|(3S,4R)-3-乙基-4-(3H-咪唑并[1,2-a]吡咯并[2,3-e]吡嗪-8-基)-N-(2,2,2-三氟乙基)吡咯烷-1-甲酰胺|CsnPharm

CAS No.: 1310726-60-3

Upadacitinib/乌帕替尼 Catalog No. CSN18721

Synonyms: ABT-494;乌帕替尼

Upadacitinib is a selective JAK1 inhibitor with an IC50 of 43 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 JAK1

IC50:43nM
描述Upadacitinib is a selective JAK1 inhibitor with IC50 value of 45nM, exhibiting less potency to JAK2 (IC50=109nM) and weak inhibitory effect on JAK3 (2.1μM) and TYK2 (4.7μM). Upadacitinib could potently inhibit STAT phosphorylation stimulated by cytokines IL-6, OSM, IL-2, and IFNγ dependent on JAK1. Upadacitinib is mainly used in treatment of rheumatoid arthritis. Oral administration of Upadacitinib at dose of 1, 3 and 10mg/kg inhibited disease pathology in rat adjuvant induced arthritis, resulting dose- and exposure-dependent reductions in paw swelling and reducing loss of bone volume. Compared with tofacitinib, Upadacitinib could both spare reticulocyte deployment and NK cell count depletion relative to efficacy, and spare common gamma chain signaling relative to IL-6 signaling.
动物研究
剂量
Rat: 3 mg/kg, 10 mg/kg^[3] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Rat: 3 mg/kg, 10 mg/kg^[3] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02706873	Rheumatoid Arthritis	Phase 3	Active, not recruiting	March 28, 2021	-
NCT02675426	Rheumatoid Arthritis	Phase 3	Active, not recruiting	August 6, 2020	-
NCT02365649	Crohn's Disease	Phase 2	Completed	-	-

更多
参考文献

[1] Nakayamada S, Kubo S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419.
[2] Kremer JM, Emery P, et al. A Phase IIb Study of ABT-494, a Selective JAK-1 Inhibitor, in Patients With Rheumatoid Arthritis and an Inadequate Response to Anti-Tumor Necrosis Factor Therapy. Arthritis Rheumatol. 2016 Dec;68(12):2867-2877.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6290 mL
- 13.1452 mL
- 26.2904 mL
- 5 mM
- 0.5258 mL
- 2.6290 mL
- 5.2581 mL
- 10 mM
- 0.2629 mL
- 1.3145 mL
- 2.6290 mL

