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A0232
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Alfuzosin hydrochloride ≥98% (HPLC), solid
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Alfuzosin hydrochloride is an alpha-adrenergic blocker used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
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A1862
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Alpidem ≥98% (HPLC), powder
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Alpidem is a potent antagonist of peripheral benzodiazepine receptor (PBR) that is located on the outer mitochondrial membrane and interacts with the mitochondrial permeability transition (MPT) pore. Alpidem is an anxiolytic drug from the imidazopyridine family. Alpidem acts selectively on the α3 receptor subtype and to a lesser extent at the α1 subtype (Kd of 0.33nM and 1.67nM respectively), of the benzodiazepine receptor.
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A6226
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AM251 >98% (HPLC), solid
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AM251 is a CB1 cannabinoid receptor antagonist.
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mouse ... Cnr1(12801), Cnr2(12802) rat ... Cnr1(25248)
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A5602
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AMD3100 octahydrochloride hydrate ≥97% (NMR), solid
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AMD3100 is a highly specific chemokine receptor CXCR4 antagonist.
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A2729
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Amisulpride ≥98% (HPLC), solid
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Amisulpride is a highly selective D2/D3 dopamine receptor antagonist and atypical antipsychotic.
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C7495
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Clofarabine ≥98% (HPLC)
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Clofarabine is a purine nucleoside antimetabolite. Clofarabine is toxic to nondividing lymphocytes and monocytes.
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SML0004
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(S)-(+)-Clopidogrel hydrogensulfate ≥98% (HPLC)
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(S)-(+)-Clopidogrel hydrogen sulfate is an antithrombotic antiplatelet agent. It specifically and irreversibly inhibits the Purinoceptor P2Y12 subtype which inhibits ADP-induced platelet aggregation. (S)-(+)-Clopidogrel hydrogen sulfate is the active isomer.
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C0614
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(±) Clopidogrel hydrogensulfate ≥98% (HPLC), powder
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Inhibits ADP-induced platelet aggregation; anti-thrombotic drug.
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C0399
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Cromolyn sodium salt ≥95%
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Cromolyn blocks the release of histamine and other pro-inflammatory mediators from mast cells.
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D8399
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Danazol ≥98%
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Danazol is a weak androgen; anterior pituitary suppressant.
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M003
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R-(−)-Deprenyl hydrochloride powder, ≥98% (HPLC)
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Selective MAO-B inhibitor; anti-Parkinsonian agent.
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human ... MAOB(4129)
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D3900
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Desipramine hydrochloride ≥98% (TLC), powder
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Tricyclic antidepressant that is a more potent inhibitor of the norepinephrine transporter (Ki = 4 nM) than the serotonin transporter (Ki = 61 nM).
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D9571
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Dolasetron mesylate hydrate ≥98% (HPLC), powder
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Dolasetron mesylate hydrate is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors.
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D3775
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Doxylamine succinate salt
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H1 histamine receptor antagonist; hypnotic.
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human ... HRH1(3269)
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D9696
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Dronedarone hydrochloride ≥98% (HPLC), powder
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Dronedarone is a Class III antiarrhythmic and a multi-channel blocker for atrial fibrillation. It blocks potassium, sodium, and calcium channels and also exhibits antiadrenergic properties.
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E2031
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Eliprodil ≥98% (HPLC), solid
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NR2B selective NMDA glutamate receptor antagonist which appears to target the "polyamine site" on the NMDA receptor, setting it apart from other NR2B receptor antagonists. Possesses neuroprotective effects in models of ischemia, but prolongs the QT interval in patients; currently under investigation for acute and chronic pain.
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human ... GRIN2B(2904) rat ... Adra1a(29412)
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F9427
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Fexofenadine hydrochloride >98% (HPLC)
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Fexofenadine is a non-sedating H1 histamine receptor antagonist.
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human ... HRH1(3269)
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F4381
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Furosemide
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"High ceiling" diuretic that strongly affects renal tubular action by increasing renal blood flow; antihypertensive. Inhibits ion co-transport in the kidney.
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human ... ALB(213), CYP1A2(1544), SLC12A1(6557)
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G2295
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Glimepiride ≥98% (HPLC), solid
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Glimepiride is a potent blocker of cardiac KATP channels activated by pinacidil with an IC50 of 6.8 nM.
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human ... KCNJ1(3758)
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I2286
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Irbesartan ≥98% (HPLC), powder
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Irbesartan is an angiotensin II type 1 (AT1) receptor antagonist with anti-hypertensive activity.
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I3639
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Isoetharine mesylate salt
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β-Adrenergic receptor agonist; bronchodilator.
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human ... ADRB1(153), ADRB2(154), ADRB3(155)
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I5627
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Isoprenaline hydrochloride
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β-adrenoceptor agonist; increases cytosolic cAMP.
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human ... ADRB1(153), ADRB2(154), ADRB3(155)
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I2760
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(−)-Isoproterenol (+)-bitartrate salt powder
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β-Adrenoceptor agonist; increases cytosolic cAMP.
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human ... ADRB1(153), ADRB2(154), ADRB3(155)
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SML0115
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MDL 11939 ≥98% (HPLC)
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MDL 11,939 is a potent, selective and orally active 5-HT2 receptor antagonist (ASTAR). Ki values values are in the low nanomolar range for 5-HT2A with over 100-fold selectivity over 5-HT2C receptors and low or no affinity for non-5-HT2 receptors or transporters.
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M3142
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Meperidine hydrochloride
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Phenylpiperidine analgesic; sedative; μ opioid receptor agonist with greater κ opioid receptor agonist activity than morphine.
