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cAMP Pathways
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ALX-270-080 Revised 17-Apr-08
MDL-12,330A . hydrochloride
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SYNONYMS cis-N-(2-Phenylcyclopentyl)azacyclotridec-1-en-2-amine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Adenylyl Cyclase Inhibitors
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ALX-270-080-M001   1 mg 28.00 USD Add To Cart
ALX-270-080-M005   5 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C23H36N2 . HCl
MW: 340.6 . 36.5
CAS NUMBER: 40297-09-4
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water (2.75mg/ml), 100% ethanol (>10mg/ml), DMSO (7mg/ml) or hot 0.1N HCl (0.5 mg/ml); insoluble in 0.1N NaOH. .
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Cell permeable irreversible inhibitor of adenylate cyclase (IC50= 250µM).
Product Specific Literature References
Actions of vasopressin and isoprenaline on the ionic transport across the isolated frog skin in the presence and the absence of adenyl cyclase inhibitors MDL12330A and SQ22536: C. Lippe & C. Ardizzone; Comp. Biochem. Physiol. 99, 209 (1991) Abstract
Tonic adenosine A2A receptor activation modulates nicotinic autoreceptor function at the rat neuromuscular junction: P. Correia-de-Sa & J.A. Ribeiro; Eur. J. Pharmacol. 271, 349 (1994) Abstract
 
 
ALX-300-147 Revised 11-Jul-08
Dihomo-γ-linolenylethanolamide
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SYNONYMS N-(2-Hydroxyethyl)-8Z,11Z,14Z-eicosatrienamide
HEA
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Endocannabinoids
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ALX-300-147-M005   5 mg 63.00 USD Add To Cart
Product Specification
FORMULA: C22H39NO2
MW: 349.6
CAS NUMBER: 150314-34-4
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: Soluble in  DMSO (30mg/ml) or dimethyl formamide (10mg/ml); 8mg/ml soluble in a 1:2 solution of ethanol:PBS (pH 7.2) (dilute the ethanol solution with PBS).
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.
HANDLING: Protect from light.

Product Description
Endocannabinoid. Binds to recombinant human CB1 (Ki=857nM) and CB2 receptor (Ki=598nM). Also inhibits adenylyl cyclase (IC50=109nM).
Product Specific Literature References
Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor: L. Hanus, et al.; J. Med. Chem. 36, 3032 (1993) Abstract
Anandamide, an endogenous cannabimimetic eicosanoid, binds to the cloned human cannabinoid receptor and stimulates receptor-mediated signal transduction: C.C. Felder, et al.; PNAS 90, 7656 (1993) Abstract
Cannabinomimetic behavioral effects of and adenylate cyclase inhibition by two new endogenous anandamides: J. Barg, et al.; Eur. J. Pharmacol. 287, 145 (1995) Abstract
Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors: C.C. Felder, et al.; Mol. Pharmacol. 48, 443 (1995) Abstract
Astrocytes in culture produce anandamide and other acylethanolamides: L. Walter, et al.; Biol. Chem. 277, 20869 (2002) Abstract
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:
Adenylyl Cyclase Inhibitors
 
 
ALX-300-148 Revised 11-Jul-08
Docosatetraenylethanolamide
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SYNONYMS N-(2-Hydroxyethyl)-7Z,10Z,13Z,16Z-docosatetraenamide
DEA
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Endocannabinoids
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ALX-300-148-M005   5 mg 63.00 USD Add To Cart
Product Specification
FORMULA: C24H41NO2
MW: 375.6
CAS NUMBER: 150314-35-5
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: 10mg/ml soluble in DMSO or dimethyl formamide; 8mg/ml soluble in 1:2 solution of ethanol:PBS (pH 7.2) (dilute the ethanol solution with PBS).
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.
HANDLING: Protect from light.

Product Description
Endocannabinoid. Also inhibits adenylate cyclase (IC50=117nM). Does also bind to TRPV1 (Ki=5.63µM).
Product Specific Literature References
Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor: L. Hanus, et al.; J. Med. Chem. 36, 3032 (1993) Abstract
Anandamide, an endogenous cannabimimetic eicosanoid, binds to the cloned human cannabinoid receptor and stimulates receptor-mediated signal transduction: C.C. Felder, et al.; PNAS 90, 7656 (1993) Abstract
Cannabinomimetic behavioral effects of and adenylate cyclase inhibition by two new endogenous anandamides: J. Barg, et al.; Eur. J. Pharmacol. 287, 145 (1995) Abstract
Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens: R.A. Ross, et al.; Br. J. Pharmacol. 132, 631 (2001) Abstract
Astrocytes in culture produce anandamide and other acylethanolamides: L. Walter, et al.; J. Biol. Chem. 277, 20869 (2002) Abstract
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:
Adenylyl Cyclase Inhibitors • TRPV1 Agonists and Antagonists / Related Products • Fatty Acids
 
 
ALX-480-048 Revised 06-Mar-07
2',3'-Dideoxyadenosine
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Adenosine Derivatives Other Products
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ALX-480-048-M001   1 mg 15.00 USD Add To Cart
ALX-480-048-M005   5 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C10H13N5O2
MW: 235.2
CAS NUMBER: 4097-22-7
MERCK INDEX: 14: 3101
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Inhibitor of adenylate cyclase. Useful tool in antiviral and anticancer studies. Blocks viral reverse transcription from RNA to DNA. Inhibitor of adenosine deaminase.
Product Specific Literature References
Interpretation of the roles of adenylosuccinate lyase and of AMP deaminase in the anti-HIV activity of 2',3'-dideoxyadenosine and 2',3'- dideoxyinosine: V. Nair & T.B. Sells; Biochim. Biophys. Acta 1119, 201 (1992) Abstract
Long-term inhibn. of human T-lymphotropic virus type III/lymphadenopathy-associated virus DNA synthesis and RNA expression in T cells protected by 2',3'-dideoxynucleosides in vitro: H. Mitsuya, et al.; PNAS 84, 2033 (1987) Abstract
Further Categories Containing This Product:
Adenylyl Cyclase Inhibitors • Antiviral Agents Other Products
 
 
ALX-480-049 Revised 03-Jun-08
2',5'-Dideoxyadenosine
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Adenosine Derivatives Other Products
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ALX-480-049-M001   1 mg 30.00 USD Add To Cart
ALX-480-049-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C10H13N5O2
MW: 235.2
CAS NUMBER: 6698-26-6
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water (20mg/ml at 50°C) or DMSO (30mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions are stable for up to 3 months when stored at -20°C.

Product Description
Cell permeable inhibitor of adenylate cyclase (ID50=250µM [1]; inhibition also reported at 1mM [2]). Inhibits growth and causes cell differentiation (1.5µM) in K562 cells [6].
Product Specific Literature References
[1] Role of adenylate cyclase in immunologic release of mediators from rat mast cells: agonist and antagonist effects of purine- and ribose- modified adenosine analogs: S.T. Holgate, et al.; PNAS 77, 6800 (1980) Abstract
[2] Inhibition of adenylate cyclase attenuates adenosine receptor-mediated relaxation in coronary artery: M.H. Sabouni, et al.; J. Pharmacol. Exp. Ther. 259, 508 (1991) Abstract
[3] Direct inhibitory effect of neurotensin on isolated gastric smooth muscle cells of guinea pig via the cyclic GMP system: Y. Chijiiwa, et al.; Digestion 54, 135 (1993) Abstract
[4] Isoproterenol antagonistic effect of 2',5'-dideoxyadenosine in the isolated perfused guinea-pig heart: M. Hartmann & J. Schrader; J. Mol. Cell. Cardiol. 25, 331 (1993) Abstract
[5] Erythroid differentiation and growth inhibition of K562 cells by 2',5'-dideoxyadenosine: synergism with interferon-alpha: K. Ogawa, et al.; Leuk. Res. 19, 749 (1995) Abstract
Further Categories Containing This Product:
Adenylyl Cyclase Inhibitors • Antiviral Agents Other Products
 
 
ALX-480-060 Revised 05-Aug-08
SQ 22,536
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SYNONYMS 9-(Tetrahydro-2-furanyl)-9H-purin-6-amine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Adenylyl Cyclase Inhibitors
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ALX-480-060-M001   1 mg 30.00 USD Add To Cart
ALX-480-060-M005   5 mg 86.00 USD Add To Cart
Product Specification
FORMULA: C9H11N5O
MW: 205.2
CAS NUMBER: 17318-31-9
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water (25mg/ml) or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 3 months at -20°C.

