinology (2008) Abstract
Berberine modifies cysteine 179 of IkappaBalpha kinase, suppresses nuclear factor-kappaB-regulated antiapoptotic gene products, and potentiates apoptosis.: M.K. Pandey, et al.; Cancer Res. 68, 5370 (2008) Abstract
Further Categories Containing This Product:
Natural Products - Anti-inflammatory Agents • Natural Products - Chemopreventive Agents • Cholesterol & Lipid Transport / Related Products • Antidiabetic Agents / Related Products • Alkaloids
 
 
ALX-350-103 Revised 18-Sep-06
Rosiglitazone . maleate
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-103-M025   25 mg 68.00 USD Add To Cart
ALX-350-103-M100   100 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C18H19N3O3S . C4H4O4
MW: 357.4 . 116.1
CAS NUMBER: 155141-29-0
MERCK INDEX: 14: 8265
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol or in aqueous buffer, pH 2.3. Solubility decreases with increasing pH in the physiological range.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for 2 years after receipt when stored at +4°C.
HAZARD: HARMFUL.

Product Description
Potent insulin sensitizing agent. Peroxisome proliferator-activated receptor γ (PPAR-γ) agonist. Hepatoxic. Antidiabetic.

Not offered in the US.
Product Specific Literature References
Differential activity of rosiglitazone enantiomers at PPAR gamma: D.J. Parks, et al.; Bioorg. Med. Chem. Lett. 8, 3657 (1998) Abstract
Rosiglitazone: J.A. Balfour & G.L. Plosker; Drugs 57, 921 (1999), (Review) Abstract
Differential effects of insulin-sensitizers troglitazone and rosiglitazone on ion currents in rat vascular myocytes: G.A. Knock, et al.; Eur. J. Pharmacol. 368, 103 (1999) Abstract
Rosiglitazone: an agent from the thiazolidinedione class for the treatment of type 2 diabetes: A. Cheng-Lai & A. Levine; Heart Dis. 2, 326 (2000), (Review) Abstract
Rosiglitazone in the treatment of type 2 diabetes mellitus: a critical review: J.M. Malinowski & S. Bolesta; Clin. Ther. 22, 1151 (2000), (Review) Abstract
Rosiglitazone (Avandia): hepatic, cardiac and hematological reactions: M. McMorran & D. Vu; CMAJ 165, 82 (2001) Abstract
A review of rosiglitazone in type 2 diabetes mellitus: A.L. Werner & M.T. Travaglini; Pharmacotherapy 21, 1082 (2001), (Review) Abstract
Further Categories Containing This Product:
Antidiabetic Agents / Related Products
 
 
ALX-350-125 Revised 21-Sep-07
Rosiglitazone
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-125-M025   25 mg 98.00 USD Add To Cart
ALX-350-125-M100   100 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C18H19N3O3S
MW: 357.4
CAS NUMBER: 122320-73-4
MERCK INDEX: 14: 8265
PURITY: ≥97% (1H-NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (>25mg/ml), 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for 2 years after receipt when stored at +4°C. Stock solutions are stable for up to 3 months when stored at -20°C.

Product Description
Potent insulin sensitizing agent. Peroxisome proliferator-activated receptor γ (PPAR-γ) agonist. Hepatoxic. Antidiabetic.
Product Specific Literature References
Differential activity of rosiglitazone enantiomers at PPAR gamma: D.J. Parks, et al.; Bioorg. Med. Chem. Lett. 81, 3657 (1998) Abstract
Rosiglitazone: J.A. Balfour & G.L. Plosker; Drugs 57, 921 (1999), (Review) Abstract
Differential effects of insulin-sensitizers troglitazone and rosiglitazone on ion currents in rat vascular myocytes: G.A. Knock, et al.; Eur. J. Pharmacol. 368, 103 (1999) Abstract
Rosiglitazone: an agent from the thiazolidinedione class for the treatment of type 2 diabetes: A. Cheng-Lai & A. Levine; Heart Dis. 2, 326 (2000), (Review) Abstract
Rosiglitazone in the treatment of type 2 diabetes mellitus: a critical review: J.M. Malinowski & S. Bolesta; Clin. Ther. 22, 1151 (2000), (Review) Abstract
Rosiglitazone (Avandia): hepatic, cardiac and hematological reactions: M. McMorran & D. Vu; CMAJ 165, 82 (2001) Abstract
A review of rosiglitazone in type 2 diabetes mellitus: A.L. Werner & M.T. Travaglini; Pharmacotherapy 21, 1082 (2001), (Review) Abstract
Further Categories Containing This Product:
Antidiabetic Agents / Related Products
 
 
ALX-350-371 Revised 10-Mar-08 New product
Harmine