1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. Arginase
  3. OATD-02

OATD-02 是一种口服有效的、竞争性的、可逆的、非共价结合的 Arginase12 的双重抑制剂。OATD-02 是一种缓释抑制剂,能有效阻断细胞内精氨酸酶的活性,IC50s 值分别为 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), 和 28 nM (rARG1)。OATD-02 可消除两种精氨酸酶诱导的肿瘤免疫抑制。OATD-02 可用于黑色素瘤的研究。

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OATD-02 Chemical Structure

OATD-02 Chemical Structure

CAS No. : 2146132-73-0

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study[1].

IC50 & Target

20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), 28 nM (rARG1)

体外研究
(In Vitro)

OATD-02 在 BMDM 细胞中抑制小鼠 ARG 的IC50 为 912.9 nM,在 CHO-K1 细胞中抑制人 ARG2 的IC50 为 171.6 nM,在人原代肝细胞中抑制 hARG1 的IC50 为 13 mM[1]

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

体内研究
(In Vivo)

OATD-02 (10 mg/kg, 口服) 在体内具有较强的长效药效,在小鼠、大鼠和犬中的口服生物利用度分别为 13%、30% 和 61%[1]
OATD-02 (5 mg/kg,口服) 在给药结束1周后仍能维持血浆中L -精氨酸浓度增加 4 倍[1]
OATD-02 (每天2次, 50 mg/kg,口服) 可抑制 B16F10 原位异种移植肿瘤的生长[1]

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

Animal Model: B16F10 orthotopic xenograft tumor model[1]
Dosage: Twice per day at 50 mg/kg for 15days
Administration: Oral gavage
Result: Inhibited tumor growth (TGI 46%).
分子量

272.15

Formula

C12H25BN2O4

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
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  • 稀释计算器

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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.

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产品名称:
OATD-02
目录号:
HY-155108
需求量: