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  4. UPF-648

UPF-648是犬尿氨酸3-单加氧酶(KMO)有效抑制剂，1uM浓度下能达到约81%的抑制效果，对犬尿素转氨酶KAT无抑制作用。

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UPF-648 Chemical Structure

UPF-648 Chemical Structure

CAS No. : 213400-34-1

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规格 价格 是否有货 数量
10 mM * 1 mL in Ethanol ￥484
In-stock
2 mg ￥340
In-stock
5 mg ￥690
In-stock
10 mg ￥1100
In-stock
25 mg ￥2300
In-stock
50 mg ￥3680
In-stock
100 mg ￥5880
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of UPF-648:

UPF-648 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

UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.

体外研究
(In Vitro)

BFF 122 inhibited KAT activity almost completely at both 1 and 0.1 mM. The effect was still remarkable at 0.01 mM (70 ± 1 % inhibition). At the same three concentrations, BFF 122 did not affect KMO activity significantly. In contrast, UPF 648 totally blocked KMO at 0.1 and 0.01 mM and was still highly active at 0.001 mM (81 ± 10 % inhibition), but the compound was essentially ineffective at blocking KAT activity[1].
UPF 648 binds close to the FAD cofactor and perturbs the local active-site structure, preventing productive binding of the substrate l-kynurenine. Functional assays and targeted mutagenesis reveal that the active-site architecture and UPF 648 binding are essentially identical in human KMO, validating the yeast KMO-UPF 648 structure as a template for structure-based drug design[3].

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

UPF-648 相关抗体:
体内研究
(In Vivo)

Applying an identical experimental design, separate rats were used to study the effect of KMO inhibition on the de novo synthesis of KP metabolites in the lesioned striatum. These animals were bilaterally injected with 0.1 mM UPF 648 and 3H-kynurenine in PBS. 0.1 mM UPF 648 significantly reduced the neosynthesis of 3-HK and QUIN in the lesioned striatum (by 77 % and 66%, respectively) and moderately (27%) but significantly increased the de novo formation of KYNA[1].
Administered to pregnant rats or mice on the last day of gestation, UPF 648 (50 mg/kg, i.p.) produced qualitatively similar changes (i.e., large increases in kynurenine and KYNA and reductions in 3-HK and QUIN) in the brain and liver of the offspring. Rat pups delivered by UPF 648-treated mothers and immediately exposed to neonatal asphyxia showed further enhanced brain KYNA levels[2].
UPF 648, has an IC50 of 20 nM and provides protection against intrastriatal QUIN injections in kynurenine aminotransferase (KAT II) deficient mice. UPF 648 treatment also shifts KP metabolism towards enhanced neuroprotective KYNA formation[3].

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

259.09

Formula

C11H8Cl2O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

Ethanol 中的溶解度 : ≥ 50 mg/mL (192.98 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8597 mL 19.2983 mL 38.5966 mL
5 mM 0.7719 mL 3.8597 mL 7.7193 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

UPF-648 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol 1 mM 3.8597 mL 19.2983 mL 38.5966 mL 96.4916 mL
5 mM 0.7719 mL 3.8597 mL 7.7193 mL 19.2983 mL
10 mM 0.3860 mL 1.9298 mL 3.8597 mL 9.6492 mL
15 mM 0.2573 mL 1.2866 mL 2.5731 mL 6.4328 mL
20 mM 0.1930 mL 0.9649 mL 1.9298 mL 4.8246 mL
25 mM 0.1544 mL 0.7719 mL 1.5439 mL 3.8597 mL
30 mM 0.1287 mL 0.6433 mL 1.2866 mL 3.2164 mL
40 mM 0.0965 mL 0.4825 mL 0.9649 mL 2.4123 mL
50 mM 0.0772 mL 0.3860 mL 0.7719 mL 1.9298 mL
60 mM 0.0643 mL 0.3216 mL 0.6433 mL 1.6082 mL
80 mM 0.0482 mL 0.2412 mL 0.4825 mL 1.2061 mL
100 mM 0.0386 mL 0.1930 mL 0.3860 mL 0.9649 mL
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:

UPF-648213400-34-1UPF648UPF 648OthersInhibitorinhibitorinhibit

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产品名称：
UPF-648
目录号：
HY-15600
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