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G-Protein Coupled Receptor Signalling
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ALX-350-104 Revised 10-May-07
Aaptamine
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SYNONYMS 8,9-Dimethoxy-1H-benzo[de][1,6]naphtyridine
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Toxins
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ALX-350-104-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C13H12N2O2
MW: 228.3
CAS NUMBER: 85547-22-4
SOURCE/HOST: Isolated from the sponge Aaptos aaptos.
PURITY: ≥97%
APPEARANCE: Oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Competitive antagonist of α-adrenoceptors in vascular smooth muscle cells. Inhibits cancer cell growth.
Product Specific Literature References
Alpha-adrenoceptor blocking action of aaptamine, a novel marine natural product, in vascular smooth muscle: Y. Ohizumi, et al.; J. Pharm. Pharmacol. 36, 785 (1984) Abstract
Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine: G.R. Pettit, et al.; J. Org. Chem. 69, 2251 (2004) Abstract
Aaptamine, a spongean alkaloid, activates p21 promoter in a p53-independent manner: S. Aoki, et al.; BBRC 342, 101 (2006) Abstract
Further Categories Containing This Product:
Adrenergics & Adrenergic Receptors / Related Products • Natural Products - Antitumor Reagents • Alkaloids • Antitumor Agents (Anti-proliferative) • Marine Natural Products
 
 
ALX-151-020 Revised 10-Feb-05
N-Acetyl-Asp-Glu-OH
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SYNONYMS α-NAAG
Spaglumic acid
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-151-020-M010   10 mg 35.00 USD Add To Cart
ALX-151-020-M050   50 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C11H16N2O8
MW: 304.3
CAS NUMBER: 3106-85-2
PURITY: ≥98%
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
Product Description
Endogenous neurotransmitter with high affinity for the brain glutamate receptor. N-acetylated α-linked acidic dipeptidase (NAALADase), a membrane-bound peptidase, hydrolyzes α-NAAG, a major brain peptide, to N-acetylaspartate and glutamate. Discriminates between mGluR2 and mGluR3. mGluR3 activator. NMDA receptor antagonist. Neuroprotective.
Product Specific Literature References
N-acetylaspartylglutamate: an endogenous peptide with high affinity for a brain glutamate receptor: R. Zaczek, et al.; PNAS 80, 1116 (1983) Abstract
Characterization of the interactions of N-acetyl-aspartyl-glutamate with [3H]L-glutamate receptors: K.J. Koller & J.T. Coyle; Eur. J. Pharmacol. 98, 193 (1984) Abstract
The neurobiology of N-acetylaspartylglutamate: R.D. Blakely & J.T. Coyle; Int. Rev. Neurobiol. 30, 39 (1988) Abstract
Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase: P.F. Jackson, et al.; J. Med. Chem. 39, 619 (1996) Abstract
The nagging question of the function of N-acetylaspartylglutamate: J.T. Coyle; Neurobiol. Dis. 4, 231 (1997) Abstract
N-acetylaspartylglutamate stimulates metabotropic glutamate receptor 3 to regulate expression of the GABA(A) alpha6 subunit in cerebellar granule cells: S. Ghose, et al.; J. Neurochem. 69, 2326 (1997) Abstract
N-acetylaspartylglutamate (NAAG) protects against rat striatal quinolinic acid lesions in vivo: L.R. Orlando, et al.; Neurosci. Lett. 236, 91 (1997) Abstract
N-acetylaspartylglutamate, N-acetylaspartate, and N-acetylated alpha-linked acidic dipeptidase in human brain and their alterations in Huntington and Alzheimer's diseases: L.A. Passani, et al.; Mol. Chem. Neuropathol. 31, 97 (1997) Abstract
Distribution of N-acetylaspartylglutamate immunoreactivity in human brain and its alteration in neurodegenerative disease: L.A. Passani, et al.; Brain Res. 772, 9 (1997) Abstract
N-acetylaspartylglutamate selectively activates mGluR3 receptors in transfected cells: B. Wroblewska, et al.; J. Neurochem. 69, 174 (1997) Abstract
Neuroprotective activity of N-acetylaspartylglutamate in cultured cortical cells: V. Bruno, et al.; Neuroscience 85, 751 (1998) Abstract
N-acetylaspartylglutamate activates cyclic AMP-coupled metabotropic glutamate receptors in cerebellar astrocytes: B. Wroblewska, et al.; Glia 24, 172 (1998) Abstract
A.P. Burlina, et al.; Eur. J. Pediatr. 158, 406 (1999) Abstract
Further Categories Containing This Product:
NMDA Receptors / Related Products • NAALADase / Related Products • Peptides
 
