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G-Protein Coupled Receptors & Ligands / Related Products
You are here: Product Lines > Signal Transduction > Receptors > G-Protein Coupled Receptors & Ligands / Related Products
 
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ALX-340-060 Revised 10-Jul-08
Arachidonoyl serotonin
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SYNONYMS AA-5HT
N-[2-(5-Hydroxy-1H-indol-3-yl)]ethyl-5Z,8Z,11Z,14Z-eicosatetraenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Anandamide & Anandamide Analogs
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ALX-340-060-M005   5 mg 55.00 USD Add To Cart
Product Specification
FORMULA: C30H42N2O2
MW: 462.7
CAS NUMBER: 187947-37-1
PURITY: ≥98%
FORMULATION: Liquid. Solution in methyl acetate.
SOLUBILITY: Soluble in 100% ethanol (15mg/ml), DMSO (30mg/ml), dimethyl formamide (30mg/ml) or PBS, pH 7.2 (290μg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description
Tight binding, competitive inhibitor of fatty acid amide hydrolase (FAAH) (IC50=12µM).
Product Specific Literature References
Arachidonoylserotonin and other novel inhibitors of fatty acid amide hydrolase: T. Bisogno, et al.; BBRC 248, 515 (1998) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Fatty Acid Amide Hydrolase [FAAH] / Related Products
 
 
ALX-340-001 Revised 28-Jul-06
Arachidonyl trifluoromethylketone
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SYNONYMS AACOCF3
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PLA2 Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-340-001-M005   5 mg 70.00 USD Add To Cart
ALX-340-001-M010   10 mg 110.00 USD Add To Cart
ALX-340-001-M050   50 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C21H31F3O
MW: 356.5
CAS NUMBER: 149301-79-1
PURITY: ≥98%
APPEARANCE: Clear to yellow oil.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Dissolve in solvent purged with nitrogen or argon. Store under nitrogen or argon in tightly sealed container. Solutions are stable for up to 1 month when stored under nitrogen or argon in tightly sealed container at -80°C.
HANDLING: PROTECT FROM AIR!
HAZARD: TOXIC.

Product Description
Selective inhibitor of both, Ca2+-dependent and Ca2+-independent phospholipase A2 (PLA2), but not secretory PLA2 (sPLA2). Also inhibits fatty acid amide hydrolase (FAAH) and anandamide amidase.
Product Specific Literature References
Inhibitors of arachidonoyl ethanolamide hydrolysis: B. Koutek, et al.; J. Biol. Chem. 269, 22937 (1994) Abstract; Full Text
Further Categories Containing This Product:
Fatty Acid Amide Hydrolase [FAAH] / Related Products
 
 
ALX-350-312 Revised 28-May-08
(-)-Arctigenin
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SYNONYMS (3R,4R)-4-[(3,4-Dimethoxyphenyl)methyl]dihydro-3-[(4-hydroxy-3-methoxyphenyl)methyl]-2-(3H)-furanone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-312-M025   25 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C21H24O6
MW: 372.4
CAS NUMBER: 7770-78-7
SOURCE/HOST: Isolated from Arctium lappa.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (34mg/ml, heating, sonication); sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Lignan derivative, which shows antitumor, anti-inflammatory, immunomodulatory and neuroprotective activities. Down-regulates anti-apoptotic protein Bcl-XL. Potent inhibitor of HIV type-I integrase and DNA topoisomerase II. Shows phytoestrogenic and cytotoxic properties against Hep62 cells.  Antagonist for platelet activating factor and Ca2+. Blocks the activation of Akt (protein kinase B; PKB) induced by glucose starvation.
Product Specific Literature References
Antiproliferative effect of Arctigenin and Arctiin: S.Y. Ryu, et al.; Arch. Pharm. Res. 18, 462 (1995)
(-)-Arctigenin as a lead structure for inhibitors of human immunodeficiency virus type-1 integrase: E. Eich, et al.; J. Med. Chem 39, 86 (1996) Abstract
Immunomodulatory effect of arctigenin, a lignan compound, on tumour necrosis factor-alpha and nitric oxide production, and lymphocyte proliferation: J.Y. Cho, et al.; J. Pharm. Pharmacol. 51, 1267 (1999) Abstract
Arctigenin protects cultured cortical neurons from glutamate-induced neurodegeneration by binding to kainate receptor: Y.P. Jang, et al.; J. Neurosci. Res. 68, 233 (2002) 68, 233 (2002) Abstract
A phytochemical study of lignans in whole plants and cell suspension cultures of Anthriscus sylvestris: A. Koulman, et al.; Planta Med. 69, 733 (2003) Abstract
Naturally occurring lignans efficiently induce apoptosis in colorectal tumor cells: B. Hausott, et al.; J. Cancer Res. Clin. Oncol. 129, 569 (2003) Abstract
Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits MAP kinases and AP-1 activation via potent MKK inhibition: the role in TNF-alpha inhibition: M.K. Cho, et al.; Int. Immunopharmacol. 4, 1419 (2004) Abstract
Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits MAP kinases and AP-1 activation via potent MKK inhibition: the role in TNF-alpha inhibition: M.K. Cho, et al.; Int. Immunopharmacol. 4, 1419 (2004) Abstract
Identification of arctigenin as an antitumor agent having the ability to eliminate the tolerance of cancer cells to nutrient starvation: S. Awale, et al.; Cancer Res. 66, 1751 (2006) Abstract
The chemopreventive effects of Saussurea salicifolia through induction of apoptosis and phase II detoxification enzyme: K. Kang, et al.; Biol. Pharm. Bull. 30, 2352 (2007) Abstract
Further Categories Containing This Product:
Bcl-2 Family Modulators • Platelet Activating Factors [PAF] & Receptors / Related Products • Natural Products - Topoisomerase Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Immunomodulators • Natural Products - Nitric Oxide Pathway Modulators • HIV / AIDS / Related Products
 
