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A9736 A-438079 hydrochloride hydrate ≥98% (HPLC) A-438079 hydrochloride hydrate is a selective P2X7 purinoceptor antagonist in both human and rat with minimal activity at 75 different G-protein-coupled receptors, enzymes, transporters, and ion channels tested.
 
SML0085 A-967079 ≥98% (HPLC) A-967079 is a potent and selective antagonist of Transient Receptor Potential Anykrin 1 (TRPA1) with IC50′s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and minimal or no activity at other TRP channels or G-protein-coupled receptors, enzymes, transporters, and ion channels out of 89 tested. A-967079 blocks TRPA1 activation in human and rat cell lines and has been shown to reduce the responses of wide dynamic range (WDR) and nociceptive specific (NS) neurons to high-intensity mechanical stimulation.
 
A2846 A-134974 dihydrochloride hydrate ≥98% (HPLC), solid A-134974 is a novel and selective adenosine kinase (AK) inhibitor with IC50 = 60 pM. Systemic A-134974 (i.p.) dose dependently reduced hyperalgesia (ED50= 1 μmol/kg) and at higher doses, reduced locomotor activity (ED50 = 16 μmol/kg). Administration of A-134974 intrathecally (i.t.) was more potent (ED50= 6 nmol) at producing antihyperalgesia than delivering the compound by intracerebralventricular (ED50 = 100 nmol, i.c.v.) or intraplantar (ED50 >300 nmol) routes. In contrast, i.c.v. administration of A-134974 was more effective in reducing locomotor activity than i.t. administration (ED50 values were 1 and >100 nmol, respectively). Increasing the pretreatment time for i.t.-delivered A-134974 caused a greater reduction in locomotor activity (ED50= 10 nmol). This was due to diffusion of A-134974 (i.t.) to supraspinal sites. These data demonstrate that the novel AK inhibitor A-134974 potently reduces thermal hyperalgesia primarily through interactions with spinal sites, whereas its ability to depress locomotor activity is predominantly mediated by supraspinal sites.
 
A6351 A-315456 >98% (HPLC), solid Selective α1D-adrenoceptor antagonist.
human ... ADRA1D(146)
A2979 A-317491 sodium salt hydrate ≥98% (HPLC), powder Novel P2X3 and P2X2/3 receptor antagonist
 
A7730 A-331440 dihydrochloride ≥98% (HPLC), solid A-331440 dihydrochloride is a non-imidazole H3 histamine receptor antagonist. Presynaptic histamine H(3) receptors regulate release of histamine and other neurotransmitters, and histamine H(3) receptor antagonists enhance neurotransmitter release. A-331440 is a histamine H(3) receptor antagonist, which binds potently and selectively to both human and rat histamine H(3) receptors (K(i)=25 nM). Mice on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. Both data shows that the histamine H(3) receptor antagonist, A-331440, has potential as an antiobesity agent.
 
A3104 A-331440 L-tartrate hydrate ≥98% (HPLC), solid Histamine affects homeostatic mechanisms, including food and water consumption, by acting on central nervous system (CNS) receptors. Presynaptic histamine H3 receptors regulate release of histamine and other neurotransmitters, and histamine H3 receptor antagonists enhance neurotransmitter release. A-331440 [4′-[3-(3(R)-(dimethylami<WBR>no)-pyrrolidin-1-yl)-propoxy]-biphenyl-4-carbonitrile] is a histamine H3 receptor antagonist which binds potently and selectively to both human and rat histamine H3 receptors (Ki<=25 nM). Mice were stabilized on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. These data show that the histamine H3 receptor antagonist, A-331440, has potential as an antiobesity agent.
 
A6604 A-350619 hydrochloride ≥98% (HPLC), solid A-350619 modulates catalytic properties of soluble guanylyl cyclase; it increases Vmas from 0.1 to 14.5 μmol/min/mg and lowers Km from 300 to 50 μM. A-350619 activation of soluble guanylate cyclase depends on the presence of a heme moiety in the enzyme and synergy with nitric oxide.
 