 
ALX-290-001 Revised 29-Nov-04
N-Acetyl-S-farnesyl-L-cysteine
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SYNONYMS AFC
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-001-M005   5 mg 50.00 USD Add To Cart
ALX-290-001-M025   25 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C20H33NO3S
MW: 367.6
CAS NUMBER: 135304-07-3
PURITY: ≥97%
APPEARANCE: Clear oil.
SOLUBILITY: Soluble in DMSO, methanol or ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Specific inhibitor of S-farnesylcysteine methyl transferase.
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ALX-290-010 Revised 20-Apr-07
N-Acetyl-S-farnesyl-L-cysteine-methyl ester
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SYNONYMS AFCME
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-010-M010   10 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C21H35NO3S
MW: 381.6
CAS NUMBER: 135304-08-4
PURITY: ≥95%
APPEARANCE: White to slightly yellow powder.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.

Product Description
Substrate for studying the reversibility of carboxyl methylation in signal-transducing G-proteins.
Product Specific Literature References
Methylation and demethylation reactions of guanine nucleotide-binding proteins of retinal rod outer segments: D. Pérez-Sala, et al.; PNAS 88, 3043 (1991) Abstract
Identifying the recognition unit for G protein methylation: E.W. Tan, et al.; J. Biol. Chem. 266, 10719 (1991) Abstract; Full Text
 
 
ALX-290-007 Revised 02-Jun-08
N-Acetyl-S-geranyl-L-cysteine
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SYNONYMS AGC
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Geranyl-related Reagents
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ALX-290-007-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C15H25NO3S
MW: 299.4
PURITY: ≥98% (TLC)
APPEARANCE: Clear to pale yellow viscous oil.
SOLUBILITY: > 25mg/ml soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions may be stored at -20 °C for up to 3 months. Product is not sterile.

Product Description
Negative control for AFC (Prod. No. ALX-290-001) and AGGC (Prod. No. ALX-290-008). Has a closely similar structure to these two compounds but lacks their biological activity.
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ALX-290-008 Revised 13-Jul-06
N-Acetyl-S-geranylgeranyl-L-cysteine
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SYNONYMS AGGC
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Geranyl-related Reagents
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ALX-290-008-M005   5 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C25H41NO3S
MW: 435.7
CAS NUMBER: 139332-94-8
PURITY: ≥98%
APPEARANCE: Viscous yellow oil.
SOLUBILITY: Soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Specifically blocks methyl esterification of geranylgeranylated proteins such as Rab proteins. Blocks receptor-mediated signal transduction in human neutrophils (IC50=4µM). Induces insulin release from HIT-T15 cells by mimicking the action of Rab3A. Inhibits β2-integrin-induced actin polymerization (IC50~45nM) in neutrophils.
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ALX-550-208 Revised 17-Dec-04
N-Acetyl-5-hydroxytryptamine
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SYNONYMS N-Acetylserotonin
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Melatonin Receptors / Related Products
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ALX-550-208-M010   10 mg 10.00 USD Add To Cart
ALX-550-208-M050   50 mg 25.00 USD Add To Cart
ALX-550-208-M500   500 mg 125.00 USD Add To Cart
Product Specification
FORMULA: C12H14N2O2
MW: 218.3
CAS NUMBER: 1210-83-9; 17994-17-1
PURITY: ≥99%
APPEARANCE: Off-white powder.
SOLUBILITY: Soluble in ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Metabolite of serotonin (Prod. No. ALX-550-328). Precursor of melatonin (Prod. No. ALX-550-071). Inhibitor of hydroxyindole-O-methyltransferase.
Product Specific Literature References
The metabolism of serotonin (5-hydroxytryptamine): W.M. McIsaac and I.H. Page; J. Biol. Chem. 234, 858 (1959) Full Text
Hydroxyindole-O-methyltransferase. I. Substrate binding: B.T. Ho, et al.; J. Pharm. Sci. 58, 130 (1969) Abstract
Hydroxyindole-O-methyltransferase. II. Inhibitory activities of some N- acyltryptamines: B.T. Ho, et al.; J. Pharm. Sci. 57, 1998 (1968) Abstract
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Serotonergics & Serotonin Receptors / Related Products
 
