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885101-89-3

中文名稱 885101-89-3(GW9508)
英文名稱 GW9508
CAS 885101-89-3
分子式 C22H21NO3
分子量 347.41
MOL 文件 885101-89-3.mol
更新日期 2024/12/17 11:16:00
885101-89-3 結構式 885101-89-3 結構式

基本信息

中文別名
4-[[(3-苯氧苯基)甲基]氨基]苯乙酸
4-[[(3-苯氧基苯基)甲基]氨基]苯丙酸
3-(4-((3-苯氧基芐基)氨基)苯基)丙酸
英文別名
GW9508
CS-618
GPR40 Agonist
GW9508, >=99%
GW9508 USP/EP/BP
885101-89-3(GW9508)
GW-9508
GW9508
GW 9508
4-(3-Phenoxybenzylamino)phenylpropionic acid
GPR40 Agonist - CAS 885101-89-3 - Calbiochem
3-(4-((3-Phenoxybenzyl)aMino)phenyl)propanoic acid
所屬類別
生物化工:GPR 激動劑

物理化學性質(zhì)

熔點90-92°C
儲存條件2-8°C
溶解度二甲基亞砜:>20mg/mL
形態(tài)白色粉末
顏色米白色
穩(wěn)定性Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
GHS05,GHS07,GHS09
警示詞危險
危險品標志Xn,N
危險類別碼22-37/38-41-50/53
安全說明26-39-60-61
危險品運輸編號UN 3077 9 / PGIII
WGK Germany3

應用領域

用途1
GW9508 is a GPR40 full agonist, used to regulate glucose in rats. Can be applied to the treatment of diabetes type 2. GPR120 selective and potent agonist also used in the treatment of diabetes type 2 due to GPR120鈥檚 ability to mediate GLP-1 secretion, insulin sensitization and anti-obesity effects.

常見問題列表

生物活性
GW9508 是一種有效的選擇性 G 蛋白偶聯(lián)受體 FFA1 (GPR40) 和 GPR40 激動劑,pEC50 值分別為 7.32 和 5.46。GW9508 對 GPR40 的選擇性是 GPR120 的 100 倍左右,對其他 GPCR,激酶,蛋白酶,整聯(lián)蛋白和 PPAR 無活性。GW9508 是一種葡萄糖敏感性胰島素促分泌劑和 ATP 敏感性鉀 (KATP) 通道開放劑。GW9508 具有抗炎和抗動脈粥樣硬化活性。
靶點

pEC50: 7.32 (GPR40) and 5.46 (GPR120)

體外研究

GW9508 stimulates intracellular Ca 2+ mobilization in HEK-293 cells expressing GPR40 (pEC 50 of 7.32) or GPR120 (pEC 50 of 5.46), but not in the parent HEK-293 cell line.
GW9508 produces a concentration-dependent increase (pEC 50 of 6.14) in glucose-stimulated insulin secretion at high glucose levels (25?mM). This resulted in a 1.52-fold increase in insulin secretion with 20?μM GW9508 in the presence of 25?mM glucose, compared with 25?mM glucose alone. The ability of GW9508 (10?μM) to enhance insulin secretion from MIN6 cells is significantly enhanced as glucose concentrations are increased.
GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. The inhibitory effect by GW9508 is abrogated by depletion of GPR40 with RNA interference. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes.

體內(nèi)研究

Administration of GW9508 200 (μM) topically to the skin suppresses ear swelling in a repeated hapten application model (BALB/c and C57BL/6 mice) and contact hypersensitivity with downregulation of CCL5 and CXCL10, respectively.

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