2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein Membrane Transporter/Ion Channel
  3. Phosphodiesterase (PDE) mAChR Potassium Channel
  4. CPL500036

CPL500036 是一种口服有效、可穿透血脑屏障的磷酸二酯酶 10A (PDE10A) 抑制剂，其 IC50 值为 1 nM (文献 1) 和 35 nM (文献 2)。CPL500036 是 M2 毒蕈碱受体 (M2 muscarinic receptor) 的负变构调节剂，其 IC50 为 9.2 μM。CPL500036 可改变基底神经节环路中的环核苷酸水平，抑制 cAMP 和 cGMP 的水解，并抑制 hERG 钾通道尾电流。CPL500036 可诱导大鼠出现僵住症，逆转损伤引起的对侧前肢使用障碍。CPL500036 可用于精神分裂症、帕金森病以及左旋多巴诱导的运动障碍的相关研究。

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CPL500036

CPL500036 Chemical Structure

CAS No. : 1829530-11-1

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CPL500036 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CPL500036 is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC50 values of 1 nM (Reference 1) and 35 nM (Reference 2). CPL500036 acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC50 of 9.2 μM. CPL500036 alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. CPL500036 induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. CPL500036 can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia[1][2].

IC50 & Target[1][2]

PDE10A

1 nM (IC50)

PDE10A

35 nM (IC50)

体外研究
(In Vitro)

CPL500036 (0.1-10 μM; 5 min) 可抑制转染 hERG-HEK-293 细胞中的 hERG 尾电流，其 IC25 为 3.2 μM[1]。
CPL500036 (0.0457-100 μM; 14 days) 在浓度高达 100 μM 时均不会影响心脏类球体的关键健康参数，但在人多能干细胞来源的 3D 心脏类球体中会损伤 DNA 结构，其 IC50 为 37.4 μM[1]。
CPL500036 (8 nM-60 μM; 72 h) 在 NCI-H1299、HepG2 和 SH-SY5Y 细胞系中，浓度高达 60 μM 时仍无细胞毒性[1]。

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

CPL500036 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax (Plasma) AUC0-24 T1/2 (Plasma) Cmax (Brain) Tmax (Brain)
Rat[1] 3 mg/kg p.o. 237.8 ng/mL 5.8 h 1,618.0 ng·h/mL 6.4 h 94.3 ng/mL 6.8 h
Dog[1] 1.5 mg/kg p.o. 98.3 ng/mL 1.3 h 199.4 ng·h/mL 2.1 h / /
体内研究
(In Vivo)

CPL500036 (0.15-2 mg/kg；口服；单次给药) 可在雄性 Sprague-Dawley 大鼠中诱导剂量依赖性僵住症[1]。
CPL500036 (0.1-0.3 mg/kg；口服；单次急性给药，连续 16 天联合 Levodopa (HY-N0304)/Benserazide (HY-121275)) 可呈剂量依赖性改善 6-羟基多巴胺损伤大鼠的感觉运动障碍[2]。

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

Animal Model: Sprague-Dawley (male, ~300 g)[1]
Dosage: 0.15 mg/kg; 0.3 mg/kg; 0.6 mg/kg; 2 mg/kg
Administration: p.o.; single dose
Result: Did not induce catalepsy at 0.15 mg/kg.
Induced a low cataleptogenic effect only at 210 min and 240 min post-administration at 0.3 mg/kg.
Induced catalepsy from 120 min to 240 min post-administration at 0.6 mg/kg, with effect less than positive control haloperidol.
Produced a strong cataleptogenic effect comparable to haloperidol at 2 mg/kg.
Confirmed minimum effective dose (MED) for catalepsy as 0.6 mg/kg via AUC data.
Animal Model: Wistar Han (male, initial body weight 270-300 g, unilateral medial forebrain bundle lesion with 6-hydroxydopamine)[2]
Dosage: 0.1 mg/kg (acute single dose; chronic daily combined with L-DOPA/benserazide); 0.3 mg/kg (acute single dose; chronic daily combined with L-DOPA/benserazide)
Administration: p.o.; single acute dose; daily for 16 days (combined with L-DOPA/benserazide)
Result: Dose-dependently reversed impaired forelimb use in the stepping test after acute administration.
Completely restored forelimb use symmetry in the cylinder test during the second post-dose testing session at 0.3 mg/kg acute dose.
Did not affect vibrissae test deficits or lesion-induced catalepsy at either acute dose.
Significantly improved impaired forelimb performance in the vibrissae test when combined acutely with L-DOPA at 0.1 mg/kg.
Reduced L-DOPA-induced contralateral rotations when combined acutely with L-DOPA at 0.3 mg/kg.
Completely reversed forelimb asymmetry in the vibrissae test after chronic combined treatment at 0.3 mg/kg.
Did not alter L-DOPA's antiparkinsonian effects in the stepping, catalepsy, or rotation tests at either chronic dose.
Significantly improved impaired forelimb use in the stepping test in the OFF phase post-chronic treatment at 0.3 mg/kg combined with L-DOPA compared to lesioned rats.
分子量

341.37

Formula

C19H15N7
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

CPL500036 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:

CPL5000361829530-11-1CPL 500036CPL-500036Phosphodiesterase (PDE)mAChRPotassium ChannelMuscarinic acetylcholine receptorKcsAHepG2basal-ganglia circuitsPDE10AcAMPPhosphodiesterase 10Ahuman muscarinic M2 receptorhuman 3D cardiac spheroidshERG potassium channelcGMPNCI-H1299Inhibitorinhibitorinhibit

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