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• Bioactive Molecules • Building Blocks • Intermediates www.ChemScene.com Orally Active Compound Library (96-well) Product Details: Catalog Number: CS-L061 Formulation: A collection of 2244 orally active compounds supplied as pre-dissolved Solutions or Solid Container: 96- or 384-well Plate with Peelable Foil Seal; 96-well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode Storage: -80°C Shipping: Blue ice Packaging: Inert gas Plate layout: CS-L061-1 1 2 3 4 5 6 7 8 9 10 11 12 a Empty Vonoprazan Mivebresib AZD0156 BAY-876 Tomivosertib PQR620 NPS-2143 R547 PAP-1 Delpazolid Empty Varenicline b Empty Varenicline (Hydrochlorid Varenicline A-205804 CI-1044 KW-8232 GSK583 Quiflapon MRK-016 Diroximel Empty e) (Tartrate) fumarate SHP099 c Empty A 922500 SHP099 (hydrochlorid Nevanimibe Pactimibe Pactimibe GNF-6231 MLi-2 KDM5-IN-1 PACMA 31 Empty e) hydrochloride (sulfate) Rilmenidine d Empty Cadazolid Treprostinil GSK3179106 Esaxerenone (hemifumarat Rilmenidine Fisogatinib BP-1-102 Avadomide Aprepitant Empty e) (phosphate) Cl-amidine AZD5153 (6- e Empty Maropitant Abscisic acid (hydrochlorid BGG463 WNK463 Ticagrelor Axitinib Hydroxy-2- CGS 15943 Pipamperone Empty e) naphthoic Setogepram Teglarinad f Empty Y-27632 GSK2193874 Lanabecestat CXD101 Ritlecitinib YL0919 PCC0208009 (sodium salt) (chloride) Futibatinib Empty TAK-659 g Empty NCB-0846 GS-444217 (hydrochlorid Navitoclax ABX464 Zibotentan Simurosertib (R)- CEP-40783 MK-8617 Empty e) Simurosertib Choline JNJ- h Empty CCT251236 (bitartrate) Sarcosine Brensocatib AS-605240 PF-06840003 EED226 Filibuvir 39758979 Vorapaxar Empty Plate layout: CS-L061-2 1 2 3 4 5 6 7 8 9 10 11 12 S1p receptor Cyclo(his-pro) Coenzyme a Empty Asenapine Silodosin agonist 1 Vadadustat Iberdomide FK614 PF-01247324 (TFA) Q9 Ralfinamide Empty GKT136901 b Empty (±)- Zanubrutinib Emodepside Fenobam GZD856 GKT136901 (hydrochlorid MRX-2843 Linrodostat Avapritinib Empty Zanubrutinib (formic) e) Elimusertib Nilotinib c Empty GDC-0077 JNJ- Elimusertib (hydrochlorid Roblitinib Darovasertib Bosutinib Gefapixant Nilotinib (monohydroc Empty 64619178 e) hloride Tecalcet NPS-2143 ZM223 d Empty MSC2530818 Olaparib Ilaprazole (Hydrochlorid (hydrochlorid GSK2982772 TM5441 Ziritaxestat NE 52-QQ57 (hydrochlorid Empty e) e) e) Dasatinib e Empty RG7800 RG7800 MLN8054 CP671305 Dasatinib (hydrochlorid Anle138b BMS-309403 BMS-309403 ASP7663 Empty hydrochloride e) (sodium) Ruboxistaurin CB-1158 f Empty Linsitinib DS-1040 BMS-816336 Prostaglandin (hydrochlorid CPI-444 (dihydrochlori Navarixin AZD4635 Rucaparib Empty (Tosylate) E2 e) de) (Camsylate) Sorafenib SSTR5 g Empty Sorafenib SB756050 (Tosylate) RG3039 antagonist 1 OSI-930 Cediranib Apimostinel Amuvatinib SR 57227A Empty Masitinib h Empty NS13001 Pazopanib Masitinib (mesylate) BIIB021 Everolimus Rapamycin Vorinostat Ixabepilone Panobinostat Empty Plate layout: CS-L061-3 1 2 3 4 5 6 7 8 9 10 11 12 Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA Tel: 732-484-9848 Fax: 888-484-5008 Email: [email protected] • Bioactive Molecules • Building Blocks • Intermediates www.ChemScene.com NVP- a Empty Belinostat Bortezomib Saracatinib Telaprevir Boceprevir Danoprevir Simeprevir ADW742 PD0325901 Sunitinib Empty Edoxaban Dabigatran b Empty Vandetanib Afatinib Afatinib BMS-536924 Edoxaban Edoxaban (tosylate Betrixaban Dabigatran etexilate Empty (dimaleate) (tosylate) monohydrate) etexilate (mesylate) MK-3207 c Empty Linagliptin Saxagliptin Narlaprevir TC-G-1008 MK-3207 Gusacitinib (Hydrochlorid LY3200882 Repotrectinib CLP290 Empty e) d Empty E7046 Fananserin SB 243213 SB-200646A ROCK-IN-2 Doramapimod Falnidamol Desidustat RSVA405 TC ASK 10 Empty Regorafenib Fasudil e Empty Toceranib ML218 Toceranib Regorafenib (monohydrate BMS-690514 L-006235 Proglumide Stiripentol (Hydrochlorid Empty (phosphate) ) (sodium) e) Raltegravir