BB-Cl-Amidine - CAS:1802637-39-3

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BB-Cl-Amidine

目录号 : KCM12079 CAS No. : 1802637-39-3 纯度 : ≥95%

Data Sheet 产品使用指南

BB-Cl-Amidine is a modified version of Cl-amidine that retains the functional components but possesses a C-terminal benzimidazole group designed to limit proteolysis of the C-terminal amide. BB-Cl-Amidine irreversibly inactivates all four PAD subtypes (k/K = 16,100, 4,100, 6,800, and 13,300 Mmin for PAD1-4, respectively) by covalently modifying an active site cysteine that is important for its catalytic activity. The cellular potency of BB-Cl-amidine against PAD4 is increased 20-fold over the parent compound (EC = 8.8 µM versus >200 µM for Cl-amidine). BB-Cl-Amidine also has a significantly longer in vivo half-life than Cl-amidine (1.75 h versus ~15 min, respectively). Both compounds inhibit the formation of neutrophil extracellular traps without altering HO production by neutrophils. BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

BB-Cl-Amidine In-stock
CAY10727 In-stock
GSK106 (hydrochloride) In-stock
GSK121 (trifluoroacetate salt) In-stock
Cl-amidine hydrochloride In-stock

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生物活性

BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor.

IC₅₀&Target

PAD

体内研究

Treatment with BB-Cl-amidine subtly reduces splenomegaly in MRL/lpr mice, while there is a trend towards increased circulating levels of anti-NET antibodies with PAD inhibitor treatment. However, neither PAD inhibitor affected body weight or total IgG levels. Indeed, treatment with both Cl-amidine and BB-Cl-amidine significantly improves endothelium-dependent vasorelaxation. The BB-Cl-amidine group also shows a strong trend towards downregulation of IRGs. Treatment with either Cl-amidine or BB-Cl-amidine significantly improves muzzle alopecia, in many cases preventing it entirely.

Animal Model:	MRL/lpr mice
Dosage:	1 mg/kg.
Administration:	Subcutaneous injection daily from 8 to 14 weeks of age.
Result:	Significantly improved endothelium-dependent vasorelaxation and showed a strong trend towards downregulation of IRGs.

分子式

C₂₆H₂₆ClN₅O

分子量

459.97

CAS号

1802637-39-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (217.41 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1741 mL	10.8703 mL	21.7405 mL
5 mM	0.4348 mL	2.1741 mL	4.3481 mL
10 mM	0.2174 mL	1.0870 mL	2.1741 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)。-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 → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.44 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 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。
2.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.44 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。
3.

请依序添加每种溶剂：10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.52 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。

纯度： ≥95%

Data Sheet

产品使用指南

Knight JS, et al. Peptidylarginine deiminase inhibition disrupts NET formation and protects against kidney, skin and vascular disease in lupus-prone MRL/lpr mice. Ann Rheum Dis. 2015 Dec;74(12):2199-206.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器