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RQ-00203078

Name: RQ-00203078
Brand: TargetMol
SKU: T2007
Price: 169 CNY
Availability: InStock
Rating: 5 (10 reviews)

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纯度: 99.6%

货号 T2007Cas号 1254205-52-1

RQ00203078是一种口服有效的TRPM8高选择性拮抗剂，对大鼠和人类TRPM8通道的IC50分别为 5.3 nM 和 8.3 nM。它对 TRPV1，TRPA1，TRPV4 或 TRPM2 通道基本没有抑制作用。

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RQ-00203078

一键复制产品信息

很棒

纯度: 99.6%

货号 T2007Cas号 1254205-52-1

RQ00203078是一种口服有效的TRPM8高选择性拮抗剂，对大鼠和人类TRPM8通道的IC50分别为 5.3 nM 和 8.3 nM。它对 TRPV1，TRPA1，TRPV4 或 TRPM2 通道基本没有抑制作用。

规格	价格	库存
1 mg	¥ 169	现货
2 mg	¥ 267	现货
5 mg	¥ 578	现货
10 mg	¥ 968	现货
25 mg	¥ 1,880	现货
50 mg	¥ 3,550	现货
100 mg	¥ 4,900	现货
500 mg	¥ 9,870	现货
1 mL x 10 mM (in DMSO)	¥ 692	现货

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产品介绍

RQ-00203078 AI Summary

RQ-00203078 exhibits a variety of bioactivities across multiple biological systems. It demonstrates potent antagonist activity at TRPM8 channels with an IC50 of 8.3 nM in humans and 5.8 nM in rats. In vivo, it displays significant antiallodynic activity in the icilin-induced wet-dog shake rat model with an ED50 of 0.65 mg/kg. Pharmacokinetic data in rats reveal a Cmax of 4145.26 nM at an oral dose of 3 mg/kg, with high oral bioavailability of 86% and a low fraction unbound (Fu) in plasma at 0.0031. In antiviral studies, RQ-00203078 significantly inhibits SARS-CoV-2-induced cytotoxicity in Caco-2 cells by 5.34% at 10 µM concentration after 48 hours, while in VERO-6 cells, it shows a minimal inhibition of 0.1% under similar conditions. Additionally, it inhibits the SARS-CoV-2 3CL-Pro protease by 2.544% at a concentration of 20 µM in a FRET assay. In HDAC6 enzymatic assays using both commercial and custom peptide substrates, RQ-00203078 shows slight inhibition percentages of -21.28% and -1.32%, respectively. Finally, regarding its influence on cell viability, it presents varying growth rates in different cell lines: from 0.33 to 0.93 in HEK293T cells, 0.75 to 0.99 in U2OS cells, and from -0.5 to 0.93 in human fibroblast cells, indicating a diverse impact on cell proliferation depending on the context..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist.
靶点活性	TRPV4:10 μM, TRPM8 (human channels):8.3 nM, TRPM8 (rat channels):5.3 nM

化学信息

分子量	554.85
分子式	C₂₁H₁₃ClF₆N₂O₅S
CAS No.	1254205-52-1
Smiles	OC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1ncc(cc1Cl)C(F)(F)F
密度	1.588 g/cm3 (Predicted)

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

DMSO: 50 mg/mL (90.11 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.6 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8023 mL	9.0114 mL	18.0229 mL	90.1144 mL
5 mM	0.3605 mL	1.8023 mL	3.6046 mL	18.0229 mL
10 mM	0.1802 mL	0.9011 mL	1.8023 mL	9.0114 mL
20 mM	0.0901 mL	0.4506 mL	0.9011 mL	4.5057 mL
50 mM	0.0360 mL	0.1802 mL	0.3605 mL	1.8023 mL