Zetomipzomib maleate KZR-616 maleate|cas:2170983-62-5|西域试剂

Zetomipzomib maleate KZR-616 maleate,99.90%

产品编号：Bellancom-114419A| CAS NO：2170983-62-5| 分子式：C₃₄H₄₆N₄O₁₂| 分子量：702.75

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-114419A		￥18000.00	杭州北京（现货）

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Zetomipzomib maleate KZR-616 maleate

产品介绍

Zetomipzomib (KZR-616) maleate 是首创的免疫蛋白酶体 (immunoproteasome) 抑制剂，选择性靶向免疫蛋白酶体亚基 LMP7 (IC₅₀: 39/57 nM=hLMP7/mLMP7) 和 LMP2 (IC₅₀: 131/179 nM=hLMP2/mLMP2)。Zetomipzomib maleate 用于多种自身免疫性疾病的潜力。

生物活性

Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC₅₀: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC₅₀: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases.

体外研究

Zetomipzomib maleate also inhibits MECL-1 subunit (IC₅₀=623 nM) and constitutive proteasome β5 subunit (IC₅₀=688 nM). Zetomipzomib maleate maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. Zetomipzomib maleate (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC).
Zetomipzomib maleate is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587).

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

体内研究

Zetomipzomib maleate (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model.

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

Animal Model:	7-8 week old female BALB/c mice (CAIA model)
Dosage:	I.v.; Dosing was repeated on days 6, 8, 11, and 13 until for 15 day
Administration:	5 mg/kg
Result:	Showed efficacy in the anticollagen antibody induced arthritis (CAIA) model.

体内研究

Zetomipzomib maleate (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model.

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

Animal Model:	7-8 week old female BALB/c mice (CAIA model)
Dosage:	I.v.; Dosing was repeated on days 6, 8, 11, and 13 until for 15 day
Administration:	5 mg/kg
Result:	Showed efficacy in the anticollagen antibody induced arthritis (CAIA) model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (355.75 mM; Need ultrasonic)

H₂O : 50 mg/mL (71.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4230 mL	7.1149 mL	14.2298 mL
5 mM	0.2846 mL	1.4230 mL	2.8460 mL
10 mM	0.1423 mL	0.7115 mL	1.4230 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 (sealed storage, 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: 100 mg/mL (142.30 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: ≥ 2.08 mg/mL (2.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.96 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (2.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.96 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 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