产品名称

英文名称：SB705498

同义词

SB-705498、501951-42-4、SB705498、(R)-1-(2-bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea、SB 705498、1-(2-bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)pyridin-2-yl]pyrrolidin-3-yl]urea、T74V9O0Y2W、GSK705498、N-(2-bromophenyl)-N'-[(3R)-1-[

产品性质

CAS编号：501951-42-4

分子式：C17H16BrF3N4O

分子量：429.23

PubChem编号：9910486

英文别名：SB-705498|501951-42-4|SB705498|(R)-1-(2-bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea|SB 705498|1-(2-bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)pyridin-2-yl]pyrrolidin-3-yl]urea|T74V9O0Y2W|GSK705498|N-(2-bromophenyl)-N'-[(3R)-1-[

规格或纯度：98%

英文名称：SB705498

生化机理：SB-705498 is a potent, selective and transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1. SB-705498 potently inhibits capsaicin-induced activation of human TRPV1 expressed in 1321N1 cells or HEK293 cells with apparent pKi of 7.5 or 7.6, respectively. Coapplication of 100 nM SB-705498 rapidly, completely and reversibly inhibits hTRPV1 expressed in HEK293 cells. Compared with placebo, SB-705498 reduced the area of capsaicin-evoked flare (P=0.0047). The heat pain threshold on non-sensitised skin was elevated following SB-705498 (estimated difference from placebo [95% confidence intervals] 1.3 degrees C [0.07,2.53], P=0.019). Following capsaicin sensitisation, the heat pain threshold and tolerance were similar between SB-705498 and placebo. However, SB-705498 increased heat pain tolerance at the site of UVB-evoked inflammation (estimated difference from placebo 0.93 degrees C [0.25,1.6], P=0.0054). The magnitude of the pharmacodynamic effects of SB-705498 appeared to be related to plasma concentration. These results indicate that SB-705498, at a clinically safe and well-tolerated dose, has target-specific pharmacodynamic activity in humans. These data provide the first clinical evidence that a TRPV1 antagonist may alleviate pain and hyperalgesia associated with inflammation and tissue injury.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：SB705498是一种hTRPV1拮抗剂，抑制TRPV1的Capsaicin，酸和热激活，IC50分别为3 nM， 0.1 nM和6 nM，该作用具有一定的电压依赖性，作用于TRPV1比作用于TRPM8选择性高100倍以上。Phase 2。

ALogP：3.8

IUPAC Name：1-(2-bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)pyridin-2-yl]pyrrolidin-3-yl]urea

INCHI：InChI=1S/C17H16BrF3N4O/c18-13-3-1-2-4-14(13)24-16(26)23-12-7-8-25(10-12)15-6-5-11(9-22-15)17(19,20)21/h1-6,9,12H,7-8,10H2,(H2,23,24,26)/t12-/m1/s1

InChi Key：JYILLRHXRVTRSH-GFCCVEGCSA-N

Canonical SMILES：C1CN(CC1NC(=O)NC2=CC=CC=C2Br)C3=NC=C(C=C3)C(F)(F)F

Isomeric SMILES：C1CN(C[C@@H]1NC(=O)NC2=CC=CC=C2Br)C3=NC=C(C=C3)C(F)(F)F

PubChem CID：9910486

CAS Registry No.：501951-42-4

ChEMBL Ligand：CHEMBL207433

溶解性：DMSO 86 mg/mL Water <1 mg/mL Ethanol 20 mg/mL

产品包装