A5861 A-61603 hydrate ≥98% (HPLC) A-61603 is an α1A agonist. In radioligand binding assays, A-61603 was at least 35-fold more potent at α1A receptors than at α1b or α1d sites. In fibroblast cells transfected with α1a receptors, A-61603 more potently stimulated phosphoinositide hydrolysis than norepinephrine, and was antagonized by prazosin. A-61603 is less potent in cells transfected with α1b or α1d receptors. It is a potent agonist at α1A receptors in rat vas deferens (200- to 300-fold more potent than norepinephrine or phenylephrine, respectively) and in isolated canine prostate strips (130- to 165-fold more potent than norepinephrine or phenylephrine, respectively). In contrast, it is only 40-fold more potent than phenylephrine at α1B sites in rat spleen and 35-fold less potent at rat aortic, α1D sites. A-61603 induces a pressor response in conscious rats at doses 50- to 100-fold lower than phenylephrine.
 
A8852 A-68930 hydrochloride ≥98% (HPLC), powder Selective D1 dopamine receptor agonist
 
A3109 A-803467 ≥98% (HPLC) A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.
 
A1471 A-85783 Potent and selective platelet-activating factor (PAF) receptor antagonist.
 
A6476 ABT-418 hydrochloride powder, ≥98% (HPLC) Neuronal nicotinic acetylcholine receptor agonist with cognition enhancing and anxiolytic activities.
 
A9227 ABT-491 hydrochloride ≥98% (HPLC) Highly potent, selective and orally active platelet-activating factor (PAF) receptor antagonist. Ki = 0.6 nM in human platelets.
 
A5111 ABT-724 trihydrochloride ≥98% (HPLC)    
SML0131 ABT-751 hydrochloride ≥98% (HPLC) ABT-751 is an orally bioavailable vascular disrupting agaent (VDA) with a broad spectrum of antitumor activity. It binds to the colchicine binding site on beta-tubulin and inhibits polymerization of microtubules.
 
B5311 Biperiden hydrochloride ≥98% (HPLC), powder Biperiden hydrochloride is antiparkinsonian; non-selective muscarinic receptor antagonist. It is used for the adjunctive treatment of all forms of Parkinson′s Disease (postencephalitic, idiopathic, and arteriosclerotic); also commonly used to improve parkinsonian signs and symptoms related to antipsychotic drug therapy. LD50 in rats 750 mg/kg; in dogs 340 mg/kg.
 
SML0095 Conessine ≥97% (HPLC) Conessine is a plant steroid alkaloid that acts as a potent and specific antagonist of histamine H3 receptors (Ki = 5.37 and 24.5 nM for human and rat receptors, respectively). Conessine is 1860-fold selective for H3 over H4 and does not bind to H1 or H2 receptors. The molecule also binds to the human α2C4 adrenergic receptor (pKi = 7.98).
 
E2535 Eprosartan mesylate ≥98% (HPLC) Angiotensin II type 1 (AT1) receptor antagonist; anti-hypertensive.
 
E3638 Estazolam Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site.
 
F6020 Fenofibrate ≥99%, powder PPARα agonist; lipid regulating drug. Increases high density lipoprotein levels by reducing cholesteryl ester transfer protein expression.
human ... PPARA(5465)
F4303 Fiduxosin hydrochloride >98% (HPLC), solid α1-Adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
H4516 Hydrocodone (+)-bitartrate salt μ opioid receptor agonist; narcotic analgesic and antitussive.
 
SML0033 Itopride hydrochloride ≥98% (HPLC) Itopride is an acetylcholinesterase (AChE) inhibitor and D2 dopamine receptor antagonist. Itopride is used as a gastroprokinetic agent.
 
