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(E/Z)-Sivopixant

Name: (E/Z)-Sivopixant
Brand: TargetMol
SKU: T9653
Price: 882 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.82%

货号 T9653Cas号 1640808-39-4

别名 (E/Z)-S-600918

(E/Z)-Sivopixant ((E/Z)-S-600918) 是一种有效的 P2X3 受体拮抗剂(IC50 为 4 nM)。(E/Z)-Sivopixant 可用于呼吸系统疾病研究。

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(E/Z)-Sivopixant

一键复制产品信息

很棒

纯度: 99.82%

货号 T9653 别名 (E/Z)-S-600918Cas号 1640808-39-4

(E/Z)-Sivopixant ((E/Z)-S-600918) 是一种有效的 P2X3 受体拮抗剂(IC50 为 4 nM)。(E/Z)-Sivopixant 可用于呼吸系统疾病研究。

规格	价格	库存
1 mg	¥ 882	现货
5 mg	¥ 2,230	现货
10 mg	¥ 3,230	现货
25 mg	¥ 4,920	现货
50 mg	¥ 6,720	现货
100 mg	¥ 9,120	现货
500 mg	¥ 17,800	现货
1 mL x 10 mM (in DMSO)	¥ 2,500	现货

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产品介绍

(E/Z)-Sivopixant AI Summary

(E/Z)-Sivopixant exhibits significant bioactivity as a potent antagonist at the P2X3 receptor, with an IC50 of 4.2 nM in human P2X3R and an IC50 of 4.0 nM at the rat P2X3 receptor. It shows functional selectivity for the P2X3 receptor over the P2X2 receptor with a selectivity ratio of 1100.0. In a rat model of neuropathic pain, it provides analgesic effects, evidenced by an ED50 of 0.4 mg/kg and 64.0% efficacy at 3 mg/kg orally (po). The compound demonstrates good oral bioavailability in rats, with F values of 52.8% and 76.8% at 1 mg/kg and 3 mg/kg dosages, respectively. Additionally, it has good solubility in JP2 fluid at pH 6.8 at 458.0 µg/mL and exhibits low protein binding in rat plasma (Fu = 0.01). Pharmacokinetically, it has a half-life of 10.1 hours and a clearance rate of 2.7 mL/min/kg in rats following intravenous (iv) administration at 1 mg/kg. (E/Z)-Sivopixant inhibits CYP enzymes with IC50 values above 20,000 nM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Furthermore, it shows low activity as an antagonist at the P2X1, P2X2, P2X4, and P2X7 receptors with IC50 values above 30,000 nM. In cell viability assays, the compound's effects vary; it promotes growth in HEK293T cells with growth rates from 0.2 to 0.97, but shows mixed results with human fibroblast and U2OS cell viability, ranging from inhibitory to stimulatory effects. Overall, (E/Z)-Sivopixant is a promising candidate for targeting P2X3 receptors with both analgesic and selective properties, favorable pharmacokinetics, and mixed effects on various cell lines' viability..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	(E/Z)-Sivopixant ((E/Z)-S-600918)is a potent P2X3 receptor antagonist, IC50 = 4 nM. (E/Z)-Sivopixant can be used for respiratory diseases research.
别名	(E/Z)-S-600918

化学信息

分子量	507.93
分子式	C₂₅H₂₂ClN₅O₅
CAS No.	1640808-39-4
Smiles	C[C@@H](Cn1c(=O)nc(Nc2ccc(Oc3ccccn3)cc2)n(Cc2ccc(Cl)cc2)c1=O)C(O)=O

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: 90 mg/mL (177.19 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.5 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	1.9688 mL	9.8439 mL	19.6878 mL	98.4388 mL
5 mM	0.3938 mL	1.9688 mL	3.9376 mL	19.6878 mL
10 mM	0.1969 mL	0.9844 mL	1.9688 mL	9.8439 mL
20 mM	0.0984 mL	0.4922 mL	0.9844 mL	4.9219 mL
50 mM	0.0394 mL	0.1969 mL	0.3938 mL	1.9688 mL
100 mM	0.0197 mL	0.0984 mL	0.1969 mL	0.9844 mL