 
ALX-350-318 Revised 17-Jun-08
(-)-Arctiin
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SYNONYMS (3R,4R)-4-[(3,4-Dimethoxyphenyl)methyl]-3-[[4-(β-D-glucopyranosyloxy)-3-methoxyphenyl]methyl]dihydro-2(3H)-furanone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-318-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C27H34O11
MW: 534.6
CAS NUMBER: 20362-31-6
SOURCE/HOST: Isolated from Arctium lappa.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (5mg/ml); sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Lignan derivative with antitumor activities. Down-regulates anti-apoptotic protein Bcl-XL. Potent inhibitor of HIV type-I integrase and DNA topoisomerase II. Shows phytoestrogenic activity and is an antagonist for platelet activating factor and Ca2+.
Product Specific Literature References
Platelet activating factor (PAF) antagonists contained in medicinal plants: lignans and sesquiterpenes: S. Iwakami, et al.; Chem. Pharm. Bull. (Tokyo) 40, 1196 (1992) Abstract
Antiproliferative effect of Arctigenin and Arctiin: S.Y. Ryu, et al.; Arch. Pharm. Res. 18, 462 (1995)
Cytotoxic components of bardanae fructus (goboshi): S. Moritani, et al.; Biol. Pharm. Bull. 19, 1515 (1996) Abstract
Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection: A.J. Vlietinck, et al.; Planta Med. 64, 97 (1998) Abstract
Anti-tumor-promoting activity of lignans from the aerial part of Saussurea medusa: M. Takasaki, et al.; Cancer Lett. 158, 53 (2000) Abstract
Isolation and identification of arctiin and arctigenin in leaves of burdock (Arctium lappa L.) by polyamide column chromatography in combination with HPLC-ESI/MS: S. Liu, et al.; Phytochem. Anal. 16, 86 (2005) Abstract
Application of preparative high-speed counter-current chromatography for separation and purification of arctiin from Fructus Arctii: X. Wang, et al.; J. Chromatogr. A. 1063, 247 (2005) Abstract
The chemopreventive effects of Saussurea salicifolia through induction of apoptosis and phase II detoxification enzyme: K. Kang, et al.; Biol. Pharm. Bull. 30, 2352 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Immunomodulators • Bcl-2 Family Modulators • Antitumor Agents (Anti-proliferative) • Platelet Activating Factors [PAF] & Receptors / Related Products • Natural Products - Topoisomerase Inhibitors • Natural Products - Antiviral / anti-HIV Agents • HIV / AIDS / Related Products
 
 
ALX-340-042 Revised 07-Jan-06
Arvanil
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SYNONYMS N-[(4-Hydroxy-3-methoxyphenyl)methyl]-5Z,8Z,11Z,14Z-eicosatetraenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-340-042-M005   5 mg 25.00 USD Add To Cart
Product Specification
FORMULA: C28H41NO3
MW: 439.6
CAS NUMBER: 128007-31-8
PURITY: ≥98%
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry.

Product Description
"Hybrid" activator of CB1 receptor (CB1: Ki=0.5µM; CB2: Ki=>15µM) and TRPV1 (Ki=0.3µM). Also inhibits anandamide uptake (IC50=3.6µM) and fatty acid amide hydrolase (FAAH) (IC50=3µM). Analgesic, vasodilatory and anti-inflammatory in vivo. Apoptosis inducer.
Product Specific Literature References
Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid receptors: D. Melck, et al.; BBRC 262, 275 (1999) Abstract
Neurobehavioral activity in mice of N-vanillyl-arachidonyl-amide: V. Di Marzo, et al.; Eur. J. Pharmacol. 406, 363 (2000) Abstract
A structure/activity relationship study on arvanil, an endocannabinoid and vanilloid hybrid: V. Di Marzo, et al.; J. Pharmacol. Exp. Ther. 300, 984 (2002) Abstract
The CB1/VR1 agonist arvanil induces apoptosis through an FADD/caspase-8-dependent pathway: R. Sancho, et al.; Br. J. Pharmacol. 140, 1035 (2003) Abstract
Evidence against the presence of an anandamide transporter: S.T. Glaser, et al.; PNAS 100, 4269 (2003) Abstract
Arvanil, a hybrid endocannabinoid and vanilloid compound, behaves as an antihyperkinetic agent in a rat model of Huntington's disease: E. de Lago, et al.; Brain Res. 1050, 210 (2005) Abstract
Arvanil inhibits T lymphocyte activation and ameliorates autoimmune encephalomyelitis: A.M. Malfitano, et al.; J. Neuroimmunol. 171, 110 (2006) Abstract
Further Categories Containing This Product:
Anandamide Uptake Inhibitors • Apoptosis Inducers & Inhibitors Other Products • TRPV1 Agonists and Antagonists / Related Products • Analgesic / Anti-nociceptive Agents / Related Products • Anti-inflammatory Agents Other Products • Fatty Acid Amide Hydrolase [FAAH] / Related Products
 
