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BB-Cl-Amidine hydrochloride Sale

目录号 : GC35480

A PAD4 inhibitor

BB-Cl-Amidine hydrochloride Chemical Structure

Cas No.:2436747-41-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,474.00
现货
1mg
¥675.00
现货
5mg
¥1,350.00
现货
10mg
¥2,340.00
现货
25mg
¥5,310.00
现货
50mg 待询 待询
100mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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.1 BB-Cl-Amidine irreversibly inactivates all four PAD subtypes (kinact/KI = 16,100, 4,100, 6,800, and 13,300 M-1min-1 for PAD1-4, respectively) by covalently modifying an active site cysteine that is important for its catalytic activity.2,3 The cellular potency of BB-Cl-amidine against PAD4 is increased 20-fold over the parent compound (EC50 = 8.8 ?M versus >200 ?M 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 H2O2 production by neutrophils.1 BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice.

1.Knight, J.S., Subramanian, V., O'Dell, A.A., et al.Peptidylarginine deiminase inhibition disrupts NET formation and protects against kidney, skin and vascular disease in lupus-prone MRL/lpr miceAnn. Rheum. Dis.74(12)2199-2206(2015) 2.Luo, Y., Arita, K., Bhatia, M., et al.Inhibitors and inactivators of protein arginine deiminase 4: Functional and structural characterizationBiochemistry45(39)11727-11736(2006) 3.Muth, A., Subramanian, V., Beaumont, E., et al.Development of a selective inhibitor of protein arginine deiminase 2.J. Med. Chem.60(7)3198-3211(2017)

Chemical Properties

Cas No. 2436747-41-8 SDF
Canonical SMILES O=C(C1=CC=C(C2=CC=CC=C2)C=C1)N[C@H](C3=NC4=CC=CC=C4N3)CCCNC(CCl)=N.Cl
分子式 C26H27Cl2N5O 分子量 496.43
溶解度 DMSO: ≥ 100 mg/mL (201.44 mM) 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0144 mL 10.0719 mL 20.1438 mL
5 mM 0.4029 mL 2.0144 mL 4.0288 mL
10 mM 0.2014 mL 1.0072 mL 2.0144 mL
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