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

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. Antidyskinetic effect.

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PD 102807

PD 102807 構造式

CAS 番号 : 23062-91-1

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PD 102807 関連抗体

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mAChR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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製品説明

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

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
54 1
Compound: PD-102807
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
[PMID: 18395442]
CHO IC50
>1 3
Compound: PD-102807
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
[PMID: 18395442]
CHO IC50
> 1 3
Compound: PD-102807
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
[PMID: 18395442]
CHO EC50
54 1
Compound: PD-102807
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
[PMID: 18395442]
体外実験

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].

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

PD 102807 関連抗体
体内実験

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

MedChemExpress (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

分子式

C23H24N2O4
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C(C)NC(C=C2)=C1C3=C2OC4N(CCC5=C4C=CC(OC)=C5)C3)OCC
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (318.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2548 mL 1.2740 mL 2.5481 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 98.52%

COA (253 KB) HNMR (264 KB) LCMS (95 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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PD 102807 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品名:
PD 102807
製品番号:
HY-107646
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