L002|cas:321695-57-2|西域试剂

L002,99.02%

产品编号：Bellancom-100671| CAS NO：321695-57-2| 分子式：C₁₅H₁₅NO₅S| 分子量：321.35

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货号	价格	库存与货期
Bellancom-100671	￥950.00	杭州北京（现货）
Bellancom-100671	￥1390.00	杭州北京（现货）
Bellancom-100671	￥3150.00	杭州北京（现货）
Bellancom-100671	￥5500.00	杭州北京（现货）
Bellancom-100671	￥9350.00	杭州北京（现货）

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L002

产品介绍

L002 是一种有效的，细胞可渗透的，可逆的和特定的乙酰转移酶 p300(KAT3B) 抑制剂，IC₅₀ 为 1.98μM。 L002 结合乙酰辅酶 A 口袋并竞争性抑制 FATp300 催化结构域，阻断组蛋白乙酰化和 p53 乙酰化，且抑制 STAT3 激活。L002 有潜力用于高血压引起的心脏肥大和纤维化的研究。

生物活性

L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC₅₀ of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.

体外研究

L002 also has weak inhibitory effects against PCAF and GCN5 (IC₅₀s =35 and 34 µM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

L002 (intraperitoneal injection; 20 μg/gm body weight; every 3rd day; 2 weeks) reverses hypertension‐induced cardiac hypertrophy and fibrosis by treatment of mice after inducing hypertension for two weeks significantly.It also reduces the levels of perivascular and interstitial collagen in the myocardium compared to non-treated hypertensive mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Wild‐type C57BL/6 male mice planted with osmotic minipumps ( Angiotensin II 1500 ng/kg/min) for 4 weeks
Dosage:	20 μg/gm body weight; every 3rd day; 2 weeks
Administration:	Intraperitoneal injection
Result:	Reversed hypertension-induced cardiac fibrosis in mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Wild‐type C57BL/6 male mice planted with osmotic minipumps ( Angiotensin II 1500 ng/kg/min) for 4 weeks
Dosage:	20 μg/gm body weight; every 3rd day; 2 weeks
Administration:	Intraperitoneal injection
Result:	Reversed hypertension-induced cardiac fibrosis in mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (194.49 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1119 mL	15.5594 mL	31.1187 mL
5 mM	0.6224 mL	3.1119 mL	6.2237 mL
10 mM	0.3112 mL	1.5559 mL	3.1119 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (6.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.47 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液