2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. PD 102807

PD 102807 是一种 M4 毒蕈碱受体拮抗剂，IC50 为 90.7 nM。PD 102807 抑制 M1、M2、M3、M5 毒蕈碱受体，IC50 分别为 6558.7、3440.7、950.0 和 7411.7 nM。具有抗运动障碍作用。

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PD 102807 Chemical Structure

PD 102807 Chemical Structure

CAS No. : 23062-91-1

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PD 102807 相关抗体

Top Publications Citing Use of Products

查看 mAChR 亚型特异性产品:

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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

PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively[1]. Antidyskinetic effect.

IC50 & Target

mAChR4

 

体外研究
(In Vitro)

PD 102807 (example 1) shows selectivity for M4 muscarinic receptor with 72-fold (M1), 38-fold (M2), 10-fold (M3), and 82-fold (M5) more selective compared to the other receptors[1].
PD 102807, a novel M4 selective antagonist, counteracts the M4 receptor-induced stimulation of [35S]-GTPγS binding to membrane G proteins with a pKB of 7.40, a value which is 63-, 33- and 10-fold higher than those display at M1 (pKB=5.60), M2 (pKB=5.88) and M3 (pKB=6.39) receptor subtypes, respectively[2].
PD-102807 is an M4 mAChR preferring antagonist, with 7-28 nM affinity for M4 mAChRs, a 14-36-fold selectivity for M4 over M3 mAChRs, and 76-2600-fold selectivity for M4 over M1, M2 and M5 mAChRs[3].

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

PD 102807 相关抗体:
体内研究
(In Vivo)

Striatal perfusion of PD-102807 (3 μM) alleviates levodopa-induced dyskinesia (LID) and inhibits nigral GABA and Glu along with striatal Glu release[3].

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

Animal Model: Male Sprague-Dawley rats[3]
Dosage: 3 μM
Administration: Administration:Perfusion started 40 min prior to L-DOPA (6 mg/Kg plus 12 mg/Kg benserazide, s.c.) administration and continued until the end of experiment.
Result: Basal dialysate levels in PD-102807 experiment were 19.19±2.62 nM and 47.77±3.42 nM for GABA and Glu in SNr, respectively, and 41.38±4.25 nM for Glu in striatum.
Reduced global Axial Limb Orolingual (ALO) Abnormal Involuntary Movements (AIM) expression from 70.75±5.64 to 25.38±6.64, significantly attenuating limb, axial and orolingual AIMs at 3 μM.
Inhibited the L-DOPA-induced rise of substantia nigra pars reticulata (SNr) GABA, SNr Glu, and striatal Glu at 3 μM.
分子量

392.45

Formula

C23H24N2O4
CAS 号
性状

固体

颜色

Off-white to light yellow

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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (318.51 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5481 mL 12.7405 mL 25.4810 mL
5 mM 0.5096 mL 2.5481 mL 5.0962 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 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

纯度: 98.52%

COA (198 KB) HNMR (264 KB) LCMS (95 KB)

产品使用指南 (1538 KB)
参考文献

PD 102807 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5481 mL 12.7405 mL 25.4810 mL 63.7024 mL
5 mM 0.5096 mL 2.5481 mL 5.0962 mL 12.7405 mL
10 mM 0.2548 mL 1.2740 mL 2.5481 mL 6.3702 mL
15 mM 0.1699 mL 0.8494 mL 1.6987 mL 4.2468 mL
20 mM 0.1274 mL 0.6370 mL 1.2740 mL 3.1851 mL
25 mM 0.1019 mL 0.5096 mL 1.0192 mL 2.5481 mL
30 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1234 mL
40 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5926 mL
50 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2740 mL
60 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0617 mL
80 mM 0.0319 mL 0.1593 mL 0.3185 mL 0.7963 mL
100 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 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:

PD 10280723062-91-1PD102807PD-102807mAChRMuscarinic acetylcholine receptorM4muscarinicAntidyskineticInhibitorinhibitorinhibit

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