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Tiaprofenic acid

Name: Tiaprofenic acid
Brand: TargetMol
SKU: T4561
Price: 108 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.51%

货号 T4561Cas号 33005-95-7

别名 噻洛芬酸, Tiaprofensaeure, Surgam, Acido tiaprofenico

Tiaprofenic acid (Acido tiaprofenico) 是可口服的非甾体抗炎药，通过抑制环氧化酶抑制前列腺素合成，可用于风湿性疾病的研究。

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Tiaprofenic acid

一键复制产品信息

很棒

纯度: 99.51%

货号 T4561 别名 噻洛芬酸, Tiaprofensaeure, Surgam, Acido tiaprofenicoCas号 33005-95-7

Tiaprofenic acid (Acido tiaprofenico) 是可口服的非甾体抗炎药，通过抑制环氧化酶抑制前列腺素合成，可用于风湿性疾病的研究。

规格	价格	库存
2 mg	¥ 108	现货
5 mg	¥ 152	现货
10 mg	¥ 236	现货
25 mg	¥ 395	现货
50 mg	¥ 581	现货
100 mg	¥ 858	现货
200 mg	¥ 1,270	现货
1 mL x 10 mM (in DMSO)	¥ 176	现货

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纯度: 99.51%

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COA HNMR LCMS 产品操作手册

产品介绍

Tiaprofenic acid AI Summary

Tiaprofenic acid exhibits a wide range of bioactivities and pharmacological properties. It inhibits CXCL8-induced chemotaxis of human polymorphonuclear cells by 7.0% at a concentration of 10e-8 M and shows substantial inhibition (>99.0%) of lipopolysaccharide-induced PGE-2 production at 10e-5 M. The compound induces genotoxicity in human embryonic kidney cells expressing luciferase-tagged ELG1, inhibits Histone Lysine Methyltransferase G9a and ELG1-dependent DNA repair, and affects HP1-beta Chromodomain Interactions with Methylated Histone Tails. It counters TGF-b cytotoxicity and inhibits firefly luciferase, leading to DNA re-replication in normal breast and colon adenocarcinoma cells. Furthermore, it acts as an inverse agonist of the GLP-1 receptor and activates BRCA1 expression. Tiaprofenic acid inhibits human tyrosyl-DNA phosphodiesterase 1 (TDP1) and blocks the entry of Ebola Virus, exhibiting antiviral activity against Foot and Mouth Disease Virus and SARS-CoV-2. In permeability studies, Tiaprofenic acid crossed the human Caco2 cell membrane with a logPapp value of -4.41, indicating its membrane permeability. It selectively exhibits activity in the UGT2B7 enzyme but not in UGT2B10 and UGT2B4. In clinical trials, it was found to have moderate liver toxicity, with a hepatotoxicity rate of 3.8%, though no severe or chronic liver conditions were observed. Against SARS-CoV-2, Tiaprofenic acid showed a low inhibition index of 0.07411 in Vero E6 cells and moderate potency with an IC50 value greater than 19952.62 nM in HRCE cells. The compound also inhibits the N-terminal His6-tagged recombinant human UCHL5 enzyme with 15.0% inhibition at 200 uM and an IC50 of 2946000.0 nM and shows 41.58% inhibition of human HDAC6 activity using a commercial peptide substrate but a -5.97% inhibition with a custom peptide substrate, suggesting substrate-dependent bioactivity. The compound's interactions extend to various human and rat receptors and enzymes, including binding affinities to ADRB2, DRD3, AVPR1A, and CNR1, and exhibiting agonist or antagonist activities at CHRM2, HTR2A, and ADRA1A. It also inhibits targets like PTGS1 and MAOA, demonstrating potency across these bioactivities with AC50 values ranging from nanomolar to micromolar concentrations..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Tiaprofenic acid (Acido tiaprofenico) is a non-steroidal anti-inflammatory drug used to treat pain, especially arthritic pain.
别名	噻洛芬酸, Tiaprofensaeure, Surgam, Acido tiaprofenico

化学信息

分子量	260.31
分子式	C₁₄H₁₂O₃S
CAS No.	33005-95-7
Smiles	CC(C(O)=O)c1ccc(s1)C(=O)c1ccccc1
密度	1.2959 g/cm3 (Estimated)
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: Insoluble

Ethanol: 30 mg/mL (115.25 mM), Sonication is recommended.

DMSO: 60 mg/mL (230.49 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.68 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.8416 mL	19.2079 mL	38.4157 mL	192.0787 mL
5 mM	0.7683 mL	3.8416 mL	7.6831 mL	38.4157 mL
10 mM	0.3842 mL	1.9208 mL	3.8416 mL	19.2079 mL
20 mM	0.1921 mL	0.9604 mL	1.9208 mL	9.6039 mL
50 mM	0.0768 mL	0.3842 mL	0.7683 mL	3.8416 mL
100 mM	0.0384 mL	0.1921 mL	0.3842 mL	1.9208 mL