| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
mAChR4
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|---|---|
| ln Vitro |
When compared to other receptors, PD 102807 (example 1) exhibits selectivity for the M4 muscarinic receptor that is 72-fold (M1), 38-fold (M2), 10-fold (M3), and 82-fold (M5) more selective[1]. In contrast to M1 (pKB=5.60), M2 (pKB=5.88), and M3 (pKB=6.39) receptor subtypes, PD 102807, a novel M4 selective antagonist, inhibits the M4 receptor-induced stimulation of [35S]-GTPγS binding to membrane G proteins with a pKB of 7.40, a value that is 63, 33, and 10 times higher[2]. A M4 mAChR preferring antagonist, PD-102807 has an affinity of 7–28 nM for M4 mAChRs, a selectivity of 14–36 for M4 over M3 mAChRs, and a selectivity of 76-2600 for M4 over M1, M2, and M5 mAChRs[3].
|
| ln Vivo |
Levodopa-induced dyskinesia (LID) is lessened by striatal perfusion of PD-102807 (3 μM), which also reduces nigral GABA and Glu as well as striatal Glu release[3].
|
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats[3]
Doses: 3 μM Route of Administration: Perfusion started 40 min prior to L-DOPA (6 mg/Kg plus 12 mg/Kg benserazide, sc) administration and continued until the end of experiment. Experimental Results: 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. decreased global Axial Limb Orolingual (ALO) Abnormal Involuntary Movements (AIM) expression from 70.75±5.64 to 25.38±6.64, Dramatically 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. |
| References |
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| Additional Infomation |
LSM-1888 is an indolyl carboxylic acid.
|
| Molecular Formula |
C23H24N2O4
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|---|---|
| Molecular Weight |
392.45
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| Exact Mass |
392.174
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| CAS # |
23062-91-1
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| PubChem CID |
4995951
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.34g/cm3
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| Boiling Point |
586ºC at 760 mmHg
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| Flash Point |
308.2ºC
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| Vapour Pressure |
1.02E-13mmHg at 25°C
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| Index of Refraction |
1.673
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| LogP |
4.048
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
616
|
| Defined Atom Stereocenter Count |
0
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| InChi Key |
VDDUJINYXKGZLV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H24N2O4/c1-4-28-23(26)20-13(2)24-18-7-8-19-17(21(18)20)12-25-10-9-14-11-15(27-3)5-6-16(14)22(25)29-19/h5-8,11,22,24H,4,9-10,12H2,1-3H3
|
| Chemical Name |
ethyl 17-methoxy-6-methyl-12-oxa-1,7-diazapentacyclo[11.8.0.03,11.04,8.014,19]henicosa-3(11),4(8),5,9,14(19),15,17-heptaene-5-carboxylate
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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