2. Metabolic Enzyme/Protease
  3. KMO
  4. CHDI-340246

CHDI-340246 是一种具有口服活性的犬尿氨酸单加氧酶 (KMO) 抑制剂。CCHDI-340246 可阻断 KMO 活性，改变犬尿氨酸通路的代谢流量，抑制 3-羟基犬尿氨酸和喹啉酸的生成，升高犬尿氨酸和犬尿喹啉酸水平，并可恢复亨廷顿病转基因小鼠模型中的电生理异常。CHDI-340246 可用于亨廷顿病的相关研究。

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CHDI-340246

CHDI-340246 Chemical Structure

CAS No. : 1426319-74-5

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CHDI-340246 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

CHDI-340246 is an orally active kynurenine monooxygenase (KMO) inhibitor. CHDI-340246 blocks KMO activity, alters the metabolic flux of the kynurenine pathway, inhibits the production of 3-hydroxykynurenine and quinolinic acid, elevates the levels of kynurenine and kynurenic acid, and restores electrophysiological abnormalities in transgenic mouse models of Huntington's disease. CHDI-340246 can be used in studies related to Huntington's disease[1][2][3].

体外研究
(In Vitro)

CHDI-340246 可强效抑制啮齿动物肝脏中的犬尿氨酸-3-单加氧酶 (KMO)，其 IC50 为 0.5 nM[2]。
CHDI-340246 可抑制细胞 KMO 活性，在原代大鼠小胶质细胞中的 IC50 为 63.81 nM，在人外周血单个核细胞 (PBMCs) 中为 89.73 nM，在过表达小鼠、人或大鼠 KMO 的 CHO 细胞中为 20-80 nM[2]。
CHDI-340246 (记录前 20 分钟给药，给药浓度 1 μM，全程维持至 LTP 记录结束) 可急性挽救 8 周龄 R6/2 小鼠脑片中海马 CA3:CA1 的 LTP 缺陷，且不会影响 R6/2 或野生型脑片的基础谷氨酸能传递[2]。
CHDI-340246 (100 nM; 15-30 min) 可急性恢复 7-8 周龄 R6/2 小鼠纹状体 SPN 的异常膜兴奋性 (使膜超极化并降低膜电阻)[2]。

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

CHDI-340246 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-t T1/2 CL Vdss F Tmax (Plasma) T1/2 (Plasma) Tmax (Brain) Cmax (Brain) T1/2 (Brain)
Mice[1] 5 mg/kg i.v. / / 43 μM·h / 0.40 L/h/kg 0.44 L/kg / 0.083 h 1.40 h 0.083 h 0.94 μM 0.84 h
Mice[1] 10 mg/kg p.o. / 67 μM 73 μM·h / / / 60 % 0.25 h 3.2 h 0.50 h 0.81 μM 1.1 h
Rat[1] 5 mg/kg i.v. / / 73 μM·h / 0.29 L/h/kg 0.32 L/kg / 0.083 h 1.8 h 0.083 h 1.60 μM 0.7 h
Rat[1] 10 mg/kg p.o. / 23 μM 91 μM·h / / / 64 % 1.0 h 2.4 h 1.0 h 0.42 μM 1.7 h
Dog[1] 2.5 mg/kg i.v. 0.083 h 49.7 μM 88 μM·h 1.8 h 0.11 L/h/kg 0.23 L/kg / / / / / /
Dog[1] 5.0 mg/kg p.o. 0.67 h 22 μM 120 μM·h 3.6 h / / 68 % / / / / /
Cynomolgus Monkey[1] 3 mg/kg i.v. 0.083 h 104 μM 220 μM·h 9.41 h 0.045 L/h/kg 0.31 L/kg / / / / / /
Cynomolgus Monkey[1] 3 mg/kg p.o. 3.38 h 188 μM 166 μM·h 4.82 h / / 75 % / / / / /
体内研究
(In Vivo)

CHDI-340246 (0-100 mg/kg；口服；单次) 可剂量依赖性地调控 Q175 杂合子亨廷顿病模型小鼠纹状体犬尿氨酸通路代谢物，在高剂量下可使 Kyn 和 KynA 持续升高[2]。
CHDI-340246 (30 mg/kg；口服；单次给药；于给予 Kyn 前 30 分钟预给药) 可抑制野生型小鼠的中枢 KMO 活性，显著降低 Kyn 诱导的纹状体细胞外 3-OH-Kyn 和 Quin 水平升高[2]。
CHDI-340246 (0-100 mg/kg；口服；每日 2 次；持续 4-8 周) 可提高雄性小鼠的存活率，部分改善纹状体谷氨酸能输入缺陷 (以 mEPSC 频率为检测指标)，但无法持续改善其行为缺陷或脑体积损失，仅在最高剂量下能使 R6/2 亨廷顿病模型小鼠的纹状体肌酸水平部分恢复正常[2]。

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

Animal Model: Q175 heterozygous, wild-type (male)[2]
Dosage: 30 mg/kg; 60 mg/kg; 100 mg/kg
Administration: p.o.; single dose
Result: Reached striatal Cmax of Kyn 75-280 nM, KynA 15-30 nM, and AA 15-30 nM in Q175 heterozygous mice.
Reached 3-OH-Kyn Cmax 1.6-2 nM from a baseline of 0.8 nM in Q175 heterozygous mice.
Showed higher AUC values for Kyn and KynA at 60 and 100 mg/kg than at 30 mg/kg in Q175 heterozygous mice, driven by longer exposure.
Showed saturation of Cmax values for Kyn and KynA at doses above 30 mg/kg in Q175 heterozygous mice.
Had higher Kyn AUC values in wild-type mice than Q175 heterozygous mice at all doses tested.
Animal Model: wild-type[2]
Dosage: 30 mg/kg
Administration: p.o.; single dose; pre-administered 30 minutes prior to Kyn
Result: Reduced the Kyn-induced elevation of brain extracellular 3-OH-Kyn levels by 75-90%.
Reduced the Kyn-induced elevation of brain extracellular Quin levels by 60-80%.
Animal Model: R6/2 transgenic, wild-type littermates (equal gender split, 4 weeks old)[2]
Dosage: 10 mg/kg; 30 mg/kg; 60 mg/kg; 100 mg/kg
Administration: p.o.; twice daily; 8 weeks
Result: Did not produce consistent effects on locomotor function, grip strength, rotarod performance, or open field activity in R6/2 mice.
Improved median survival rates in male R6/2 mice treated with 60 or 100 mg/kg compared to vehicle-treated male R6/2 mice.
Showed no significant effects on whole brain, striatal, or cortical volume via MRI.
Normalized striatal creatine levels towards wild-type levels at the 100 mg/kg dose via MRS.
分子量

290.70

Formula

C14H11ClN2O3
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

CHDI-340246 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

CHDI-3402461426319-74-5CHDI340246CHDI 340246KMOKynurenine-3-monooxygenaseR6/2 mouse slicesstriatal SPNsHuntington's diseasehuman PBMCsprimary rat microgliaCHO cellstransgenic mouse modelskynurenine monooxygenaseQ175 heterozygous Huntington's disease model micecynomolgus monkey hepatocytesInhibitorinhibitorinhibit

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