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G-Protein Coupled Receptor Signalling
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ALX-350-291 Revised 19-Oct-07
Hymenidin
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SYNONYMS 2-Debromooroidin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-291-M001   1 mg 230.00 USD Add To Cart
Product Specification
FORMULA: C11H12BrN5O
MW: 310.2
CAS NUMBER: 107019-95-4
SOURCE/HOST: Isolated from Hymeniacidon sp.
PURITY: ≥95%
APPEARANCE: Amorphous solid.
SOLUBILITY: Soluble in DMSO or 100 % ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC. CYTOTOXIC.

Product Description
Antagonist of serotonergic receptors. Inhibitor of CDK5/p25 (IC50=4µM) and GSK-3β (IC50=12µM). 
Product Specific Literature References
A novel antagonist of serotonergic receptors, hymenidin, isolated from the Okinawan marine sponge Hymeniacidon sp: J. Kobayashi, et al.; Experientia 42, 1176 (1986) Abstract
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000)
Brominated pyrrole alkaloids from marine Agelas sponges reduce depolarization-induced cellular calcium elevation: U. Bickmeyer, et al.; Toxicon. 44, 45 (2004) Abstract
Marine compounds for the therapeutic treatment of neurological disorders: D. Alonso, et al.; Expert Opininon on Therapeutic Patents 15, 1377 (2005)
 
 
ALX-480-038 Revised 18-Jun-08
IBMX
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SYNONYMS 3-Isobutyl-1-methylxanthine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Adenosine Receptors / Related Products
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ALX-480-038-M500   500 mg 99.00 USD Add To Cart
ALX-480-038-G001   1 g 195.00 USD Add To Cart
Product Specification
FORMULA: C10H14N4O2
MW: 222.3
CAS NUMBER: 28822-58-4
RTECS: ZD8500000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or methanol (warm, 50mg/ml); almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.
IDENTITY: Identity determined by IR.

