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883031-03-6

中文名稱 883031-03-6
英文名稱 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
CAS 883031-03-6
分子式 C26H28F3N3O2
分子量 471.51
MOL 文件 883031-03-6.mol
更新日期 2024/12/16 11:47:41
883031-03-6 結(jié)構(gòu)式 883031-03-6 結(jié)構(gòu)式

基本信息

中文別名
化合物HC-067047
英文別名
HC 067047
HC-067047 >=98% (HPLC)
HC-067047
HC 067047
HC067047
1221277-90-2
2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
1H-Pyrrole-3-carboxamide, 2-methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-

物理化學(xué)性質(zhì)

儲存條件2-8°C
溶解度在DMSO中的溶解度≥15mg/mL
形態(tài)粉末
顏色白色至棕褐色
穩(wěn)定性從購買之日起 2 年內(nèi)保持穩(wěn)定。 DMSO 或乙醇溶液可在 -20℃ 下保存長達(dá) 3 個月。

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301-H319
危險品標(biāo)志T
危險類別碼25-36
安全說明26-45
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3
883031-03-6價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-100208883031-03-6
HC-067047
883031-03-65mg660元
2024/11/08HY-100208883031-03-6
HC-067047
883031-03-610mM * 1mLin DMSO685元
2024/11/08HY-100208883031-03-6
HC-067047
883031-03-610mg1100元

常見問題列表

生物活性
HC-067047是一種選擇性的TRPV4拮抗劑,對人TRPV4,大鼠TRPV4和小鼠TRPV4的IC50分別為48 nM,133 nM和17 nM。
靶點
TargetValue
mTRPV4
(Cell-free assay)
17 nM
hTRPV4
(Cell-free assay)
48 nM
rTRPV4
(Cell-free assay)
133 nM
體外研究

HC-067047 (1 μM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells.
HC-067047 (1 μM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein.
HC-067047 (1 μM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation.
HC-067047 (1 μM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis.

RT-PCR

Cell Line: HEI-OC1 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: The mRNA expression was significantly decreased.

Western Blot Analysis

Cell Line: HEI-OC1 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: The expression of TRPV4 protein was significantly decreased.

Cell Proliferation Assay

Cell Line: HEI-OC1 cells
Concentration: 1 μM
Incubation Time: 48 hours
Result: Inhibited cell proliferation.

Apoptosis Analysis

Cell Line: HEI-OC1 cells
Concentration: 1 μM
Incubation Time: 48 hours
Result: Promoted cell apoptosis.
體內(nèi)研究

HC-067047 (0-50 mg/kg; intraperitoneal injection; for 30 minutes; cyclophosphamide-treated WT and Trpv4 ?/? mice, and naive WT mice) treatment increases functional bladder capacity and reduces micturition frequency in WT mice with cystitis. HC-067047 do not affect bladder function in Trpv4 ?/? mice.

Animal Model: Cyclophosphamide-treated WT and Trpv4 ?/? mice, and naive WT mice
Dosage: 0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg
Administration: Intraperitoneal injection; for 30 minutes
Result: Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4 ?/? mice.
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