Cl-amidine hydrochloride|cas:1373232-26-8|西域试剂

Cl-amidine hydrochloride,99.27%

产品编号：Bellancom-100574A| CAS NO：1373232-26-8| 分子式：C₁₄H₂₀Cl₂N₄O₂| 分子量：347.24

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货号	价格	库存与货期
Bellancom-100574A	￥1200.00	杭州北京（现货）
Bellancom-100574A	￥1900.00	杭州北京（现货）
Bellancom-100574A	￥3800.00	杭州北京（现货）
Bellancom-100574A	￥6100.00	杭州北京（现货）
Bellancom-100574A	￥9800.00	杭州北京（现货）

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Cl-amidine hydrochloride

产品介绍

Cl-amidine hydrochloride 是口服有效的 PAD 抑制剂，其对 PAD1、PAD3 和 PAD4 的 IC₅₀ 值分别为0.8 μM、 6.2 μM 和 5.9 μM。Cl-amidine hydrochloride 可诱导癌细胞的凋亡。Cl-amidine hydrochloride 可诱导 miR-16 (miRNA-16, microRNA-16)，引起细胞周期阻滞。Cl-Amidine hydrochloride 可阻断组蛋白 3 瓜氨酸化和中性粒细胞胞外陷阱的形成，并提高败血症小鼠的存活率。

生物活性

Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC₅₀ values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model^[4]^[5].

体外研究

Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (k_inact/K_I=13,000 M_-1•min-1 for PAD4).
Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine.
Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model^[4].

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

Apoptosis Analysis.

Cell Line:	TK6 lymphoblastoid cells and HT29 colon cancer cells.
Concentration:	0, 5, 10, 15, 20, 25, 50 μg/mL.
Incubation Time:	24 h.
Result:	Induced apoptosis dose-dependently.

体内研究
(In Vivo)

Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice.
Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently.

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

Animal Model:	C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:	75 mg/kg.
Administration:	IP once daily.
Result:	Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.

Animal Model:	C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:	5, 25, 75 mg/kg.
Administration:	Oral gavage once daily.
Result:	Led to significant reductions in the histology scores.

体内研究

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

Animal Model:	C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:	75 mg/kg.
Administration:	IP once daily.
Result:	Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.

Animal Model:	C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:	5, 25, 75 mg/kg.
Administration:	Oral gavage once daily.
Result:	Led to significant reductions in the histology scores.

体内研究

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

Animal Model:	C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:	75 mg/kg.
Administration:	IP once daily.
Result:	Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.

Animal Model:	C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
Dosage:	5, 25, 75 mg/kg.
Administration:	Oral gavage once daily.
Result:	Led to significant reductions in the histology scores.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (143.99 mM; Need ultrasonic)

H₂O : 50 mg/mL (143.99 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8799 mL	14.3993 mL	28.7985 mL
5 mM	0.5760 mL	2.8799 mL	5.7597 mL
10 mM	0.2880 mL	1.4399 mL	2.8799 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 (stored under nitrogen, away from moisture)。-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： PBS
Solubility: 5.5 mg/mL (15.84 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (3.60 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.60 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (3.60 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.60 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (3.60 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.60 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。