M2147 Mevinolin from Aspergillus sp. ≥98% (HPLC) Lovastatin is a cholesterol lowering drug and competitive inhibitor of HMG-CoA reductase, a rate limiting enzyme in cholesterol synthesis. Blocks the production of mevalonate, a critical compound in the production of cholesterol and isoprenoids. This product is a substrate of Pgp and CYP3A. It increases cellular resistance to anticancer agents such as doxorubicin and induces apoptosis in myeloma cells. The roles of Pgp and CYP3A, possible connection between drug resistance, regulation of the mevalonate pathway, and iosprenylation of signaling proteins in these observations remain to be resolved. The product induces apoptosis in numerous cancer cell lines perhaps, in part, by inhibiting the isoprenylation of Rho family GTPases. It causes cell cycle arrest in G1 and G2/M phases.
human ... HMGCR(3156)
rat ... Hmgcr(25675)
N4396 Nalbuphine hydrochloride hydrate ≥98% (HPLC) Partial agonist for μ and κ opioid receptors.
human ... OPRK1(4986), OPRM1(4988)
P0130 Progesterone ≥99% Induces maturation and secretory activity of the uterine endothelium; suppresses ovulation. Progesterone is implicated in the etiology of breast cancer.
human ... ABCB1(5243), AR(367), CYP2C9(1559), EBP(10682), ESR1(2099), ESR2(2100), NR3C1(2908), NR3C2(4306), PGR(5241), SERPINA6(866)
mouse ... Esr1(13982)
rat ... Ar(24208), Nr3c1(24413), Pgr(25154)
P4670 Propafenone hydrochloride Blocks hKv1.5 and ATP-sensitive K+ channels; class 1C antiarrhythmic agent that is also an antagonist at β adrenergic receptors.
human ... ABCB1(5243), ADRB1(153), ADRB2(154), ADRB3(155), CYP1A2(1544)
S8072 Sertindole ≥97.5% (HPLC) Sertindole is a 5-HT2 serotonin and D2 dopamine receptor antagonist and antipsychotic.
Sertindole readily passes the blood-brain barrier and is metabolized into compounds that show greater affinity for 5-HT2 receptors and less for D2 receptors. It is an effective treatment agent for schizophrenia as it improves cognitive impairment.1 Sertindole also acts as antagonist to human cardiac potassium channel, HERG and produces prolonged QT interval.2
 
S9944 Sibutramine hydrochloride monohydrate ≥98% (HPLC), solid Sibutramine is a serotonin and noradrenaline reuptake inhibitor (SNRI). It is an antiobesity drug, which decreases calorie intake and increases energy expanditure. Sibutramine antagonizes MPTP-induced dopamine depletion in mouse brain.
 
T4680 Terazosin hydrochloride ≥98% (TLC), powder α1-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
T1019 (±)-Thiopental Thiopental is an anesthetic that decreases cerebral metabolic rate without altering the blood flow or oxygen consumption.
 
T4827 Trandolapril ≥98% (HPLC), white powder Studies have reported that trandolapril inhibits atherosclerosis1 and decreases the occurrence of atrial fibrillation2.
Trandolapril is an ACE inhibitor. Trandolapril differs from other ACE inhibitors in that it has a longer biological half-life and a high degree of lipophilicity.
 
T6376 Triamcinolone Triamcinolone is a synthetic glucocorticoid agonist; induces gene expression and apoptosis; inhibits prostaglandin synthesis; impairs tumor necrosis factor (TNF)-α-induced degradation of κB-α; potentiates the differentiation-inducing effects of bone morphogenetic proteins (BMP-2, -4, -6).
human ... PTGS2(5743)
P4543 Valproic acid sodium salt ≥98% Anti-convulsant that also has efficacy as a mood stabilizer in bipolar disorder.
 
Z4277 Zileuton ≥98% (HPLC) Zileuton is an anti-asthmatic, an inhibitor of 5-lipoxygenase; the initial enzyme in the biosynthesis of leukotrienes from arachidonic acid.