Product Description
Cell permeable adenylate cyclase inhibitor. Blocks PTH-stimulation of adenylate cyclase. Reduces PGE2-induced inhibition of O2- production. Useful as a probe for adenylate cyclase in a variety of receptor systems including prostaglandins and neurotransmitters.
Product Specific Literature References
Inhibition of adenylate cyclase of catfish and rat hepatocyte membranes by 9-(tetrahydro-2-furyl)adenine (SQ 22536): E. Fabbri, et al.; J. Enzym. Inhib. 5, 87 (1991) Abstract
Reversal of synaptic depression by serotonin at Aplysia sensory neuron synapses involves activation of adenylyl cyclase: B.A. Goldsmith & T.W. Abrams; PNAS 88, 9021 (1991) Abstract
Actions of vasopressin and isoprenaline on the ionic transport across the isolated frog skin in the presence and the absence of adenyl cyclase inhibitors MDL12330A and SQ22536: C Lippe & C. Ardizzone; Comp. Biochem. Physiol. 99, 209 (1991) Abstract
cAMP modulates multiple K+ currents, increasing spike duration and excitability in Aplysia sensory neurons: B.A. Goldsmith & T.W. Abrams; PNAS 89, 11481 (1992) Abstract
Roles of intracellular cAMP and protein kinase A in the actions of dopamine and neurotensin on midbrain dopamine neurons: W.X. Shi & B.S. Bunney; J. Neurosci. 12, 2433 (1992) Abstract
Relaxation and inhibition of contractile response to electrical field stimulation by Beraprost sodium in canine airway smooth muscle: J. Tamaoki, et al.; Proaglandins 45, 363 (1993) Abstract
Characterization of the PGE receptor subtype mediating inhibition of superoxide production in human neutrophils: E. Talpain, et al.; Br. J. Pharmacol. 114, 1459 (1995) Abstract
 
 
ALX-350-001 Revised 05-Apr-08
Forskolin
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SYNONYMS Colforsin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-001-M001   1 mg 20.00 USD Add To Cart
ALX-350-001-M005   5 mg 52.00 USD Add To Cart
ALX-350-001-M010   10 mg 85.00 USD Add To Cart
ALX-350-001-M025   25 mg 185.00 USD Add To Cart
ALX-350-001-M050   50 mg 325.00 USD Add To Cart
Product Specification
FORMULA: C22H34O7
MW: 410.5
CAS NUMBER: 66575-29-9
MERCK INDEX: 14: 2476
SOURCE/HOST: Isolated from Coleus forskohlii.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to green crystals.
SOLUBILITY: Soluble in ethyl acetate (10mg/ml), anhydrous DMSO (5mg/ml) or 100% ethanol (6mg/ml). DMSO is the recommended solvent for activation of cAMP.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Stock solutions in DMSO are stable for up to 4 months when stored at +4°C.

Product Description
Activates adenylate cyclase leading to an increase in the intracellular concentration of cAMP. Widely used tool for the investigation of the role of cAMP as a second messenger with a broad range of potential therapeutic applications. Inotropic agent and vasodilator. Induces platelet aggregation. Inhibits ion channels by a mechanism that does not involve cAMP. Non-competitive inhibitor of nicotinic acetylcholine receptors.
Product Specific Literature References
Forskolin: a unique diterpene activator of cyclic AMP-generating systems: K.B. Seamon & J.W. Daly; J. Cyclic Nucleotide Res. 7, 201 (1981), Review Abstract
Forskolin, an activator of adenylate cyclase, increases CA2+-dependent electrical activity induced by glucose in mouse pancreatic B cells: J.C. Henquin, et al.; Endocrinology 112, 2218 (1983) Abstract
Pharmacology and inotropic potential of forskolin in the human heart: M.R. Bristow, et al.; J. Clin. Invest. 74, 212 (1984) Abstract
Forskolin and antidiuretic hormone stimulate a Ca2+-activated K+ channel in cultured kidney cells: S.E. Guggino, et al.; Am. J. Physiol. 249, F448 (1985) Abstract
Use of forskolin to study the relationship between cyclic AMP formation and bone resorption in vitro: U.H. Lerner, et al.; Biochem J. 240, 529 (1986) Abstract
Forskolin: a specific stimulator of adenylyl cyclase or a diterpene with multiple sites of action?: A. Laurenza, et al.; Trends Pharmacol. Sci. 10, 442 (1989), Review Abstract
Effect of forskolin on cytosolic Ca++ level and contraction in vascular smooth muscle: A. Abe & H. Karaki; J. Pharmacol. Exp. Ther. 249, 895 (1989) Abstract
Forskolin acts as a noncompetitive inhibitor of nicotinic acetylcholine receptors: M.L. Aylwin & M.M. White; Mol. Pharmacol. 41, 908 (1992) Abstract
The effect of forskolin on blood flow, platelet metabolism, aggregation and ATP release: J.T. Christenson, et al.; Vasa 24, 56 (1995) Abstract
Forskolin as a tool for examining adenylyl cyclase expression, regulation, and G protein signaling: P.A. Insel & R.S. Ostrom; Cell Mol. Neurobiol. 23, 305 (2003), Review Abstract
Effect of forskolin on the expression of claudin-5 in human trophoblast BeWo cells: M. Harada, et al.; Pharmazie 62, 291 (2007) Abstract
Further Categories Containing This Product:
Adenylyl Cyclase Activators • Ion Channels & Transporters Other Products • Acetylcholine Receptors (Nicotinic) / Related Products • Natural Products for Neurological Research • Natural Products - Nitric Oxide Pathway Modulators
 