Product Description
Potent, non-specific inhibitor of phosphodiesterases. More potent than theophylline (Prod. No. ALX-480-062) at adenosine receptors. Accelerates conversion of mouse fibroblast cells into adipose cells.
Product Specific Literature References
Effects of xanthine derivatives on lipolysis and on adenosine 3',5'- monophosphate phosphodiesterase activity: J.A. Beavo, et al.; Mol. Pharmacol. 6, 597 (1970) Abstract
Adenosine 3':5'-cyclic monophosphate and insulin release: W. Montague & J.R. Cook; Biochem. J. 120, 9P (1970) Abstract
The role of adenosine 3':5'-cyclic monophosphate in the regulation of insulin release by isolated rat islets of Langerhans: W. Montague & J.R. Cook; Biochem. J. 122, 115 (1971) Abstract
Cyclic nucleotide phosphodiesterase activity in normal mouse pancreatic islets: S.J. Ashcroft, et al.; FEBS Lett. 20, 263 (1972) Abstract
The mode of action of adenosine 3’:5’-cyclic monophosphate in mammalian islets of Langerhans. Effects of insulin secretagogues on islet-cell protein kinase activity: W. Montague & S.L. Howell; Biochem. J. 134, 321 (1973) Abstract
Effects of methylxanthines on adenosine 3’,5’-monophosphate and corticosterone in the rat adrenal: A. Peytremann, et al.; Endocrinology 92, 525 (1973) Abstract
Concentration of adenosine 3’:5’-cyclic monophosphate in mouse pancreatic islets measured by a protein-binding radioassay: R.H. Cooper, et al.; Biochem. J. 134, 599 (1973) Abstract
Determination of theophylline in plasma by electron capture gas chromatography: H.A. Schwertner, et al.; Anal. Chem. 48, 1875 (1976) Abstract
Methyl xanthine phosphodiesterase inhibitors behave as prostaglandin antagonists in a perfused rat mesenteric artery preparation: D.F. Horrobin, et al.; Prostaglandins 13, 33 (1977) Abstract
Selective inhibition of cyclic nucleotide phosphodiesterases by analogues of 1-methyl-3-isobutylxanthine: G.L. Kramer, et al.; Biochemistry 16, 3316 (1977) Abstract
Cyclic nucleotide phosphodiesterases of human and rat gastric mucosa: U. Klotz, et al.; Naunyn-Schmiedebergs Arch. Pharmacol. 296, 187 (1977) Abstract
Allergic reactions, cyclic AMP and histamine release: P.S. Skov, et al.; Experientia 33, 965 (1977) Abstract
Differentiation of 3T3-L2 fibroblasts into adipose cells in bromodeoxyuridine-suppressed cultures: T.R. Russell; PNAS 76, 4451 (1979) Abstract
Inhibition of growth of primary and metastatic Lewis lung carcinoma cells by the phosphodiesterase inhibitor isobutylmethylxanthine: P. Janik, et al.; Cancer Res. 40, 1950 (1980) Abstract
Induction of a transient elevation in intracellular levels of adenosine-3’,5’-cyclic monophosphate by chemotactic factors: an early event in human neutrophil activation: L. Simchowitz, et al.; J. Immunol. 124, 1482 (1980) Abstract
Selective inhibition of cyclic AMP and cyclic GMP phosphodiesterases of cardiac nuclear fraction: G.S. Ahluwalia & A.R. Rhoads; Biochem. Pharmacol. 31, 665 (1982) Abstract
Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes: R.F. Bruns, et al.; Mol. Pharmacol. 29, 331 (1986) Abstract
Methylxanthine inhibitors of phosphodiesterases: J.N. Wells & J.R. Miller; Methods Enzymol. 159, 489 (1988) Abstract
Psychomotor-stimulant effects of 3-isobutyl-1-methylxanthine: comparison with caffeine and 7-(2-chloroethyl) theophylline: V.L. Coffin and R.D. Spealman; Eur. J. Pharmacol. 170, 35 (1989) Abstract
Differential effects of Ro 20-1724 and isobutylmethylxanthine on the basal force of contraction and beta-adrenoceptor-mediated response in the rat ventricular myocardium: Y. Katano & M. Endoh; BBRC 167, 123 (1990) Abstract
Bemoradan--a novel inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue: J.B. Moore, Jr., et al.; Biochem. Pharmacol. 42, 679 (1991) Abstract
Effect of an antihypertensive hydrazine derivative on Ca2+ current of single frog cardiac cells: F. Scamps, et al.; Eur. J. Pharmacol. 244, 119 (1993) Abstract
Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity: C. Tomes, et al.; Cell. Signal. 5, 615 (1993) Abstract
Further Categories Containing This Product:
Phosphodiesterases / Related Products
 
 
ALX-550-049 Revised 09-Oct-08
(±)-Ibotenic acid
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SYNONYMS (±)α-Amino-3-hydroxy-5-isoxazoleacetic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Neurotoxins
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ALX-550-049-M001   1 mg 55.00 USD Add To Cart
ALX-550-049-M005   5 mg 220.00 USD Add To Cart
ALX-550-049-M025   25 mg 690.00 USD Add To Cart
Product Specification
FORMULA: C5H6N2O4
MW: 158.1
CAS NUMBER: 2552-55-8
MERCK INDEX: 14: 4877
RTECS: NY2100000
SOURCE/HOST: Synthetic.
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: TOXIC.

Product Description
Potent glutamate receptor agonist. Neurotoxic agent.
Product Specific Literature References
Central actions of ibotenic acid and muscimol: G.A. Johnston, et al.; Biochem. Pharmacol. 17, 2488 (1968) Abstract
Spinal interneurone excitation by conformationally restricted analogues of L-glutamic acid: G.A. Johnston, et al.; Nature 248, 804 (1974) Abstract
Excitatory amino acid transmitters: J.C. Watkins and R.H. Evans; Annu. Rev. Pharmacol. Toxicol. 21, 165 (1981), (Review) Abstract
Agonists and antagonists for metabotropic glutamate receptors: P.L. Ornstein, et al.; Curr. Pharm. Design 1, 355 (1995), (Review)
 