 
ALX-301-013 Revised 08-Jul-08
Azelaoyl-PAF
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SYNONYMS 1-O-Hexadecyl-2-O-(9-carboxyoctanoyl)-sn-glyceryl-3-phosphocholine
PRODUCT LINE Inflammation
PRODUCT CATEGORY Platelet Activating Factors [PAF] & Receptors / Related Products
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ALX-301-013-M001   1 mg 58.00 USD Add To Cart
ALX-301-013-M005   5 mg 261.00 USD Add To Cart
Product Specification
FORMULA: C33H66NO9P
MW: 651.9
SOURCE/HOST: Synthetic.
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: Soluble in DMSO (8mg/ml) or dimethyl formamide (33mg/ml) or PBS, pH 7.2 (10mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description
Potent PPARγ agonist which competes for the thiazoladinedione binding site. More potent than 15-deoxy-Δ12,14-prostaglandin J2 (Prod. No. ALX-340-022) and equipotent with rosiglitazone (Prod. No. ALX-350-125) as a ligand for this receptor.
Product Specific Literature References
Oxidized alkyl phospholipids are specific, high affinity peroxisome proliferator-activated receptor gamma ligands and agonists: S.S. Davies, et al.; J. Biol. Chem. 276, 16015 (2001) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Phospholipids / Related Products • PPAR Agonists
 
 
ALX-550-105 Revised 18-Jan-05
(±)-trans-Azetidine-2,4-dicarboxylic acid
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SYNONYMS t-ADA
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-105-M001   1 mg 15.00 USD Add To Cart
ALX-550-105-M005   5 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C5H7NO4
MW: 145.1
CAS NUMBER: 161596-62-9
PURITY: ≥95%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Selective agonist for group I mGluRs.
Product Specific Literature References
Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogues (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives: A.P. Kozikowski, et al.; J. Med. Chem. 36, 2706 (1993) Abstract
Trans-azetidine-2,4-dicarboxylic acid activates neuronal metabotropic receptors: M. Favaron, et al.; Neuroreport 4, 967 (1993) Abstract
Metabotropic glutamate receptor subtypes differentially influence neuronal recovery from in vitro hypoxia/hypoglycemia in rat hippocampal slices: T. Opitz, et al.; Neuroscience 68, 989 (1995) Abstract
Block of spatial learning by mGluR agonist tADA in rats: G. Riedel, et al.; Neuropharmacology 34, 559 (1995) Abstract
Open field behaviour in rats: role of metabotropic glutamate receptors: W. Wetzel, et al.; Neuroreport 6, 2389 (1995) Abstract
Physiological and pharmacological profile of trans-azetidine-2,4- dicarboxylic acid: metabotropic glutamate receptor agonism and effects on long-term potentiation: D. Manahan-Vaughan, et al.; Neuroscience 72, 999 (1996) Abstract
Activation of phospholipases C and D by the novel metabotropic glutamate receptor agonist tADA: J. Klein, et al.; Neuropharmacology 36, 261 (1997) Abstract
Antisense ablation of type I metabotropic glutamate receptor mGluR1 inhibits spinal nociceptive transmission: M.R. Young, et al.; J. Neurosci. 18, 10180 (1998) Abstract; Full Text
 
 
ALX-550-117 Revised 16-Aug-02
(2R,4R)-(+)-Azetidine-2,4-dicarboxylic acid
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-117-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C5H7NO4
MW: 145.1
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Specific Literature References
Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogues (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives: A.P. Kozikowski, et al.; J. Med. Chem. 36, 2706 (1993) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999), (Reviev) Abstract
 
 
ALX-550-116 Revised 16-Aug-02
(2S,4S)-(-)-Azetidine-2,4-dicarboxylic acid
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-116-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C5H7NO4
MW: 145.1
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Specific Literature References
Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogues (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives: A.P. Kozikowski, et al.; J. Med. Chem. 36, 2706 (1993) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999), (Review) Abstract
 
 
ALX-550-320 Revised 07-Dec-04
Benserazide . hydrochloride
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SYNONYMS DL-Serine 2-[(2,3,4-trihydroxyphenyl)methyl]hydrazide . HCl
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Dopaminergics & Dopamine Receptors / Related Products
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ALX-550-320-G001   1 g 35.00 USD Add To Cart
ALX-550-320-G005   5 g 135.00 USD Add To Cart
Product Specification
FORMULA: C10H15N3O5. HCl
MW: 257.3 . 36.5