MK-2206 IPN60090 Samuraciclib f Empty Raclopride Sotrastaurin Raltegravir (potassium (dihydrochlori IPN60090 (dihydrochlori PTC-028 ROC-325 (hydrochlorid Empty salt) de) de) e) Samuraciclib g Empty (trihydrochlori Seclidemstat Ensartinib Sutezolid Linezolid Emricasan ACY-957 Losmapimod IDH-305 Cintirorgon Empty de) hydrochloride Fedratinib h Empty Vorasidenib Pamiparib QC6352 Pamapimod Talmapimod Theliatinib Pocapavir Ki20227 Fedratinib (hydrochlorid Empty e hydrate) Plate layout: CS-L061-4 1 2 3 4 5 6 7 8 9 10 11 12 Dapagliflozin Empty AZD-8055 OSI-027 HPGDS Vismodegib Balapiravir Capsaicin Capsaicin Dapagliflozin ((2S)-1,2- Canagliflozin Empty a inhibitor 1 (purity>99%) propanediol, Daclatasvir b Empty Ixazomib Ixazomib Delanzomib TAK-715 (dihydrochlori Daclatasvir LY2811376 Fasiglifam Cobicistat Lexibulin Empty citrate de) Secoisolaricir Pomaglumeta c Empty esinol d methionil (Z)-Orantinib Darapladib GSK1904529 Telatinib GSK-626616 ARRY-380 Tegobuvir Ketanserin Empty diglucoside (hydrochlorid A (analog ) Sarpogrelate Y-27632 d Empty Ketanserin (hydrochlorid SRX246 Ponesimod Nevirapine Delavirdine Efavirenz Rilpivirine Flurbiprofen (dihydrochlori Empty (tartrate) e) (mesylate) de) Valproic acid Alagebrium Rucaparib e Empty Valproic acid (sodium salt) 5-Azacytidine RO-28-1675 GSK356278 Zamicastat Liarozole chloride Dazoxiben (phosphate) Empty Niraparib f Empty Rucaparib Niraparib (hydrochlorid Niraparib T0901317 SB-705498 Arimoclomol Rentiapril Neticonazole Palosuran Empty e) (tosylate) (maleate) Palosuran Epertinib g Empty (hydrochlorid Voclosporin Furprofen SY-640 Ningetinib Ningetinib PF-03463275 Selamectin PQR530 (hydrochlorid Empty e) Tosylate e) Asimadoline h Empty Tetrahydrobio (hydrochlorid AX-024 AX-024 SC-26196 PD-166793 Abrocitinib E6130 AS1269574 SIB-1553A Empty pterin e) hydrochloride Plate layout: CS-L061-5 1 2 3 4 5 6 7 8 9 10 11 12 Ganaplacide a Empty L 152804 PAT-505 Ximelagatran Cilomilast Ritanserin Hyaluronidas GNE-6776 Mirogabalin Ferric maltol (hydrochlorid Empty e besylate e) Facinicline Almorexant CP-100356 b Empty CCT 137690 Almorexant (hydrochlorid (hydrochlorid GNE-493 Pemetrexed Pemetrexed (R)- PF-06471553 (hydrochlorid Empty e) e) (disodium) Bicalutamide e) Foliglurax c Empty GW 501516 Emedastine Talazoparib Pretomanid Delamanid Loxoribine URB-597 L-368,899 GNE-781 (monohydroc Empty tosylate hydrochloride hloride) Seltorexant d Empty Clotrimazole Istradefylline Preladenant Rosiptor Seltorexant (hydrochlorid Tucidinostat Vorolanib Balovaptan Baloxavir Empty e) marboxil Parsaclisib e Empty Mavacamten Praliciguat Tulrampator Atabecestat Elenbecestat Enarodustat Firibastat Fulacimstat Lazertinib (hydrochlorid Empty e) Lanraplenib Danegaptide f Empty Ralaniten Cilofexor Edicotinib Lanraplenib (succinate) Nidufexor Pemigatinib Soticlestat Hydrochloride Ziresovir Empty g Empty GW2580 Rezivertinib Tolebrutinib Camicinal S 18986 VER-82576 AZD1390 IRAK4-IN-7 RG7112 Alisertib Empty Trametinib h Empty MK-0752 Lenvatinib Lenvatinib Pomalidomid MGCD-265 Tozadenant Ibrutinib Trametinib (DMSO NDT 9513727 Empty (mesylate) e analog solvate) Plate layout: CS-L061-6 Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA Tel: 732-484-9848 Fax: 888-484-5008 Email: [email protected] • Bioactive Molecules • Building Blocks • Intermediates www.ChemScene.com 1 2 3 4 5 6 7 8 9 10 11 12 Eplivanserin LM11A-31 a Empty (±)-CPSI- AS601245 A-770041 (hemifumarat (dihydrochlori Rivastigmine TC-G 1005 Risperidone PF-02413873 SNT-207707 Empty 1306 e) de) (tartrate) Alendronate b Empty SNT-207858 CVT-12012 NS11394 Fingolimod SB 239063 SD 0006 Asenapine (sodium Sitaxsentan JNJ- Empty (free base) (maleate) hydrate) (sodium) 38877618 Nintedanib c Empty AZD7325 esylate GLPG1837 PF-05180999 Finerenone E-7386 MK-8353 EBI-2511 AZD7594 BAY-677 Empty (Rac)- d Empty BAY-678 GDC-0927 INCB-057643 LSZ-102 RGX-104 RGX-104 NMDAR