技术信息

CAS号

1310726-60-3

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H19F3N6O

运输

蓝冰

分子量

380.37

别名

ABT-494;乌帕替尼

溶解度

DMSO	76.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	75.0 mg/mL (197.2 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02706873	Rheumatoid Arthritis	Phase 3	Active, not recruiting	March 28, 2021	-
NCT02675426	Rheumatoid Arthritis	Phase 3	Active, not recruiting	August 6, 2020	-
NCT02365649	Crohn's Disease	Phase 2	Completed	-	-
NCT03345849	Crohn's Disease	Phase 3	Recruiting	April 21, 2021	-
NCT02955212	Rheumatoid Arthritis (RA)	Phase 3	Recruiting	June 13, 2020	-
NCT03104374	Psoriatic Arthritis	Phase 3	Recruiting	February 26, 2022	-
NCT02706847	Rheumatoid Arthritis	Phase 3	Active, not recruiting	August 6, 2020	-
NCT02706951	Rheumatoid Arthritis	Phase 3	Active, not recruiting	August 7, 2020	-
NCT02925117	Atopic Dermatitis	Phase 2	Active, not recruiting	January 24, 2019	-
NCT02049138	Rheumatoid Arthritis	Phase 2	Active, not recruiting	February 20, 2021	-
NCT02629159	Rheumatoid Arthritis	Phase 3	Active, not recruiting	August 10, 2020	-
NCT03345823	Crohn's Disease	Phase 3	Enrolling by invitation	March 22, 2023	-
NCT03104400	Psoriatic Arthritis	Phase 3	Recruiting	September 6, 2023	-
NCT03086343	Rheumatoid Arthritis (RA)	Phase 3	Recruiting	March 28, 2021	-
NCT02819635	Ulcerative Colitis (UC)	Phase 3	Recruiting	February 17, 2022	-
NCT03725202	Giant Cell Arteritis (GCA)	Phase 3	Not yet recruiting	April 25, 2023	-
NCT02720523	Rheumatoid Arthritis (RA)	Phase 2	Active, not recruiting	July 19, 2020	-
NCT03682705	Rheumatoid Arthritis (RA)	Phase 2	Recruiting	January 31, 2020	-
NCT03661138	Atopic Dermatitis	Phase 3	Recruiting	May 8, 2022	Japan ... more >> Central Clinic /ID# 206558 Not yet recruiting Nagoya-shi, Aichi, Japan, 4640821 Nagoya City University Hospital /ID# 207566 Not yet recruiting Nagoya-shi, Aichi, Japan, 467-8602 Yasumoto Dermatology Clinic /ID# 206480 Not yet recruiting Chikushino-shi, Fukuoka, Japan, 8180083 Kiryu Dermatology Clinic /ID# 206044 Not yet recruiting Fukuoka City, Fukuoka, Japan, 8130044 Matsuda Tomoko Dermatological Clinic /ID# 206288 Not yet recruiting Fukuoka-shi, Fukuoka, Japan, 8190167 Medical Corporation Matsuo Clinic /ID# 207323 Not yet recruiting Fukuoka-shi, Fukuoka, Japan, 8190373 Higuchi Dermatology Urology Clinic /ID# 206287 Not yet recruiting Kasuga-shi, Fukuoka, Japan, 8160802 Kiryu Kosei General Hospital /ID# 206155 Not yet recruiting Kiryu-shi, Gunma, Japan, 376-0024 Gunma University Hospital /ID# 207016 Not yet recruiting Maebashi-shi, Gunma, Japan, 371-8511 Fukuyama City Hospital /ID# 206761 Recruiting Fukuyama-shi, Hiroshima, Japan, 721-8511 Asahikawa Medical University Hospital /ID# 206521 Not yet recruiting Asahikawa-shi, Hokkaido, Japan, 078-8510 Kitago Dermatology Clinic /ID# 207025 Not yet recruiting Sapporo-shi, Hokkaido, Japan, 003-0833 Kato Dermatology Clinic /ID# 206561 Recruiting Sapporo-shi, Hokkaido, Japan, 0030026 Hokkaido P.W.F.A.C. Sapporo-Kosei General Hospital /ID# 206519 Not yet recruiting Sapporo-shi, Hokkaido, Japan, 060-0033 Hyogo Prefectural Amagasaki General Medical Center /ID# 206974 Not yet recruiting Amagasaki-shi, Hyogo, Japan, 660-8550 Kobayashi skin clinic /ID# 206106 Not yet recruiting Kobe-shi, Hyogo, Japan, 6540011 Kobe University Hospital /ID# 206200 Not yet recruiting Kobe, Hyogo, Japan, 650-0017 Medical corporation Kojunkai Kosugi Dermatology Clinic /ID# 206766 Recruiting Kawasaki-shi, Kanagawa, Japan, 211-0063 Nippon Medical School Musashi Kosugi Hospital /ID# 206656 Not yet recruiting Kawasaki-shi, Kanagawa, Japan, 211-8533 Suizenji Dermatology Clinic /ID# 205871 Recruiting Kumamoto-shi, Kumamoto, Japan, 8620950 Nagasaki University Hospital /ID# 206118 Not yet recruiting Nagasaki-shi, Nagasaki, Japan, 852-8501 Isonokami dermatological clinic /ID# 206923 Not yet recruiting Daito-shi, Osaka, Japan, 5740046 Shizuoka General Hospital /ID# 207122 Not yet recruiting Shizuoka-shi, Shizuoka, Japan, 420-8527 Medical Corporation Seikakai Mildix Skin Clinic /ID# 206829 Not yet recruiting Adachi-ku, Tokyo, Japan, 1200034 Fukuwa clinic /ID# 206760 Recruiting Chuo-ku, Tokyo, Japan, 1030027 Hosono Clinic /ID# 205953 Not yet recruiting Chuo-ku, Tokyo, Japan, 1040031 Ichinomiya Municipal Hospital /ID# 205942 Not yet recruiting Ichinomiya-shi, Tokyo, Japan, 491-8558 Mita Dermatology Clinic /ID# 206694 Not yet recruiting Minato-ku, Tokyo, Japan, 1080014 Medical