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CAS No.: 190786-44-8

Bepotastine besilate/苯磺酸贝托司汀 Catalog No. CSN10415

Synonyms: TAU 284;Bepotastine (besylate);Bepotastine besylate

Bepotastine besilate is a selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Histamine Receptor H1

pIC50:5.7
描述Bepotastine besilate (BB) is a second-generation H1-antihistamine that, as an ophthalmic solution, is approved in the United States by the Food and Drug Administration (FDA) for the treatment of allergic conjunctivitis. BB is effective and well-tolerated in the treatment of allergic rhinitis. Side effects are infrequent in patients with AR who do not have kidney or liver disease^[3]. Bepotastine may also have other immunoactive properties, such as inhibition of eosinophil migration, interleukin-5 (IL-5), leukotrienes (e.g., LTB4) and platelet-activating factor (PAF)^[4]. Bepotastine in vivo dose-dependently inhibited the acceleration of histamine-induced vascular permeability and inhibited homologous passive cutaneous anaphylaxis in guinea pig studies. In mouse models of itching, oral bepotastine inhibited the frequency and duration of scratching behavior. Multiple in vivo animal toxicology studies have demonstrated bepotastine to be safe with no significant effects on respiratory, circulatory, central nervous, digestive, or urinary systems^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02686294	Rhinitis, Allergic, Perennial	Phase 1	Completed	-	Korea, Republic of ... more >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 Collapse <<
NCT02682745	Rhinitis, Allergic, Perennial	Phase 1	Completed	-	Korea, Republic of ... more >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 Collapse <<
NCT03200496	Healthy	Phase 1	Completed	-	Korea, Republic of ... more >> Korea University Anam Hospital Seoul, Korea, Republic of Collapse <<

更多
参考文献

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
- 1.8279 mL
- 9.1397 mL
- 18.2794 mL
- 5 mM
- 0.3656 mL
- 1.8279 mL
- 3.6559 mL
- 10 mM
- 0.1828 mL
- 0.9140 mL
- 1.8279 mL

技术信息

CAS号

190786-44-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H31ClN2O6S

运输

蓝冰

分子量

547.06

别名

TAU 284;Bepotastine (besylate);Bepotastine besylate;bepotastine besilate;Bepreve;Talion;苯磺酸贝托司汀

溶解度

DMSO	109.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	Insoluble

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

NCT02686294	Rhinitis, Allergic, Perennial	Phase 1	Completed	-	Korea, Republic of ... more >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 Collapse <<
NCT02682745	Rhinitis, Allergic, Perennial	Phase 1	Completed	-	Korea, Republic of ... more >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 Collapse <<
NCT03200496	Healthy	Phase 1	Completed	-	Korea, Republic of ... more >> Korea University Anam Hospital Seoul, Korea, Republic of Collapse <<
NCT01277341	Seasonal Allergic Rhinitis	Phase 2	Completed	-	United States, California ... more >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Collapse <<
NCT01339507	-	-	Completed	-	United States, Texas ... more >> Derek Cunningham Austin, Texas, United States, 78746 Collapse <<
NCT00586664	Allergic Conjunctivitis	Phase 3	Completed	-	United States, California ... more >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Collapse <<
NCT01578278	Seasonal Allergic Rhinitis	Phase 2	Completed	-	United States, California ... more >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Collapse <<
NCT00586625	Allergic Conjunctivitis	Phase 3	Completed	-	-
NCT01174823	Allergic Conjunctivitis	Phase 2	Completed	-	United States, California ... more >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Collapse <<
NCT00586664	-	-	Completed	-	-
NCT01346371	Allergic Conjunctivitis	Phase 4	Unknown	August 2012	United States, Minnesota ... more >> Minnesota Eye Consultants, P.A. Minneapolis, Minnesota, United States, 55404 Collapse <<
NCT01222299	Allergic Rhinitis	Phase 1 Phase 2	Completed	-	United States, California ... more >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Collapse <<
NCT00586625	-	-	Completed	-	-
NCT02332044	Healthy	Phase 1	Completed	-	-
NCT01897428	Allergic Rhinitis ... more >> Urticaria Pruritus Collapse <<	Phase 1	Completed	-	Korea, Republic of ... more >> Dept. of Clinical Pharmacology & Toxicology, Anam Hospital Seoul, Korea, Republic of, 136-705 Collapse <<
NCT01925313	Healthy	Phase 1	Completed	-	Korea, Republic of ... more >> Yonsei university severance hospital Seoul, Korea, Republic of Collapse <<
NCT00424398	Conjunctivitis, Allergic	Phase 2 Phase 3	Completed	-	United States, California ... more >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92630 Collapse <<
NCT01425632	Perennial Allergic Rhinitis	Phase 3	Completed	-	Japan ... more >> Reserch site Chubu, Japan Reserch site Hokuriku, Japan Reserch site Kanto, Japan Reserch site Kinki, Japan Reserch site Kyusyu, Japan Collapse <<
NCT01840605	Dermatitis At... more >>opic Collapse <<	Phase 3	Completed	-	Japan ... more >> Medical Corporation Kojinkai Asanuma Dermatology Clinic Hokkaido, Japan Collapse <<
NCT01425632	-	-	Completed	-	-
NCT01840605	-	-	Completed	-	-
NCT00424398	-	-	Completed	-	-
NCT01128556	Histamine Responsive Allergy P... more >>atients Collapse <<	Phase 4	Completed	-	United States, Texas ... more >> North Texas Institute for Clinical Trials Fort Worth, Texas, United States, 76132 Collapse <<
NCT01450176	Eye Allergies	Not Applicable	Completed	-	United States, Tennessee ... more >> McCabe Vision Center Murfreesboro, Tennessee, United States, 37129 Collapse <<
NCT01753739	Seasonal Allergic Rhinitis	Phase 2	Completed	-	United States, California ... more >> Bausch & Lomb Incorporated Irvine, California, United States, 92618-2301 Collapse <<
NCT01861522	Perennial Allergic Rhinitis	Phase 3	Completed	-	Japan ... more >> Reserch site Fukuoka, Japan Reserch site Toyama, Japan Collapse <<
NCT01861522	-	-	Completed	-	-
NCT01900054	-	-	Completed	-	-
NCT01443442	Allergic Conjunctivitis	Phase 4	Completed	-	United States, California ... more >> Eye Car Center, Southern California college of Optometry Fullerton, California, United States, 92831 Eye Care Center, Southern Caalifornia College of Optometry Fullerton, California, United States, 92831 Collapse <<
NCT01337557	Allergic Conjunctivitis	Phase 4	Unknown	November 2011	-
NCT01900054	Perennial Allergic Rhinitis	Phase 3	Completed	-	Japan ... more >> Reserch site Kanagawa, Japan Collapse <<

Bepotastine besilate/苯磺酸贝托司汀 Catalog No. CSN10415

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