NAcM-OPT Tafenoquine BAY-1316957 Empty (free Acid) antagonist 1 (Succinate) 3,4'- e Empty FT113 TAS0728 Calcium Pinaverium Tyk2-IN-5 CWHM-1008 DMX-5804 Dihydroxyflav BI-749327 GSK2983559 Empty dobesilate bromide one GDC-0575 f Empty Unesbulin PF-06869206 ABBV-744 eCF506 PRN1008 GDC-0575 dihydrochlorid ARQ 531 VIT-2763 O-304 Empty e H3B-6545 g Empty ACP-105 S-23 T025 TAS6417 AZ32 Ripretinib Menaquinone H3B-6545 (hydrochlorid CF53 Empty -7 e) Retagliptin PF-06700841 h Empty H3B-5942 UCB9608 SMN-C3 CG-806 (phosphate) Retagliptin PF-06747711 (P-Tosylate) SMS2-IN-2 ACT-709478 Empty Plate layout: CS-L061-7 1 2 3 4 5 6 7 8 9 10 11 12 Almonertinib 5- a Empty PXS-4728A Almonertinib (hydrochlorid TVB-2640 TL02-59 Mito-TEMPO DT-061 (1S,2S,3R)- Methyltetrahy Anserine Empty e) DT-061 drofolic acid PLX5622 Se- b Empty Sphingomyeli trans-AUCB BI-671800 (hemifumarat VTP50469 (S)-PF- Olutasidenib Methylseleno LY3295668 Sotorasib Empty n e) 06873600 cysteine PXS-5153A c Empty (monohydroc Salcaprozate Ly93 FGFR1/DDR2 DLK-IN-1 N,N'-Diacetyl- ONO-7475 SHP394 VU6012962 GB1107 Empty hloride) (sodium) inhibitor 1 L-cystine Pyridoxal d Empty MRTX-1257 LY2940094 Rineterkib LY2452473 Benproperine Eslicarbazepi MA-0204 isonicotinoyl JNJ- G5-7 Empty (phosphate) ne hydrazone 63576253 Propiverine e Empty Glumetinib BIBB 515 (hydrochlorid URB937 BRD0705 BRD5648 Purfalcamine Dabuzalgron UTL-5g AZD7507 Empty e) S55746 f Empty Deucravacitini S55746 (hydrochlorid USP25/28 MJN110 Ibrolipim UNC569 THPP-1 ABX-1431 RG7834 Empty b e) inhibitor AZ1 DDD107498 Enclomiphen g Empty (succinate) Eprosartan Danicopan Org-12962 AS-041164 e (citrate) AZD1940 SX-682 S18-000003 Ensifentrine Empty Fingolimod Erlotinib PF-06446846 Pazopanib BMS-599626 h Empty Trofosfamide AZD9567 (hydrochlorid Afizagabar (Hydrochlorid PFE-360 (hydrochlorid (Hydrochlorid (Hydrochlorid MW-150
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    © Copyright 2019 Savannah Jane Kerr McFeely Clinical Significance and Regulatory Framework for the Evaluation of Organic Anion Transporting Polypeptide 1B-Based Drug-Drug Interactions Savannah Jane Kerr McFeely A dissertation submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy University of Washington 2019 Reading Committee: Isabelle Ragueneau-Majlessi, Chair Jashvant Unadkat Bhagwat Prasad Program Authorized to Offer Degree: Pharmaceutics University of Washington Abstract Clinical Significance and Regulatory Framework for the Evaluation of Organic Anion Transporting Polypeptide 1B-Based Drug-Drug Interactions Savannah Jane Kerr McFeely Chair of the Supervisory Committee: Dr. Isabelle Ragueneau-Majlessi Department of Pharmaceutics This dissertation research aims to conduct a comprehensive analysis of the clinical role of organic anion transporting polypeptides (OATPs) 1B1 and 1B3 and the regulatory approach for their evaluation. The work included here has identified the most relevant clinical substrates and inhibitors. Additionally, the contributing factors in the variability of in vitro inhibition constants as well as real-world implications for OATP1B1/1B3 drug-drug interactions are discussed. In Chapter 2, six compounds were identified as potential clinical markers of OATP1B1/1B3 activity through the use of a novel indexing system. These drugs were identified from a list of 34 clinical substrates identified from a thorough analysis of the available in vitro and in vivo data. These findings also suggest that the risk for comedication interactions involve drugs from multiple therapeutic areas showing a reliance on hepatic uptake via the OATP transporters. Chapters 3 seeks to better understand the variability of in vitro inhibition data. By analyzing available OATP1B1/1B3 IC50 values, the primary contributing factors to in vitro variability were identified as the cell system used and inclusion of a preincubation with the inhibitor.
