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MedKoo Cat#: 522634 | Name: MK-7622
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MK-7622 is a cholinesterase inhibitor under evaluation for the treatment of Alzheimer's disease. No studies have been published on this compound in the peer-reviewed literature or other publicly available documents. In October 2013, Merck began a Phase 2 trial in the United States to evaluate the compound's tolerability and efficacy as a symptomatic adjunct to donepezil therapy in patients with probable AD as diagnosed by two conventional diagnostic criteria, the NINCDS-ADRDA and DSM-IV.

Chemical Structure

MK-7622
MK-7622
CAS#1227923-29-6

Theoretical Analysis

MedKoo Cat#: 522634

Name: MK-7622

CAS#: 1227923-29-6

Chemical Formula: C25H25N3O2

Exact Mass: 399.1947

Molecular Weight: 399.49

Elemental Analysis: C, 75.16; H, 6.31; N, 10.52; O, 8.01

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 800.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 1,950.00 Ready to ship
1g USD 2,950.00 2 weeks
2g USD 4,450.00 2 weeks
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Related CAS #
No Data
Synonym
MK7622; MK 7622; MK-7622.
IUPAC/Chemical Name
3-((1S,2S)-2-hydroxycyclohexyl)-6-((6-methylpyridin-3-yl)methyl)benzo[h]quinazolin-4(3H)-one
InChi Key
JUVQLZBJFOGEEO-GOTSBHOMSA-N
InChi Code
InChI=1S/C25H25N3O2/c1-16-10-11-17(14-26-16)12-18-13-21-24(20-7-3-2-6-19(18)20)27-15-28(25(21)30)22-8-4-5-9-23(22)29/h2-3,6-7,10-11,13-15,22-23,29H,4-5,8-9,12H2,1H3/t22-,23-/m0/s1
SMILES Code
O=C1N([C@@H]2[C@@H](O)CCCC2)C=NC3=C1C=C(CC4=CC=C(C)N=C4)C5=CC=CC=C53
Appearance
White to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator.
In vitro activity:
To assess the in vitro activity of the M1 PAMs used in this study, compounds were tested using CHO cells stably expressing the M1 receptor. The previously published M1 PAM PF-06764427 [10, 16] (Fig. 1a, left) and Merck’s MK-7622 [27] (Fig.(Fig.1a,1a, right) were evaluated for their ability to mobilize intracellular calcium (Ca2+) in the M1-CHO cells. The raw calcium traces (Fig. 1b) indicate that both PF-06764427 and MK-7622 induce robust increases in Ca2+ mobilization in the absence of an orthosteric mAChR agonist. Interestingly, there is a similar degree of intracellular Ca2+ mobilization with MK-7622 alone (Ago EC50 2930 nM ± 95, Fig. 1d). Both PF-06764427 (PAM EC50 30 nM ± 3, Fig. 1e) and MK-7622 (PAM EC50 16 nM ± 4, Fig. 1f) act as potent and selective [10] (Supplemental Fig. 1) M1 PAMs in the presence of the orthosteric agonist ACh. Therefore, in addition to their PAM activity, both PF-06764427 and MK-7622 have significant intrinsic agonist activity in this cell-based Ca2+ mobilization assay. Neuropsychopharmacology. 2018 Jul; 43(8): 1763–1771. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6006294/
In vivo activity:
