2. Metabolic Enzyme/Protease
  3. IMPDH
  4. VX-148

VX-148，一种口服有效的免疫抑制剂，是一种非竞争性肌苷-5'-单磷酸脱氢酶 (IMPDH) 抑制剂，其对 IMPDH Ⅱ 和 IMPDH Ⅰ 的 Ki 值分别为6 和 14 nM。VX-148 能显著抑制人外周血单核细胞 (PBMC) 在T细胞丝裂原 (PHA) 或B细胞丝裂原 (SPAS) 刺激下的增殖，IC50 分别为82 nM和73 nM。VX-148 对淋巴细胞 (如L1210、Jurkat T细胞、Raji B细胞) 具有高选择性，IC50 值为 245-511 nM，但对非淋巴系细胞无显著毒性。VX-148 可在小鼠模型中抑制抗体应答，在异体皮肤移植模型中显著延长移植皮肤的存活时间。VX-148 可以用于自身免疫性疾病 (如类风湿关节炎、银屑病) 和器官移植抗排斥研究。

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VX-148

VX-148 Chemical Structure

CAS No. : 297730-05-3

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VX-148 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VX-148 is an orally active immunosuppressant, which is a non-competitive inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor with Ki values for IMPDH Ⅱ and IMPDH Ⅰ of 6 and 14 nM respectively. VX-148 can significantly inhibit the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated by T-cell mitogen (PHA) or B-cell mitogen (SPAS), with IC50 values of 82 nM and 73 nM respectively. VX-148 has high selectivity for lymphocytes (such as L1210, Jurkat T cells, and Raji B cells), with IC50 values ranging from 245 to 511 nM, but has no significant toxicity to non-lymphoid cells. VX-148 can inhibit antibody responses in mouse models and significantly prolong the survival time of transplanted skin in allogeneic skin transplantation models. VX-148 can be used in the research of autoimmune diseases (such as rheumatoid arthritis, psoriasis) and organ transplantation anti-rejection[1][2].

IC50 & Target[2]

IMPDH1

6 nM (Ki)

IMPDH2

14 nM (Ki)

分子量

435.48

Formula

C23H25N5O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

VX-148 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VX-148297730-05-3VX148VX 148IMPDHInosine-5’-monophosphate dehydrogenaseMPAmycophenolic acidCsAcyclosporin ASPASstaphylococcal protein A immobilized on Sepharose CL-4BDMSOInhibitorinhibitorinhibit

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目录号：
HY-118917
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