货号	规格	价格	上海	北京	珠海	重庆	武汉
S89266-5mg促销	98.00%	￥1500.00 ￥1200.00 S89266-5mg ￥1200.00 现货	5 5	-	-	-	-
S89266-10mg促销	98.00%	￥2170.00 ￥1730.00 S89266-10mg ￥1730.00 现货	6 6	-	-	-	-
S89266-25mg促销	98.00%	￥3690.00 ￥2950.00 S89266-25mg ￥2950.00 现货	5 5	-	-	-	-
S89266-100mg促销	≥98%	￥8590.00 ￥6870.00 S89266-100mg ￥6870.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Danicamtiv (MYK-491, SAR 440181) 是一种新型的心脏肌球蛋白(cardiac myosin) 激活剂，可增强心肌细胞收缩

靶点：

cardiac myosin;Myosin

体外研究：

Danicamtiv metabolism pathways in vitro included CYP-mediated amide-cleavage, N-demethylation, as well as isoxazole- and piperidine-ring-opening.Danicamtiv show high permeability and no efflux in a Caco-2 cell line

体内研究：

Danicamtiv selectively enhances cardiac actomyosin activity, the molecular force‐generating unit of the sarcomere, prolonging contraction while preserving actin-myosin detachment, allowing relaxation, and without impacting Ca2+ homeostasis

细胞实验：

Cell lines: Caco-2/TC7 cell lines, male human hepatocytes Concentrations: 1 µM, 10 µM Incubation Time: 0, 2, 4, 6, 8, and 24 h Method: Incubations of plated human hepatocytes (1.4 million viable cells/mL, 0.2 mL, n = 2) with danicamtiv (1 µM) are performed in a cell culture incubator (37 °C, 5% CO₂, 95% humidity). Incubations are quenched with 200 µL of ACN containing 50 nM CBZ internal standard at incubation times 0, 2, 4, 6, 8, and 24 h. Supernatants are analysed by LC-MS/MS for the analysis of danicamtiv from preclinical pharmacokinetic studies. Caco-2 cells are seeded on 96-well cell culture plates with PCF membrane filters and maintained for 21/25 days post-seeding with culture medium exchanged every 4th day. The bidirectional permeability (efflux) experiments are conducted on a TECAN automated liquid handling platform. Danicamtiv is examined at 1 and 10 μM, permeability controls are tested at 10 μM, and efflux controls are tested either at 2 μM or 1 μM in duplicate wells

动物实验：

Animal Models: male beagle dogs Dosages: 2–3 mg/kg Administration: p.o. , i. pl.

参考文献：

1. Adriaan A Voors, et al. Effects of danicamtiv, a novel cardiac myosin activator, in heart failure with reduced ejection fraction: experimental data and clinical results from a phase 2a trial. Eur J Heart Fail. 2020 Sep;22(9):1649-1658. 2. Grillo MP, et al. Preclinical in vitro and in vivo pharmacokinetic properties of danicamtiv, a new targeted myosin activator for the treatment of dilated cardiomyopathy. Xenobiotica. 2021 Feb;51(2):222-238.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.297 ml	11.483 ml	22.966 ml
5 mM	0.459 ml	2.297 ml	4.593 ml
10 mM	0.23 ml	1.148 ml	2.297 ml
50 mM	0.046 ml	0.23 ml	0.459 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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