MK-7622
Based on 1 Customer Validation
MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC50 = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD).
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- Reinheit: 99.80%
- CAS. Nr.: 1227923-29-6
- Formel: C25H25N3O2
- Molecular Weight:399.48
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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mAChR1 |
MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC50 = 21 nM)[1].
MK-7622 shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium (EC50 = 2930 nM without ACh; PAM EC50 = 16 nM with ACh)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rhesus monkeys[1]
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Dosage:0.1, 0.3, 1.0 mg/kg
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Administration:p.o. once 5 hours before testing
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Result:Significantly attenuated scopolamine-induced impairment in difficult trials of rhesus monkeys' object retrieval detour task at 0.3 and 1.0 mg/kg.
Demonstrated dose-responsive effects in rhesus monkeys' qEEG: reduced theta, alpha, and sigma power, most robust in the first 8 hours; most affected delta power at 8-12 hours; modestly increased beta and gamma in the first 2 hours at lower doses.
Exhibited roughly dose-proportional exposures in rhesus monkeys; showed CSF concentrations consistent with free brain concentrations, serving as a surrogate.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1227923-29-6
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Appearance Solid
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Molecular Weight 399.48
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Formel C25H25N3O2
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Color Off-white to light yellow
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SMILES
O=C1N([C@@H]2[C@@H](O)CCCC2)C=NC3=C1C=C(CC4=CC=C(C)N=C4)C5=CC=CC=C53
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Synonyms
M1 receptor modulator
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 70 mg/mL (175.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Uslaner JM, et al. Preclinical to Human Translational Pharmacology of the Novel M1 Positive Allosteric Modulator MK-7622. J Pharmacol Exp Ther. 2018 Jun;365(3):556-566. [Content Brief]
[2]. Moran SP, et al. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. [Content Brief]
[3]. Beshore DC, et al. MK-7622: A First-in-Class M1Positive Allosteric Modulator Development Candidate. ACS Med Chem Lett. 2018 Apr 30;9(7):652-656. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5033 mL | 12.5163 mL | 25.0325 mL | 62.5814 mL |
| 5 mM | 0.5007 mL | 2.5033 mL | 5.0065 mL | 12.5163 mL | |
| 10 mM | 0.2503 mL | 1.2516 mL | 2.5033 mL | 6.2581 mL | |
| 15 mM | 0.1669 mL | 0.8344 mL | 1.6688 mL | 4.1721 mL | |
| 20 mM | 0.1252 mL | 0.6258 mL | 1.2516 mL | 3.1291 mL | |
| 25 mM | 0.1001 mL | 0.5007 mL | 1.0013 mL | 2.5033 mL | |
| 30 mM | 0.0834 mL | 0.4172 mL | 0.8344 mL | 2.0860 mL | |
| 40 mM | 0.0626 mL | 0.3129 mL | 0.6258 mL | 1.5645 mL | |
| 50 mM | 0.0501 mL | 0.2503 mL | 0.5007 mL | 1.2516 mL | |
| 60 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 1.0430 mL | |
| 80 mM | 0.0313 mL | 0.1565 mL | 0.3129 mL | 0.7823 mL | |
| 100 mM | 0.0250 mL | 0.1252 mL | 0.2503 mL | 0.6258 mL |
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