 
ALX-270-091 Revised 02-Jul-04
IMMA
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SYNONYMS Indomethacin morpholinylamide
BML-190
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-270-091-M005   5 mg 33.00 USD Add To Cart
Product Specification
FORMULA: C23H23N2O4Cl
MW: 426.9
PURITY: ≥98%
APPEARANCE: Crystalline solid.
SOLUBILITY: Soluble in DMSO or dimethylformamide purged with an inert gas.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Selective CB2 receptor ligand (CB1: Ki>2mM; CB2: Ki=435nM).
Product Specific Literature References
New class of potent ligands for the human peripheral cannabinoid receptor: N. Tremblay, et al.; Bioorg. Med. Chem. Lett. 6, 2263 (1996)
 
 
ALX-550-412 Revised 22-Apr-08
JNJ 16259685
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-412-M005   5 mg 80.00 USD Add To Cart
ALX-550-412-M025   25 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C20H23NO3
MW: 325.4
CAS NUMBER: 409345-29-5
PURITY: ≥98% (1H-NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Sub-nanomolar potent, non-competitive mGlu1 antagonist (Ki=0.34nM). Inhibits glutamate-induced Ca2+ response at the human mGluR1 (IC50=0.55nM). Selective over mGluR5 (>400-fold). Displays no activity at mGluR2, mGluR3, mGluR4, mGluR6, AMPA or NMDA receptors (IC50>10µM). Centrally active following systemic administration.
Product Specific Literature References
JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist: H. Lavreysen, et al.; Neuropharmacology 47, 961 (2004) Abstract
Effects of mGlu1 receptor blockade on anxiety-related behaviour in the rat lick suppression test: T. Steckler, et al.; Psychopharmacology 179, 198 (2005) Abstract
Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial Water maze task: T. Steckler, et al.; Behav. Brain. Res. 164, 52 (2005) Abstract
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists: D. Mabire, et al.; J. Med. Chem. 48, 2134 (2005) Abstract
Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices: I. Fukunaga, et al.; Br. J. Pharmacol. 151, 870 (2007) Abstract
Two new non-competitive mGlu1 receptor antagonists are potent tools to unravel functions of this mGlu receptor subtype: T. Knöpfel; Br. J. Pharmacol. 151, 723 (2007) Abstract
 
 
ALX-630-077 Revised 27-Nov-07
Joro Spider Toxin
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SYNONYMS JSTX-3
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Neurotoxins
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ALX-630-077-C100   100 µg 590.00 USD Add To Cart
Product Specification
FORMULA: C27H47N7O6
MW: 565.7
CAS NUMBER: 112163-33-4
SOURCE/HOST: Synthetic. Originally isolated from the spider Nephila clavata.
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Hygroscopic. Protect from light and moisture.
HAZARD: VERY TOXIC.

Product Description
Specific, irreversible inhibitor of excitatory post-synaptic potentials. Blocks post-synaptic glutamate potentials. Blocks quisqualate-sensitive glutamate receptors. However, aspartate-induced depolarization, nerve terminal spikes, resting membrane conductance, and inhibitory postsynaptic potentials are unaffected. Antiepileptic. Potent neurotoxin.
Product Specific Literature References
Spider venom contains specific receptor blocker of glutaminergic synapses: N. Kawai, et al.; Brain Res. 247, 169 (1982) Abstract
Uterine arginase inhibition affect the rat embryonic development: Y. Aramaki, et al.; Proc. Jpn. Acad. Ser. B 62, 359 (1986)
Newly synthesized analogues of the spider toxin block the crustacean glutamate receptor: K. Shudo, et al.; Neurosci. Res. 5, 82 (1987) Abstract
Spider toxins as tools for dissecting elements of excitatory amino acid transmission: H. Jackson and P.N. Usherwood; TINS 11, 278 (1988) Abstract
Effects of a spider toxin (JSTX) on hippocampal CA1 neurons in vitro: M. Saito, et al.; Brain Res. 481, 16 (1989) Abstract
A histochemical study of glutamate receptor in rat brain using biotinyl spider toxin: K. Shimazaki, et al.; Neurosci. Lett. 114, 1 (1990) Abstract
A voltage-clamp study of the effects of Joro spider toxin and zinc on excitatory synaptic transmission in CA1 pyramidal cells of the guinea pig hippocampal slice: Y. Sahara, et al.; Neurosci. Res. 10, 200 (1991) Abstract
Spider toxin and pertussis toxin differentiate post- and presynaptic glutamate receptors: N. Kawai; Neurosci. Res. 12, 3 (1991), (Review) Abstract
Arylamine spider toxins antagonize NMDA receptor-mediated synaptic transmission in rat hippocampal slices: A. L. Mueller, et al.; Synapse 9, 244 (1991) Abstract
Ca2+ permeability and joro spider toxin sensitivity of AMPA and kainate receptors on cerebellar granule cells: J. R. Savidge & D. R. Bristow; Eur. J. Pharmacol. 351, 131 (1998) Abstract
Antiepileptic effect of acylpolyaminetoxin JSTX-3 on rat hippocampal CA1 neurons in vitro: S. D. Salamoni, et al.; Brain Res. 1048, 170 (2005) Abstract
Further Categories Containing This Product:
Glutamate Receptors (Metabotropic) / Related Products
 