In light of the finding that both PF-06764427 and MK-7622 have robust allosteric agonist activity in both cell line and native tissue assays, it was hypothesized that MK-7622 would induce behavioral convulsions in a manner similar to those observed with PF06764427. Therefore, a dose-escalation study in mice was performed to assess seizure liability of the M1 ago-PAM MK-7622. Consistent with the previous study with PF-06764427, 30 and 100 mg/kg MK-7622 induces robust convulsions that reached stage 5 on the modified Racine scale [16, 26, 32] in wild-type but not M1 KO mice (Fig. 5a). Interestingly, MK-7622 (1, 3, and 10 mg/kg) did not significantly improve performance in the novel object recognition task (p = 0.9110, one-way ANOVA) (Fig. 5c).Collectively, these findings suggest that M1 ago-PAMs, such as MK-7622 and PF-06764427, induce behavioral convulsions that are not observed with PAMs lacking agonist activity such as VU0453595. Neuropsychopharmacology. 2018 Jul; 43(8): 1763–1771. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6006294/
Solvent mg/mL mM comments
Solubility
DMSO 100.0 250.33
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 399.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Uslaner JM, Kuduk SD, Wittmann M, Lange HS, Fox SV, Min C, Pajkovic N, Harris D, Cilissen C, Mahon C, Mostoller K, Warrington S, Beshore DC. Preclinical to Human Translational Pharmacology of the Novel M1 Positive Allosteric Modulator MK7622. J Pharmacol Exp Ther. 2018 Jun;365(3):556-566. doi: 10.1124/jpet.117.245894. Epub 2018 Mar 21. PMID: 29563325. 2. Moran SP, Dickerson JW, Cho HP, Xiang Z, Maksymetz J, Remke DH, Lv X, Doyle CA, Rajan DH, Niswender CM, Engers DW, Lindsley CW, Rook JM, Conn PJ. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. doi: 10.1038/s41386-018-0033-9. Epub 2018 Mar 14. PMID: 29581537; PMCID: PMC6006294. 3. Uslaner JM, Kuduk SD, Wittmann M, Lange HS, Fox SV, Min C, Pajkovic N, Harris D, Cilissen C, Mahon C, Mostoller K, Warrington S, Beshore DC. Preclinical to Human Translational Pharmacology of the Novel M1 Positive Allosteric Modulator MK7622. J Pharmacol Exp Ther. 2018 Jun;365(3):556-566. doi: 10.1124/jpet.117.245894. Epub 2018 Mar 21. PMID: 29563325 4. . Moran SP, Dickerson JW, Cho HP, Xiang Z, Maksymetz J, Remke DH, Lv X, Doyle CA, Rajan DH, Niswender CM, Engers DW, Lindsley CW, Rook JM, Conn PJ. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. doi: 10.1038/s41386-018-0033-9. Epub 2018 Mar 14. PMID: 29581537; PMCID: PMC6006294.
In vitro protocol:
1. Uslaner JM, Kuduk SD, Wittmann M, Lange HS, Fox SV, Min C, Pajkovic N, Harris D, Cilissen C, Mahon C, Mostoller K, Warrington S, Beshore DC. Preclinical to Human Translational Pharmacology of the Novel M1 Positive Allosteric Modulator MK7622. J Pharmacol Exp Ther. 2018 Jun;365(3):556-566. doi: 10.1124/jpet.117.245894. Epub 2018 Mar 21. PMID: 29563325. 2. Moran SP, Dickerson JW, Cho HP, Xiang Z, Maksymetz J, Remke DH, Lv X, Doyle CA, Rajan DH, Niswender CM, Engers DW, Lindsley CW, Rook JM, Conn PJ. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. doi: 10.1038/s41386-018-0033-9. Epub 2018 Mar 14. PMID: 29581537; PMCID: PMC6006294.
In vivo protocol:
1.. Uslaner JM, Kuduk SD, Wittmann M, Lange HS, Fox SV, Min C, Pajkovic N, Harris D, Cilissen C, Mahon C, Mostoller K, Warrington S, Beshore DC. Preclinical to Human Translational Pharmacology of the Novel M1 Positive Allosteric Modulator MK7622. J Pharmacol Exp Ther. 2018 Jun;365(3):556-566. doi: 10.1124/jpet.117.245894. Epub 2018 Mar 21. PMID: 29563325. 2. Moran SP, Dickerson JW, Cho HP, Xiang Z, Maksymetz J, Remke DH, Lv X, Doyle CA, Rajan DH, Niswender CM, Engers DW, Lindsley CW, Rook JM, Conn PJ. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. doi: 10.1038/s41386-018-0033-9. Epub 2018 Mar 14. PMID: 29581537; PMCID: PMC6006294.