|(R)-1-(2-溴苯基)-3-(1-(5-(三氟甲基)吡啶-2-基)吡咯烷-3-基)脲|CsnPharm

CAS No.: 501951-42-4

(R)-1-(2-Bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea Catalog No. CSN15682

Synonyms: SB-705498

SB-705498 is a selective antagonist of transient receptor potential vanilloid 1 (TRPV1) with pIC50 of 7.1.

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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

描述TRPV1 is a non-selective cation channel, predominantly expressed by peripheral sensory neurons. It plays a key role in the detection of noxious painful stimuli, such as capsaicin, acid and heat. SB-705498 is a potent TRPV1 antagonist with pK_b value of 7.5 in FLIPR-Ca²⁺-based assays versus capsaicin at TRPV1. Co-application of 1μM SB-705498 completely and reversibly inhibited capsaicin-mediated activation of human TRPV1 by measure of whole cell currents by patch clamp. Pre-treatment with SB-705498 at doses of 3mg/kg and 10mg/kg, p.o., for 2h, dose-dependently antagonized capsaicin induced secondary hyperalgesia in rat. SB-705498 can potently inhibit the multiple modes of TRPV1 activation, including capsaicin-, acid- and heat-mediated activation of human TRPV1.

动物研究

剂量

Cat: 2 mg/kg^[3] (i.v.) Guinea pigs: 10 mg/kg - 100 mg/kg^[4] (i.p.); 3 mg/kg - 30 mg/kg^[5] (p.o.)

给药途径

i.v., i.p., p.o.

动物药代数据

Animal	Rats^[2]	Dogs^[2]
Dose	3 mg/kg	1 mg/kg
Administration	p.o.	p.o.
F	0.86	0.42
T_1/2	3.1 h	3.4 h
Vss	0.9 L/kg	1.9 L/kg

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
NCT00281684	Toothache	Phase 2	Completed	-	Italy ... more >> GSK Investigational Site Verona, Veneto, Italy, 37134 Korea, Republic of GSK Investigational Site Seoul, Korea, Republic of, 110-768 United Kingdom GSK Investigational Site Croydon, Surrey, United Kingdom, CR7 7YE GSK Investigational Site Leeds, United Kingdom, LS2 9NG GSK Investigational Site Manchester, United Kingdom, M13 9WL Collapse <<
NCT00907933	Rhinitis	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site London, United Kingdom, NW10 7EW Collapse <<
NCT01673529	Dermatitis, Atopic	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site Cambridge, United Kingdom, CB2 2GG 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
- 2.3297 mL
- 11.6486 mL
- 23.2973 mL
- 5 mM
- 0.4659 mL
- 2.3297 mL
- 4.6595 mL
- 10 mM
- 0.2330 mL
- 1.1649 mL
- 2.3297 mL

技术信息

CAS号

501951-42-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H16BrF3N4O

运输

蓝冰

分子量

429.23

别名

SB-705498

溶解度

DMSO	177.0 mg/mL (412.4 mM)
Water	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

NCT00281684	Toothache	Phase 2	Completed	-	Italy ... more >> GSK Investigational Site Verona, Veneto, Italy, 37134 Korea, Republic of GSK Investigational Site Seoul, Korea, Republic of, 110-768 United Kingdom GSK Investigational Site Croydon, Surrey, United Kingdom, CR7 7YE GSK Investigational Site Leeds, United Kingdom, LS2 9NG GSK Investigational Site Manchester, United Kingdom, M13 9WL Collapse <<
NCT00907933	Rhinitis	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site London, United Kingdom, NW10 7EW Collapse <<
NCT01673529	Dermatitis, Atopic	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site Cambridge, United Kingdom, CB2 2GG Collapse <<
NCT00461682	Irritable Colon	Phase 2	Terminated	-	United Kingdom ... more >> GSK Investigational Site London, United Kingdom, W12 0NN Collapse <<
NCT00731250	Rhinitis	Phase 1	Completed	-	Netherlands ... more >> GSK Investigational Site Amsterdam, Netherlands, 1105 AZ Collapse <<
NCT01424397	Rhinitis	Phase 2	Completed	-	Austria ... more >> GSK Investigational Site Vienna, Austria, A-1150 Collapse <<
NCT00269022	Migraine, Acute	Phase 2	Completed	-	Australia, New South Wales ... more >> GSK Investigational Site Randwick, New South Wales, Australia, 2031 Canada, Ontario GSK Investigational Site Toronto, Ontario, Canada, M1L 4S4 Netherlands GSK Investigational Site Leiden, Netherlands, 2333 ZA United Kingdom GSK Investigational Site Cambridge, Cambridgeshire, United Kingdom, CB2 2GG Collapse <<
NCT01439308	Rhinitis	Phase 2	Completed	-	Netherlands ... more >> GSK Investigational Site Amsterdam, Netherlands, 1105 AZ Collapse <<
NCT01476098	Rhinitis	Phase 2	Completed	-	United Kingdom ... more >> GSK Investigational Site Manchester, United Kingdom, M23 9QZ Collapse <<
NCT01424514	-	-	Completed	-	-
NCT00461682	-	-	Terminated	-	-
NCT01424514	Rhinitis	Phase 2	Completed	-	Canada, Ontario ... more >> GSK Investigational Site Mississauga, Ontario, Canada, L4W 1N2 Collapse <<

(R)-1-(2-Bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea Catalog No. CSN15682

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