Emraclidine, also known as CVL-231 and PF-06852231, is a novel, brain-penetrant, highly selective M4 receptor positive allosteric modulator in development for the treatment of schizophrenia.
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Name | Emraclidine |
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Iupac Chemical Name | 1-(2,4-dimethyl-5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-yl)-2-{1-[2-(trifluoromethyl)pyridin-4-yl]azetidin-3-yl}ethan-1-one |
Synonyms | Emraclidine, CVL-231; CVL 231; CVL231; PF-06852231; PF 06852231; PF06852231; |
Molecular Formula | C20H21F3N4O |
Molecular Weight | 390.40 |
Smile | O=C(N1CC2=NC(C)=CC(C)=C2C1)CC3CN(C4=CC(C(F)(F)F)=NC=C4)C3 |
InChiKey | DTCZNKWBDTXEBS-UHFFFAOYSA-N |
InChi | InChI=1S/C20H21F3N4O/c1-12-5-13(2)25-17-11-27(10-16(12)17)19(28)6-14-8-26(9-14)15-3-4-24-18(7-15)20(21,22)23/h3-5,7,14H,6,8-11H2,1-2H3 |
CAS Number | 2170722-84-4 |
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Packaging | Price | Availability | Purity | Shipping Time |
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1g | Get quote | Enquiry | 98% Min. | Enquiry |
Formulation | Off-white solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
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. |
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1: Krystal JH, Kane JM, Correll CU, Walling DP, Leoni M, Duvvuri S, Patel S, Chang I, Iredale P, Frohlich L, Versavel S, Perry P, Sanchez R, Renger J. Emraclidine, a novel positive allosteric modulator of cholinergic M4 receptors, for the treatment of schizophrenia: a two-part, randomised, double-blind, placebo-controlled, phase 1b trial. Lancet. 2022 Dec 17;400(10369):2210-2220. doi: 10.1016/S0140-6736(22)01990-0. PMID: 36528376.
2: Cookson J, Jonsson F. A new cholinergic mechanism for antipsychotics: emraclidine and M4 muscarinic receptors. Lancet. 2022 Dec 17;400(10369):2159-2161. doi: 10.1016/S0140-6736(22)02421-7. PMID: 36528365.
3: Tsapakis EM, Diakaki K, Miliaras A, Fountoulakis KN. Novel Compounds in the Treatment of Schizophrenia-A Selective Review. Brain Sci. 2023 Aug 11;13(8):1193. doi: 10.3390/brainsci13081193. PMID: 37626549; PMCID: PMC10452918.
4: Naguy A, Pridmore S, Alamiri B. The Future of Schizophrenia Psychopharmacotherapy: More Antipsychotic Atypicality? Guess So! Psychopharmacol Bull. 2023 Feb 28;53(1):55-57. PMID: 36873922; PMCID: PMC9981338.