 
ALX-350-154 Revised 08-May-08
Tylophorine
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SYNONYMS (-)-R-Tylophorine
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-154-MC05   0.5 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C24H27NO4
MW: 393.5
CAS NUMBER: 111408-21-0
MERCK INDEX: 14: 9831
SOURCE/HOST: Isolated from Tylophora indica.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Phenanthroindolizidine alkaloid which shows antitumor activity. Exhibits potent suppression of inducible nitric oxide synthase (iNOS; NOS II) and cyclooxygenase-2 (COX-2). Enhances the phosphorylation of Akt (protein kinase B; PKB) and thus decreases the expression and phosphorylation levels of c-Jun protein, thereby causing the subsequent inhibition of AP1 activity. Exerts anti-inflammatory effects. Adenylyl cyclase modulator. For the biogenetic precursor see septicine (Prod. No. ALX-350-159)
Product Specific Literature References
Pharmacological investigations of tylophorine, the major alkaloid of Tylophora indica: C. Gopalakrishnan, et al.; Indian J. Med. Res. 69, 513 (1979) Abstract
Effect of tylophorine, a major alkaloid of Tylophora indica, on immunopathological and inflammatory reactions: C. Gopalakrishnan, et al.; Indian J. Med. Res. 71, 940 (1980) Abstract
The responsiveness of leukocyte adenyl cyclase to tylophorine in asthmatic subjects: V. Raina & S. Raina; BBRC 94, 1074 (1980) Abstract
Enantiopure N-Acyldihydropyridones as Synthetic Intermediates: Asymmetric Synthesis of (-)-Septicine and (-)-Tylophorine: D.L. Comins, et al.; J. Org. Chem. 62, 7435 (1997) Abstract
Novel mode of action of tylophorine analogs as antitumor compounds: W. Gao, et al.; Cancer Res. 64, 678 (2004) Abstract; Full Text
Anti-inflammatory mechanisms of phenanthroindolizidine alkaloids: C.W. Yang, et al.; Mol. Pharmacol. 69, 749 (2006) Abstract; Full Text
Total syntheses of the tylophora alkaloids cryptopleurine, (-)-antofine, (-)-tylophorine, and (-)-ficuseptine C: A. Fürstner & J.W. Kennedy; Chemistry 12, 7398 (2006) Abstract
Antitumor agents 251: synthesis, cytotoxic evaluation, and structure-activity relationship studies of phenanthrene-based tylophorine derivatives (PBTs) as a new class of antitumor agents: L. Wei, et al.; Bioorg. Med. Chem. 14, 6560 (2006) Abstract
Antitumor agents 253. Design, synthesis, and antitumor evaluation of novel 9-substituted phenanthrene-based tylophorine derivatives as potential anticancer agents: L. Wei, et al.; J. Med. Chem. 50, 3674 (2007) Abstract
Related Products
Further Categories Containing This Product:
Natural Products - Nitric Oxide Pathway Modulators • Natural Products - Anti-inflammatory Agents • Adenylyl Cyclases Other Products • COX Inhibitors • Alkaloids
 
 
ALX-350-159 Revised 08-May-08
Septicine
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SYNONYMS 6,7-Bis(3,4-dimethoxyphenyl)-1,2,3,5,8,8a-hexahydroindolizine
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-159-M001   1 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C24H29NO4
MW: 395.5
CAS NUMBER: 42922-10-1
SOURCE/HOST: Isolated from Tylophora asthmatica.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow crystalline solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
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Indolizidine alkaloid. Antitumor compound. Biogenetic precursor of the alkaloid tylophorine (Prod. No. ALX-350-154).