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A8423 Amiodarone hydrochloride ≥98% Non-selective ion channel blocker with broad fungicidal activity. Amiodarone induces an immediate influx of Ca2+ in Saccharomyces cerevisiae, followed by mitochondrial fragmentation and cell death.
 
A129 Amoxapine Tricyclic antidepressant; inhibits uptake of norepinephrine; inhibits 5-HT2 serotonergic receptors.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
C5976 CL 316,243 hydrate ≥98% (HPLC), powder CL 316,243 is a β3 adrenoceptor agonist; anti-obesity agent.
human ... ADRB3(155)
C9498 CL-82198 ≥98% (HPLC), powder CL-82198 is a selective inhibitor of MMP-13 that displays no activity at MMP-1, MMP-9 or TACE. It is also a selective S1′ pocket binder, binding within the entire S1′ pocket of MMP-13, docking with the morpholine ring adjacent to the catalytic zinc atom without zinc chelation.
 
C6643 Clofibrate liquid Peroxisome proliferator-activated receptor-α (PPARα) agonist. Antihyperlipoproteinemic believed to act by inhibiting cholesterol biosynthesis.
human ... PPARA(5465)
mouse ... Ppara(19013)
C2499 CP-339818 ≥98% (HPLC) CP-338818 blocks both Kv1.3 and Kv1.4. Kv1.3 is expressed in brain and in effector memory T (Tem) cells, and Kv1.4 is expressed in brain cells. Kv1.3 and Kv1.4 are members of the Shaker family of voltage-gated potassium channels. Both channels are involved in setting the membrane potential of neurons. In addition, Kv1.3 maintains the membrane potential for T memory cells and is up-regulated upon T cell activation, contributing to multiple immune processes and disorders. Blockers of Kv1.3 have long been sought for therapeutic benefit, and they are also valuable tools for studying the immune system. CP-339818 is valuable for immune system studies, where the absence of Kv1.4 makes it functionally selective for Kv1.3, and it has shown suppression of T cell activation. CP-339818 is also valuable for the study of Kv1.4 function.
 
D2069 Desvenlafaxine hydrochloride ≥98% (HPLC), powder Desvenlafaxine hydrochloride is a dual SERT/NET reuptake inhibitor. It is a major active metabolite of venlafaxine (#542); brain penetrant; Ki = 40 nM and 122 nM for hSERT and hNET, respectively (weak binding at the hDAT). Inhibition of [3H]5-HT or [3H]NE uptake for the hSERT or hNET produced IC50 values of 47 and 531 nM.
 
SML0206 EAA-090 ≥98% (HPLC) EAA-090 inhibits the binding of ligands to glutamate receptors and blocks NMDA-induced currents. It is neuroprotective against glutamate and ischemia-induced toxicity.
EAA-090 is a potent NMDA receptor antagonist with neuroprotective properties. In isoflurane-anesthetized dogs, EAA-090 reduces the minimum alveolar concentration (MAC) of isoflurane and increases systolic, mean, and diastolic arterial blood pressure.
 
E0516 Etodolac Non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX-1 and COX-2.
human ... PTGS1(5742), PTGS2(5743)
G110 Guanabenz acetate salt powder Centrally acting α2 adrenoceptor agonist; I2 imidazoline binding site ligand; antihypertensive.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
I2909 Indoramin hydrochloride ≥98% (HPLC), solid α1-adrenoceptor antagonist.
 
M2017 Mazindol ≥98% (TLC), powder Anorectic agent; inhibits the dopamine, norepinephrine and serotonin transporters with Kis of 27.6 nM, 3.2 nM, and 153 nM, respectively.
human ... SLC6A2(6530), SLC6A3(6531), SLC6A4(6532)
rat ... Htr1a(24473), Htr2a(29595), Slc6a3(24898), Slc6a4(25553)
M2824 Meptazinol hydrochloride Meptazinol entered the human pharmaceutical market as a racemic mixture in the 1980s for use as an analgesic. Its pharmacology is not completely understood; however, its analgesic properties are mostly due to its partial agonism at the mu1 opioid receptor. Due to its partial agonism, Meptazinol antagonizes morphine dependence in vivo. Its advantage over other opiates is its reduced capacity to cause addition and respiratory depression, also due to its intrinsic activity as a partial agonist. Meptazinol has been found to have additional activity as an acetylcholinesterase (AChE) inhibitor, particularly in its (-) enantiomeric form, which may partially explain its analgesic properties. AChE inhibitors are used to treat Alzheimer′s disease, providing additional interest in this compound.
 
P4651 Promethazine hydrochloride H1 histamine receptor antagonist; CNS depressant; anticholinergic.
human ... HRH1(3269)
Q3625 Quinidine anhydrous Class IA antiarrhythmic; potassium channel blocker.
human ... ABCB1(5243), CYP2D6(1565), CYP3A4(1576), KCNH1(3756)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Cyp2d1(266684), Cyp2d2(25053), Cyp2d3(24303), Cyp2d4v1(171522)
U6010 UPF-1069 ≥98% (HPLC), powder UPF-1069 is a PARP inhibitor with modest selectivity for PARP-2 (0.3 uM) over PARP-2 (8.0 uM).
 
V7264 Venlafaxine hydrochloride ≥98% (HPLC), powder Venlafaxine is an antidepressant. The mechanism of the antidepresant action of venlafaxine in humans is associated with its potentiation of neurotransmitter activity in the CNS. Venlafaxine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and weak inhibitor of dopamine reuptake. Venlafaxine has no significant activity for muscarinic, histaminergic, or α-1 adrenergic receptors in vitro. Venlafaxine does not possess MAO inhibitor activity.
 
W1895 WAY-100135 ≥98% (HPLC) WAY-100135 is a potent, selective 5-HT1A receptor antagonist (IC50 = 15 nM). It is selective over 5-HT1B, 1C, 2,α1, α2 and D2 receptors (IC50 > 1000 nM).
 
W0270 WAY 161503 hydrochloride ≥98% (HPLC) The 5-HT2C receptors have been implicated in conditions including obesity, anxiety, depression, OCD, schizophrenia, migraine, nociception and erectile dysfunction.
 
W1520 WAY-200070 ≥98% (HPLC) Potent, selective estrogen receptor-beta (ER-β) agonist (IC50 2.3 nM vs 155 nM for ER-α) with anxiolytic-like and antidepressant-like effects.
 
SML0081 Zacopride hydrochloride hydrate ≥98% (HPLC) Zacopride is a sub-nanomolar antagonist of the serotonin 5-HT3 receptor that also displays agonist-like activity against 5-HT4 receptors. It is a potent anxiolytic in animal models, and also has strong antiemetic effects, and also increases aldosterone levels via activation of 5-HT4 receptor in the adrenal glands.