  • Durham E-Theses

    Durham E-Theses

    Durham E-Theses Elemental Fluorine for the Greener Synthesis of Life-Science Building Blocks HARSANYI, ANTAL How to cite: HARSANYI, ANTAL (2016) Elemental Fluorine for the Greener Synthesis of Life-Science Building Blocks, Durham theses, Durham University. Available at Durham E-Theses Online: http://etheses.dur.ac.uk/11705/ Use policy The full-text may be used and/or reproduced, and given to third parties in any format or medium, without prior permission or charge, for personal research or study, educational, or not-for-prot purposes provided that: • a full bibliographic reference is made to the original source • a link is made to the metadata record in Durham E-Theses • the full-text is not changed in any way The full-text must not be sold in any format or medium without the formal permission of the copyright holders. Please consult the full Durham E-Theses policy for further details. Academic Support Oce, Durham University, University Oce, Old Elvet, Durham DH1 3HP e-mail: [email protected] Tel: +44 0191 334 6107 http://etheses.dur.ac.uk 2 Durham University A thesis entitled Elemental Fluorine for the Greener Synthesis of Life-Science Building Blocks by Antal Harsanyi (College of St. Hild and St. Bede) A candidate for the degree of Doctor of Philosophy Department of Chemistry, Durham University 2016 Antal Harsanyi: Elemental fluorine for the greener synthesis of life-science building blocks Abstract Fluorinated organic compounds are increasingly important in many areas of our modern lives, especially in pharmaceutical and agrochemical applications where the incorporation of this element can have a major influence on biochemical properties.
  • Endocrine Abstracts Vol 65

    Endocrine Abstracts Vol 65

    Endocrine Abstracts November 2019 Volume 65 ISSN 1479-6848 (online) Society for Endocrinology BES 2019 11–13 November 2019, Brighton published by Online version available at bioscientifica www.endocrine-abstracts.org Volume 65 Endocrine Abstracts November 2019 Society for Endocrinology BES 2019 11–13 November 2019, Brighton VOLUME EDITORS The abstracts submitted were marked by the Abstract Marking panel, selected by the Programme Organising Committee. Programme Committee D Bassett (Programme Secretary) (London) Laura Matthews (Leeds) Andrew Childs (Programme Co-ordinator) (London) Carla Moran (Cambridge) Nils Krone (Programme Co-ordinator) (Sheffield) Annice Mukherjee (Salford) Helen Simpson (Programme Co-ordinator) (London) Francesca Spiga (Bristol) Davide Calebiro (Birmingham) Jeremy Tomlinson (Oxford) Ben Challis (Cambridge) Jennifer Walsh (Sheffield) Mandy Drake (Edinburgh) Abstract Marking Panel Ramzi Ajjan (Leeds) Neil Gittoes (Birmingham) John Newell-Price (Sheffield) Richard Anderson (Edinburgh) Helena Gleeson (Birmingham) Mark Nixon (Edinburgh) Ruth Andrew (Edinburgh) Philippa Hanson (London) Finbarr O’Harte (Ulster) Weibke Arlt (Birmingham) Martin Hewison (Birmingham) Adrian Park (Cambridge) Mo Aye (Hull) Claire Higham (Manchester) Simon Pearce (Newcastle) Tom Barber (Warwick) Steve Hillier (Edinburgh) Andrew Powlson (Cambridge) Duncan Bassett (London) Andy James (Newcastle) Teresa Rea (Belfast) Roger Brown (Edinburgh) Channa Jayasena (London) Martin Read (Birmingham) Paul Carroll (London) Niki Karavitaki (Oxford) Aled Rees (Cardiff)