 
ALX-550-523 Revised 11-Apr-07
JP83
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SYNONYMS 3’-Carbamoyl-biphenyl-3-yl-hexylphenylcarbamate
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Fatty Acid Amide Hydrolase [FAAH] / Related Products
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ALX-550-523-M005   5 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C26H28N2O3
MW: 416.5
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide; sparingly soluble in aqueous buffers.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 2 years after receipt when stored at -20°C.

Product Description
Irreversible inhibitor of human fatty acid amide hydrolase (FAAH) (IC50=14nM), when tested using radiolabelled oleamide as the substrate.
Product Specific Literature References
Mechanism of carbamate inactivation of FAAH: implications for the design of covalent inhibitors and in vivo functional probes for enzymes: J.P. Alexander and B.F. Cravatt; Chem. Biol. 12, 1179 (2005) Abstract
 
 
ALX-550-385 Revised 22-Sep-08
JWH-015
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SYNONYMS (2-Methyl-1-propyl-1H-indol-3-yl)-1-naphthalenylmethanone
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-550-385-M005   5 mg 75.00 USD Add To Cart
ALX-550-385-M025   25 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C23H21NO
MW: 327.4
CAS NUMBER: 155471-08-2
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol (8mg/ml) or DMSO (3mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. Solutions are stable for up to 3 months when stored at -20°C.
HAZARD: IRRITANT.

Product Description
Selective CB2 receptor agonist (Ki=13.8nM at human cloned CB1 and CB2 receptors).
Product Specific Literature References
Evidence for the presence of CB2-like cannabinoid receptors on peripheral nerve terminals: G. Griffin, et al.; Eur. J. Pharmacol. 339, 53 (1997) Abstract
Pharmacology of cannabinoid receptor ligands: R.G. Pertwee; Curr. Med. Chem. 6, 635 (1999) Abstract
The third transmembrane helix of the cannabinoid receptor plays a role in the selectivity of aminoalkylindoles for CB2, peripheral cannabinoid receptor: C.N. Chin, et al.; J. Pharmacol. Exp. Ther. 291, 837 (19993) Abstract
 
 
ALX-380-066 Revised 07-Apr-08
Kendomycin
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SYNONYMS (-)-TAN 2162
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-066-C100   100 µg 95.00 USD Add To Cart
ALX-380-066-C500   500 µg 370.00 USD Add To Cart
Product Specification
FORMULA: C29H42O6
MW: 486.6
CAS NUMBER: 59785-91-0
SOURCE/HOST: Isolated from Streptomyces violaceoruber.
PURITY: ≥98%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Potent endothelin receptor antagonist. Anti-osteoporotic compound. Shows remarkable antibacterial and cytotoxic activity. Mediates its cytotoxic effects, at least in part, through proteasome inhibition.
Product Specific Literature References
2000 Structure and biosynthesis of kendomycin, a carboxylic ansa-compound from Streptomyces: A.Zeeck & H.B. Bode; J. Chem. Soc. Perkin Trans. 323 (2000)
Evidence for the mode of action of the highly cytotoxic Streptomyces polyketide kendomycin: Y.A. Elnakady, et al.; Chembiochem. 8, 1261 (2007) Abstract
 
 
ALX-550-051 Revised 27-Aug-07
Ketanserin . tartrate