Corporation Jitai-kai Nakano Dermatology Clinic /ID# 206882 Not yet recruiting Nakano-ku, Tokyo, Japan, 1640001 Matsuyama Dermatology Clinic /ID# 205998 Not yet recruiting Nakano-ku, Tokyo, Japan, 1650026 Tokyo Rosai Hospital /ID# 205809 Recruiting Ohta-ku, Tokyo, Japan, 143-0013 Miu Skin Clinic /ID# 206911 Recruiting Ota-ku, Tokyo, Japan, 114-0052 Tanpopo Dermatology Clinic /ID# 207013 Not yet recruiting Ota-ku, Tokyo, Japan, 1430023 Naoko Dermatology Clinic /ID# 205334 Not yet recruiting Setagaya-ku, Tokyo, Japan, 1580097 Tachikawa Dermatology Clinic /ID# 206996 Recruiting Tachikawa-shi, Tokyo, Japan, 1900023 Kansai Rosai Hospital /ID# 205918 Recruiting Amagasaki, Japan, 660-8511 Yaesu Nihonbashi Skin Clinic /ID# 207125 Not yet recruiting Chuo-ku, Japan, 1030028 Tokai University Hospital /ID# 206657 Not yet recruiting Isehara, Japan, 259-1143 Kizawa Memorial Hospital /ID# 205684 Not yet recruiting Minokamo, Japan, 505-0034 Nihon University Itabashi Hosp /ID# 206186 Not yet recruiting Tokyo, Japan, 173-0032 Toyama Prefectural Ctr Hosp /ID# 206286 Not yet recruiting Toyama, Japan, 930-0975 Yokohama Rosai Hospital /ID# 206648 Not yet recruiting Yokohama, Japan, 222-0036 Collapse <<
NCT03738397	Atopic Dermatitis	Phase 3	Not yet recruiting	July 23, 2020	United States, California ... more >> Wallace Medical Group, Inc. /ID# 208524 Not yet recruiting Beverly Hills, California, United States, 90211 Dermatology Res. Assoc., CA /ID# 209097 Not yet recruiting Los Angeles, California, United States, 90045 United States, Nebraska Skin Specialists, PC /ID# 208843 Not yet recruiting Omaha, Nebraska, United States, 68144 Finland Oulu University Hospital /ID# 208961 Not yet recruiting Oulu, Pohjois-Pohjanmaa, Finland, 90220 Malaysia University Malaya Med Ctr /ID# 208861 Not yet recruiting Kuala Lumpur, Malaysia, 50603 Sweden Falun Lasarett /ID# 206784 Not yet recruiting Falun, Sweden, SE-79182 Collapse <<
NCT03345836	Crohn's Disease	Phase 3	Recruiting	April 15, 2020	-
NCT03568318	Atopic Dermatitis	Phase 3	Recruiting	May 6, 2022	-
NCT03607422	Atopic Dermatitis	Phase 3	Recruiting	June 8, 2022	-
NCT03569293	Atopic Dermatitis	Phase 3	Recruiting	May 6, 2022	-
NCT03725007	Juvenile Idiopathic Arthritis ... more >>(JIA) Collapse <<	Phase 1	Not yet recruiting	July 18, 2024	United States, Minnesota ... more >> University of Minnesota - Pediatrics/Rheumatology /ID# 202897 Not yet recruiting Minneapolis, Minnesota, United States, 55454-1450 United States, Pennsylvania Children's Hospital of Pittsburgh of UPMC /ID# 202994 Not yet recruiting Pittsburgh, Pennsylvania, United States, 15224-1334 United States, Washington Seattle Children's Hospital /ID# 203003 Not yet recruiting Seattle, Washington, United States, 98105 Germany PRI - Pediatric Rheumatology Research Institute /ID# 205954 Not yet recruiting Bad Bramstedt, Germany, 24576 Helios Klinikum Berlin Buch /ID# 206859 Not yet recruiting Berlin, Germany, 13125 Kinder- & Jugendrheumatologie /ID# 206571 Not yet recruiting Hamburg, Germany, 22081 Asklepios Klinik St. Augustin /ID# 203264 Not yet recruiting Sankt Augustin, Germany, 53757 Italy IRCCS Ospedale Pediatrico Bambino Gesù /ID# 203835 Not yet recruiting Rome, Lazio, Italy, 00165 IRCCS Istituto G. Gaslini /ID# 203648 Not yet recruiting Genoa, Italy, 16148 Puerto Rico Centro de Reumatologia Pediatrico de Puerto Rico /Id# 204406 Not yet recruiting Bayamon, Puerto Rico, 00959 Mindful Medical Research /ID# 204488 Not yet recruiting San Juan, Puerto Rico, 00918-3756 Spain Hospital Sant Joan de Deu /ID# 203915 Not yet recruiting Esplugues de Llobregat, Spain, 08950 Hosp Infantil Univ Nino Jesus /ID# 206466 Not yet recruiting Madrid, Spain, 28009 Hospital Univ Ramon y Cajal /ID# 203917 Not yet recruiting Madrid, Spain, 28034 Hospital Universitario La Paz /ID# 203927 Not yet recruiting Madrid, Spain, 28046 Hospital Universitario La Fe /ID# 203914 Not yet recruiting Valencia, Spain, 46026 Collapse <<
NCT03646604	Atopic Dermatitis	Phase 1	Not yet recruiting	October 15, 2022	-
NCT02782663	Crohn's Disease (CD)	Phase 2	Active, not recruiting	August 23, 2025	-
NCT03006068	Ulcerative Colitis (UC)	Phase 3	Enrolling by invitation	July 20, 2024	-
NCT03653026	Ulcerative Colitis (UC)	Phase 3	Recruiting	July 3, 2024	-
NCT03178487	Ankylosing Spondylitis (AS)	Phase 2	Active, not recruiting	November 11, 2020	-

Upadacitinib/乌帕替尼 Catalog No. CSN18721

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