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M4659
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Milrinone ≥97% (TLC), powder
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Phosphodiesterase type III inhibitor; cAMP-specific, cGMP-inhibitable; potent cardiotonic, positive inotropic vasodilator.
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human ... PDE3A(5139), PDE3B(5140), PDE4B(5142), PDE5A(8654), PTPRA(5786) rat ... Pde3a(50678)
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N4382
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Nalidixic acid sodium salt powder
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Nalidixic acid sodium salt is an inhibitor of bacterial DNA polymerase (DNA gyrase) and avian myeloblastoma virus reverse transcriptase. Inhibits nucleic acid and protein synthesis in Saccharomyces cerevisiae.1
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N8534
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Nilutamide solid
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Nilutamide is an antiandrogen used in the treatment of prostate cancer.
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human ... AR(367)
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O9512
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Oxaliplatin solid
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Oxaliplatin is an anti-tumor agent with activity against colorectal cancer; cytotoxicity follows the formation of adducts with DNA.
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P134
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(−)-Pentazocine ≥98% (HPLC)
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P127
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(+)-Pentazocine solid
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σ receptor agonist; active enantiomer of pentazocine.
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human ... EBP(10682) rat ... Chrm1(25229), Chrm2(81645), Drd2(24318), Oprm1(25601)
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P1784
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Pentoxifylline solid
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Phosphodiesterase inhibitor; inhibits synthesis of tumor necrosis factor α (TNF-α).
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human ... ADORA2B(136), LITAF(9516), PDE4B(5142), TNF(7124) rat ... Tnf(24835)
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R0404
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Ramipril ≥98% (HPLC)
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Angiotensin converting enzyme (ACE) inhibitor.
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human ... ACE(1636)
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R116
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Riluzole solid
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Glutamate release inhibitor; anticonvulsant
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rat ... Scnn1g(24768)
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SML0015
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SR 142948A ≥98% (HPLC)
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SR 142948A is a non-peptide Neurotensin receptor antagonist
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SML0179
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SR 27897 hydrate ≥98% (HPLC)
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SR 27897 is a potent, selective antagonist of the Cholecystokinin (CCK) receptor CCK1. SR-27897 blocks the elevation of leptin levels in the CNS following injection of CCK-8 peptide, and causes an increase in food intake in rats.
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S7201
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SR-46349 hemifumarate salt ≥98% (HPLC)
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ASTAR (Antagonist of Serotonin 5HT2A Receptors).
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S5701
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SR 49059 ≥97% (HPLC)
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SR 49059 is a potent and selective Arginine Vasopressin (AVP) V1a-receptor antagonist. AVP is a hormone that plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). There are three AVP receptor subtypes V1a, V1b, and V2. All belong to the large rhodopsin-like G-protein-coupled receptor family. V(1a) antagonists improve water balance and cardiac hypertrophy in CHF and might be beneficial for the treatment of water retention and cardiac remodeling in CHF. SR 49059 has also shown initial positive results in the treatment of Raynaud′s disease, dysmenorrhoea, and tocolysis.
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S8688
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SR 59230A ≥98% (HPLC), powder
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SR 59230A is a β3-adrenoceptor antagonist.
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human ... ADRB3(155)
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S7771
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(S)-(−)-Sulpiride ≥98% (titration)
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D2 dopamine receptor antagonist; antipsychotic.
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human ... DRD2(1813), DRD3(1814) rat ... Adra1a(29412), Drd2(24318), Drd3(29238), Htr1a(24473), Htr2a(29595)
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S8010
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(±)-Sulpiride
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D2 dopamine receptor antagonist; antipsychotic.
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human ... CA1(759), CA2(760), CA4(762), CA5A(763), CA5B(11238), CA9(768), DRD2(1813)
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T9652
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Terfenadine
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Non-sedating second generation H1 histamine receptor antagonist. Mainly metabolized by Cyp3A4, 5, 7. Inhibits CYP2C8.
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human ... ABCB1(5243), CYP2C8(1558), CYP3A4(1576), HRH1(3269), IL4(3565), IL5(3567), KCNH1(3756), KCNH2(3757) mouse ... Abcb1a(18671), Abcb1b(18669) rat ... Hrh1(24448)
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T4580
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Tiludronate disodium salt hydrate ≥98% (HPLC)
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Tiludronate is a bisphosphonate bone resorption inhibitor. Tiludronate inhibits protein-tyrosine-phosphatase, leading to detachment of osteoclasts from the bone surface. It also inhibits the osteoclastic proton pump and is used to treat Paget′s disease.
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T7455
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Tolvaptan ≥98% (HPLC), powder
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Tolvaptan (OPC 41061) is a potent, orally active non-peptide vasopressin V2 selective antagonist. IC50 = 3 nM at the rat V2 receptor; 29 times more selective for the V2 than for V1a. Tolvaptan has also been shown to inhibit the development of polycystic kidney disease in several animal models.
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V3640
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Valpromide ≥97% (NMR)
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Valpromide (VPD) is a derivative of valproic acid (VPA) and is used as an antiepileptic drug. It is hydrolyzed quickly to VPA in vivo, but has intrinsic anticonvulsant activity.
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X4879
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Xaliproden hydrochloride ≥97% (HPLC), solid
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5-HT1A serotonin receptor agonist; neuroprotectant
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X3129
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XRP44X ≥98% (HPLC)
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XRP44X is a Ras-Net (Elk-3) pathway inhibitor; tubulin polymerization inhibitor Colchicine binding site.
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Z103
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Zolpidem ≥98% (HPLC), solid
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Potent and selective agonist for the benzodiazepine receptor associated with the GABAA receptor; hypnotic.
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human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA5(2558), GABRA6(2559) rat ... Gabra1(29705), Gabra2(29706), Gabra5(29707), Tspo(24230)
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