 
ALX-550-200 Revised 09-Aug-02
N-Acetyltryptamine
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY Melatonin Receptors / Related Products
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ALX-550-200-M005   5 mg 50.00 USD Add To Cart
ALX-550-200-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C12H14N2O
MW: 202.3
CAS NUMBER: 1016-47-3
PURITY: ≥97%
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Partial agonist for melatonin receptors.
Product Specific Literature References
Characterization of a retinal melatonin receptor: M.L. Dubocovich; J. Pharmacol. Exp. Ther. 234, 395 (1985) Abstract
Luzindole (N-0774): a novel melatonin receptor antagonist: M.L. Dubocovich; J. Pharmacol. Exp. Ther. 246, 902 (1988) Abstract
 
 
ALX-550-017 Revised 17-Jan-05
cis-ACPD
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SYNONYMS (±)-1-Aminocyclopentane-cis-1,3-dicarboxylic acid
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-017-M005   5 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C7H11NO4
MW: 173.2
CAS NUMBER: 39026-63-6
PURITY: ≥97%
APPEARANCE: White solid.
SOLUBILITY: Soluble in dilute aqueous base.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

(1S,3S)-ACPD
(1R,3R)-ACPD
Product Description
Potent NMDA agonist. Equimolar mixture of (1R,3R)-ACPD (Prod. No. ALX-550-018) and (1S,3S)-ACPD (Prod. No. ALX-550-019).
Product Specific Literature References
Receptors for the excitatory amino acids in the mammalian central nervous system: H. McLennan; Prog. Neurobiol. 20, 251 (1983) Abstract
Structure/activity relations of N-methyl-D-aspartate receptor ligands as studied by their inhibition of [3H]D-2-amino-5-phosphonopentanoic acid binding in rat brain membranes: H.J. Olverman, et al.; Neuroscience 26, 17 (1988) Abstract
In vitro and in vivo pharmacology of trans- and cis-(+-)-1-amino-1,3-cyclopentanedicarboxylic acid: dissociation of metabotropic and ionotropic excitatory amino acid receptor effects: D.D. Schoepp, et al.; J. Neurochem. 56, 1789 (1991) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999), (Review) Abstract
Further Categories Containing This Product:
NMDA Receptors / Related Products • Excitatory Amino Acids
 
 
ALX-550-020 Revised 11-Mar-08
trans-ACPD
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SYNONYMS (±)-1-Aminocyclopentane-trans-1,3-dicarboxylic acid
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-020-M005   5 mg 55.00 USD Add To Cart
ALX-550-020-M025   25 mg 220.00 USD Add To Cart
Product Specification
FORMULA: C7H11NO4
MW: 173.2
CAS NUMBER: 67684-64-4, 39026-64-7
RTECS: GY4060000
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in dilute aqueous base or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: HARMFUL.
IDENTITY: Identity determined by NMR.

 (1R,3S)-ACPD
Product Description
Equimolar mixture of (1S,3R)-ACPD (Prod. No. ALX-550-021) and (1R,3S)-ACPD. Selective agonist for mGluRs (active at both group I and group II mGluRs).
Product Specific Literature References
The excitatory amino acid receptors: their classes, pharmacology, and distinct properties in the function of the central nervous system: D.T. Monaghan, et al.; Annu. Rev. Pharmacol. Toxicol. 29, 365 (1989) Abstract
Trans-ACPD, a selective agonist of the phosphoinositide-coupled excitatory amino acid receptor: E. Palmer, et al.; Eur. J. Pharmacol. 166, 585 (1989) Abstract
In vitro and in vivo pharmacology of trans- and cis-(+-)-1-amino-1,3-cyclopentanedicarboxylic acid: dissociation of metabotropic and ionotropic excitatory amino acid receptor effects: D.D. Schoepp, et al.; J. Neurochem. 56, 1789 (1991) Abstract
Molecular diversity of glutamate receptors and implications for brain function: S. Nakanishi; Science 258, 597 (1992) Abstract
Neuroprotective sigma ligands attenuate NMDA and trans-ACPD-induced calcium signaling in rat primary neurons: K.L. Klette, et al.; Brain Res. 756, 231 (1997) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999), (Review) Abstract
Metabotropic glutamate receptor agonists reduce glutamate release from cultured astrocytes: Z.C. Ye & H. Sontheimer; Glia 25, 270 (1999) Abstract
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Further Categories Containing This Product:
Excitatory Amino Acids
 
 
ALX-550-018 Revised 03-Mar-05
(1R,3R)-ACPD
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